Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
1324 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
16154396 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
16197727.0 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
44285019 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
57514683 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
91898441 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL441738 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
DB04931 302 None 19 Human Functional pEC50 = 10.8 10.8 -14 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm00018a005
CHEMBL413212 215515 None 0 Human Functional pEC50 = 10.7 10.7 3 4
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
CHEMBL428615 215921 None 0 Human Functional pEC50 = 10.7 10.7 1 5
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
1324 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16154396 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
16197727.0 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
44285019 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
57514683 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
91898441 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
CHEMBL441738 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
DB04931 302 None 19 Human Functional pEC50 = 10.7 10.7 -14 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None None 10.1021/jm030111j
155527254 171353 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1038 17 14 11 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.8b00238
CHEMBL4460053 171353 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1038 17 14 11 -0.6 CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.8b00238
57646411 76949 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070245 76949 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1739 49 24 20 -1.7 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
1323 2688 None 38 Mouse Functional pEC50 = 10.4 10.4 -1 7
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
92432 2688 None 38 Mouse Functional pEC50 = 10.4 10.4 -1 7
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 10.4 10.4 -1 7
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
1323 2688 None 38 Human Functional pEC50 = 10.4 10.4 -33 7
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
92432 2688 None 38 Human Functional pEC50 = 10.4 10.4 -33 7
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL430239 2688 None 38 Human Functional pEC50 = 10.4 10.4 -33 7
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
118722941 116306 None 0 Mouse Functional pEC50 = 10.3 10.3 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358549 116306 None 0 Mouse Functional pEC50 = 10.3 10.3 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722937 116302 None 0 Mouse Functional pEC50 = 10.3 10.3 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358545 116302 None 0 Mouse Functional pEC50 = 10.3 10.3 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722933 116299 None 0 Mouse Functional pEC50 = 10.2 10.2 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358541 116299 None 0 Mouse Functional pEC50 = 10.2 10.2 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
1323 2688 None 38 Mouse Functional pEC50 = 10.2 10.2 -1 7
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
92432 2688 None 38 Mouse Functional pEC50 = 10.2 10.2 -1 7
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 10.2 10.2 -1 7
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
155551846 175238 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1589 48 22 20 -3.2 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.8b00238
CHEMBL4569789 175238 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1589 48 22 20 -3.2 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.8b00238
CHEMBL415661 215658 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL2371851 212598 None 0 Mouse Functional pEC50 = 10.2 10.2 -1 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O 10.1021/jm0490843
118722944 116309 None 0 Mouse Functional pEC50 = 10.2 10.2 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358552 116309 None 0 Mouse Functional pEC50 = 10.2 10.2 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1323 2688 None 38 Mouse Functional pEC50 = 10.1 10.1 -1 7
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
92432 2688 None 38 Mouse Functional pEC50 = 10.1 10.1 -1 7
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL430239 2688 None 38 Mouse Functional pEC50 = 10.1 10.1 -1 7
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
44310104 81619 None 0 Mouse Functional pEC50 = 10.1 10.1 -4 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
CHEMBL216295 81619 None 0 Mouse Functional pEC50 = 10.1 10.1 -4 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1040 16 13 13 -1.5 CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0303608
1324 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16154396 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
16197727.0 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
44285019 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
57514683 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
91898441 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
DB04931 302 None 19 Mouse Functional pEC50 = 10.0 10.0 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm701093y
118722930 116297 None 0 Mouse Functional pEC50 = 10.0 10.0 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358539 116297 None 0 Mouse Functional pEC50 = 10.0 10.0 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL412495 215458 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
16746823 18164 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 679 6 0 6 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL1269576 18164 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 679 6 0 6 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL2372570 212730 None 0 Human Functional pEC50 = 10.0 10.0 -1 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O 10.1021/jm9017866
CHEMBL407809 215145 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
90643803 111806 None 0 Human Functional pEC50 = 9.9 9.9 -3 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Human Functional pEC50 = 9.9 9.9 -3 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
10408 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 23 Human Functional pEC50 = 9.9 9.9 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
1323 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
92432 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
1323 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
92432 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.9 9.9 -33 7
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
118722926 116294 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358535 116294 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
1324 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
1324 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16154396 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16197727 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
16197727.0 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
44285019 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
57514683 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
91898441 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
DB04931 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None None 10.1021/jm0492756
CHEMBL5090946 217775 None 0 Human Functional pEC50 = 9.9 9.9 -4 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
172449425 195974 None 0 Human Functional pEC50 = 9.9 9.9 123 4
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5414451 195974 None 0 Human Functional pEC50 = 9.9 9.9 123 4
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1148 14 16 18 -2.8 C[C@@H]1NC(=O)c2cc(-c3cn([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)nn3)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
118722931 116298 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358540 116298 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
118722938 116303 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358546 116303 None 0 Mouse Functional pEC50 = 9.9 9.9 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722942 116307 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358550 116307 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
118722943 116308 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358551 116308 None 0 Mouse Functional pEC50 = 9.9 9.9 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1034 17 13 13 -1.1 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
1324 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
16154396 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
16197727 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
16197727.0 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
44285019 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
57514683 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
91898441 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
DB04931 302 None 19 Human Functional pEC50 = 9.9 9.9 -14 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None None 10.1021/jm201489a
127036484 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136532 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
1324 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16154396 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727.0 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
44285019 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
57514683 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
91898441 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
DB04931 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
1324 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
16154396 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
16197727.0 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
44285019 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
57514683 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
91898441 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
DB04931 302 None 19 Mouse Functional pEC50 = 9.9 9.9 -10 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0490843
57646437 76950 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684621 76950 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929804 76950 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070246 76950 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1855 51 23 23 -2.2 CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
127036484 136532 None 0 Mouse Functional pEC50 = 9.8 9.8 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL3735690 136532 None 0 Mouse Functional pEC50 = 9.8 9.8 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1024 17 14 11 -1.0 CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2015.10.095
CHEMBL266879 213165 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm0501432
57646441 76948 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070243 76948 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1706 46 22 20 -1.4 CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL1688107 211293 None 0 Mouse Functional pEC50 = 9.8 9.8 1 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL5083551 217358 None 0 Human Functional pEC50 = 9.8 9.8 -10 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL2369484 212086 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL3646885 214483 None 0 Human Functional pEC50 = 9.7 9.7 74 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118722927 116295 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358536 116295 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3287329 213770 None 0 Human Functional pEC50 = 9.7 9.7 1 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
1323 2688 None 38 Human Functional pEC50 = 9.7 9.7 -33 7
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
92432 2688 None 38 Human Functional pEC50 = 9.7 9.7 -33 7
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.7 9.7 -33 7
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c01587
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm501027w
44415914 139357 None 0 Human Functional pEC50 = 9.7 9.7 5 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL379054 139357 None 0 Human Functional pEC50 = 9.7 9.7 5 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 762 16 6 7 1.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
10408 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
5329 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
9941379.0 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
CHEMBL2070241 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
DB11653 720 None 23 Human Functional pEC50 = 9.7 9.7 -1 4
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/jm201489a
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm301253y
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/jm101425m
1324 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16154396 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
16197727.0 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
44285019 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
57514683 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
91898441 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
DB04931 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None None 10.1021/jm049579s
CHEMBL405087 215001 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1324 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
16154396 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
16197727.0 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
44285019 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
57514683 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
91898441 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
DB04931 302 None 19 Human Functional pEC50 = 9.7 9.7 -14 8
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL2372859 212759 None 1 Mouse Functional pEC50 = 9.7 9.7 2 2
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm501027w
90643808 111810 None 0 Human Functional pEC50 = 9.7 9.7 -14 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111810 None 0 Human Functional pEC50 = 9.7 9.7 -14 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None None 10.1021/jm010524p
1324 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727.0 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 302 None 19 Mouse Functional pEC50 = 9.7 9.7 -10 8
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16132144 211738 None 29 Human Functional pEC50 = 9.7 9.7 -12 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
16133793 211738 None 29 Human Functional pEC50 = 9.7 9.7 -12 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
44273719 211738 None 29 Human Functional pEC50 = 9.7 9.7 -12 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.7 9.7 -12 8
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm00018a005
CHEMBL5080489 217177 None 0 Human Functional pEC50 = 9.7 9.7 1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
118722936 116301 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358544 116301 None 0 Mouse Functional pEC50 = 9.7 9.7 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
50899078 18161 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 623 4 0 5 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL1269573 18161 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 623 4 0 5 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL2373515 212838 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
90643802 111805 None 0 Human Functional pEC50 = 9.6 9.6 -14 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 9.6 9.6 -14 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3646890 214488 None 0 Human Functional pEC50 = 9.6 9.6 72 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
10408 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 23 Human Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
56659456 63722 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 1 4 6.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801215 63722 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 1 4 6.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1 10.1016/j.bmcl.2010.06.062
CHEMBL408257 215164 None 0 Human Functional pEC50 = 9.6 9.6 2 2
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
90643804 111807 None 0 Human Functional pEC50 = 9.6 9.6 -8 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Human Functional pEC50 = 9.6 9.6 -8 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL264352 213076 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL1688107 211293 None 0 Mouse Functional pEC50 = 9.6 9.6 1 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
172461542 196823 None 0 Human Functional pEC50 = 9.6 9.6 17 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5432868 196823 None 0 Human Functional pEC50 = 9.6 9.6 17 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 961 12 14 11 -0.7 C[C@H]1NC(=O)c2cc(C(=N)N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5087839 217610 None 0 Human Functional pEC50 = 9.6 9.6 2 3
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
1324 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16154396 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16197727 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
16197727.0 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
44285019 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
57514683 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
91898441 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
DB04931 302 None 19 Mouse Functional pEC50 = 9.6 9.6 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00053
CHEMBL267900 213196 None 0 Human Functional pEC50 = 9.6 9.6 5 2
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL491870 216565 None 0 Human Functional pEC50 = 9.6 9.6 -9 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
118722932 115582 None 0 Mouse Functional pEC50 = 9.5 9.5 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3352878 115582 None 0 Mouse Functional pEC50 = 9.5 9.5 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1038 33 13 11 1.2 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
90643805 111808 None 0 Human Functional pEC50 = 9.5 9.5 1 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Human Functional pEC50 = 9.5 9.5 1 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
1324 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
16154396 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
16197727 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
16197727.0 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
44285019 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
57514683 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
91898441 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
DB04931 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm030452x
118735099 118863 None 0 Human Functional pEC50 = 9.5 9.5 4 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421676 118863 None 0 Human Functional pEC50 = 9.5 9.5 4 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 746 15 9 6 1.6 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
118735101 118865 None 0 Human Functional pEC50 = 9.5 9.5 9 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421678 118865 None 0 Human Functional pEC50 = 9.5 9.5 9 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 824 15 9 6 2.4 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
44415913 79982 None 0 Human Functional pEC50 = 9.5 9.5 -4 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212614 79982 None 0 Human Functional pEC50 = 9.5 9.5 -4 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 736 16 6 7 0.8 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL385556 214814 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL3037885 213385 None 0 Human Functional pEC50 = 9.5 9.5 -1 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(03)00114-8
1324 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16154396 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16197727 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
16197727.0 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
44285019 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
57514683 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
91898441 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
DB04931 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.0c00561
CHEMBL3646880 214479 None 0 Human Functional pEC50 = 9.5 9.5 29 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O nan
CHEMBL5090285 217743 None 0 Human Functional pEC50 = 9.5 9.5 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3358542 214028 None 0 Mouse Functional pEC50 = 9.5 9.5 2 2
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(C)=O)C(N)=O 10.1021/jm501027w
1324 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727.0 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 302 None 19 Mouse Functional pEC50 = 9.5 9.5 -10 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL429236 215977 None 0 Mouse Functional pEC50 = 9.5 9.5 -15 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
44416057 81222 None 0 Human Functional pEC50 = 9.5 9.5 1 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215833 81222 None 0 Human Functional pEC50 = 9.5 9.5 1 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 745 17 6 7 0.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
137637283 156071 None 0 Human Functional pEC50 = 9.5 9.5 2 3
Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4061566 156071 None 0 Human Functional pEC50 = 9.5 9.5 2 3
Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins
ChEMBL 984 15 12 10 -0.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
122194229 124050 None 0 Mouse Functional pEC50 = 9.5 9.5 -14 4
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL3629347 124050 None 0 Mouse Functional pEC50 = 9.5 9.5 -14 4
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
1323 2688 None 38 Human Functional pEC50 = 9.5 9.5 -33 7
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
92432 2688 None 38 Human Functional pEC50 = 9.5 9.5 -33 7
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.5 9.5 -33 7
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None None 10.1021/acs.jmedchem.8b00170
CHEMBL415165 215636 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None None 10.1021/jm0501432
56666386 63723 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 1 4 6.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801216 63723 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 1 4 6.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1 10.1016/j.bmcl.2010.06.062
56676638 63714 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 0 4 6.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801146 63714 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 655 4 0 4 6.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1 10.1016/j.bmcl.2010.06.062
CHEMBL414965 215626 None 0 Mouse Functional pEC50 = 9.4 9.4 -8 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
11993702 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
11993702.0 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
5416 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
9272 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
CHEMBL3301624 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
DB11700 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00095
1324 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16154396 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16197727 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
16197727.0 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
44285019 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
57514683 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
91898441 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
DB04931 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.6b01707
11993702 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
11993702.0 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
5416 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
9272 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
CHEMBL3301624 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
DB11700 3593 None 20 Human Functional pEC50 = 9.4 9.4 -2 5
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None None 10.1021/acs.jmedchem.2c00793
1324 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16154396 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
16197727.0 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
44285019 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
57514683 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
91898441 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
DB04931 302 None 19 Human Functional pEC50 = 9.4 9.4 -14 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL491870 216565 None 0 Mouse Functional pEC50 = 9.4 9.4 3 4
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
90643806 111809 None 0 Human Functional pEC50 = 9.4 9.4 -12 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 9.4 9.4 -12 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
1324 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16154396 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16197727 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
16197727.0 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
44285019 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
57514683 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
91898441 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
DB04931 302 None 19 Mouse Functional pEC50 = 9.4 9.4 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00856
CHEMBL3646891 214489 None 0 Human Functional pEC50 = 9.4 9.4 30 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
16172929 215461 None 14 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL412536 215461 None 14 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
6918780 63487 None 0 Human Functional pEC50 = 9.4 9.4 204 2
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
CHEMBL179836 63487 None 0 Human Functional pEC50 = 9.4 9.4 204 2
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 637 10 2 6 3.6 CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
CHEMBL386081 214835 None 0 Mouse Functional pEC50 = 9.4 9.4 -23 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010061n
172441600 195257 None 0 Human Functional pEC50 = 9.4 9.4 5 4
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@H](C(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL5399539 195257 None 0 Human Functional pEC50 = 9.4 9.4 5 4
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 943 11 12 10 -0.0 C#Cc1ccc2c(c1)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@H](C(N)=O)CS2 10.1021/acs.jmedchem.2c01587
CHEMBL444219 216391 None 0 Mouse Functional pEC50 = 9.4 9.4 4 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 9.4 9.4 -5 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL267794 213192 None 0 Mouse Functional pEC50 = 9.4 9.4 -13 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL405335 215016 None 0 Mouse Functional pEC50 = 9.4 9.4 -2 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
CHEMBL5090670 217767 None 0 Human Functional pEC50 = 9.3 9.3 3 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
1324 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16154396 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
16197727.0 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
44285019 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
57514683 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
91898441 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
DB04931 302 None 19 Mouse Functional pEC50 = 9.3 9.3 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01894
CHEMBL2070244 211643 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
122194229 124050 None 0 Mouse Functional pEC50 = 9.3 9.3 -14 4
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.10.095
CHEMBL3629347 124050 None 0 Mouse Functional pEC50 = 9.3 9.3 -14 4
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay
ChEMBL 1646 50 23 21 -4.1 CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.10.095
44416106 141533 None 0 Human Functional pEC50 = 9.3 9.3 4 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384176 141533 None 0 Human Functional pEC50 = 9.3 9.3 4 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 617 12 4 5 1.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44448629 167561 None 0 Rat Functional pEC50 = 9.3 9.3 3 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167561 None 0 Rat Functional pEC50 = 9.3 9.3 3 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL3646882 214481 None 0 Human Functional pEC50 = 9.3 9.3 35 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O nan
172441036 195202 None 0 Human Functional pEC50 = 9.3 9.3 5 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5398659 195202 None 0 Human Functional pEC50 = 9.3 9.3 5 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 944 11 12 11 -0.1 C[C@H]1NC(=O)c2cc(C#N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
1324 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL413912 215560 None 0 Human Functional pEC50 = 9.3 9.3 -7 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.07.046
1324 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16154396 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
16197727.0 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
44285019 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
57514683 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
91898441 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
DB04931 302 None 19 Human Functional pEC50 = 9.3 9.3 -14 8
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None None 10.1016/s0960-894x(03)00552-3
CHEMBL5080784 217194 None 0 Human Functional pEC50 = 9.3 9.3 -2 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL264132 213065 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cncn2C)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
45487403 199891 None 0 Mouse Functional pEC50 = 9.3 9.3 -53 4
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569693 199891 None 0 Mouse Functional pEC50 = 9.3 9.3 -53 4
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 788 22 9 7 2.4 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL414718 215611 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
127047475 139836 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
132991507 139836 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL3798421 139836 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL428801 215933 None 0 Human Functional pEC50 = 9.2 9.2 -21 5
Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm00018a005
118722939 116304 None 0 Mouse Functional pEC50 = 9.2 9.2 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358547 116304 None 0 Mouse Functional pEC50 = 9.2 9.2 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
10146211 64350 None 0 Human Functional pEC50 = 9.2 9.2 61 3
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 64350 None 0 Human Functional pEC50 = 9.2 9.2 61 3
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
56669819 63712 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 4 0 3 7.0 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801144 63712 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 4 0 3 7.0 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1 10.1016/j.bmcl.2010.06.062
49862748 15155 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 657 5 0 6 5.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1 10.1016/j.bmcl.2010.06.068
CHEMBL1209799 15155 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 657 5 0 6 5.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1 10.1016/j.bmcl.2010.06.068
1323 2688 None 38 Human Functional pEC50 = 9.2 9.2 -33 7
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
92432 2688 None 38 Human Functional pEC50 = 9.2 9.2 -33 7
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
CHEMBL430239 2688 None 38 Human Functional pEC50 = 9.2 9.2 -33 7
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL None None None None 10.1016/s0960-894x(03)00114-8
10146211 64350 None 0 Human Functional pEC50 = 9.2 9.2 61 3
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL181162 64350 None 0 Human Functional pEC50 = 9.2 9.2 61 3
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 649 10 2 6 3.6 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
11061068 31300 None 0 Human Functional pEC50 = 9.2 9.2 138 3
Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
CHEMBL140154 31300 None 0 Human Functional pEC50 = 9.2 9.2 138 3
Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm025539h
1338 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL3646884 214482 None 0 Human Functional pEC50 = 9.2 9.2 39 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL412523 215460 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
129627786 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
1330 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16129617 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16129674 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16133751 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16133802 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16133802.0 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16162116 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
3767 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
4516 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
60210072 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
6965 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL2103784 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
DB01284 280 None 26 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16132144 211738 None 29 Human Functional pEC50 = 9.2 9.2 -12 8
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm500064t
16133793 211738 None 29 Human Functional pEC50 = 9.2 9.2 -12 8
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm500064t
44273719 211738 None 29 Human Functional pEC50 = 9.2 9.2 -12 8
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm500064t
CHEMBL214332 211738 None 29 Human Functional pEC50 = 9.2 9.2 -12 8
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm500064t
127046235 139725 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL3797690 139725 None 0 Human Functional pEC50 = 9.2 9.2 -2 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1004 36 12 13 -1.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL428326 215899 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm0501432
CHEMBL406842 215084 None 0 Mouse Functional pEC50 = 9.2 9.2 -6 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
56662904 63724 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 0 4 7.1 CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801217 63724 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 0 4 7.1 CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1 10.1016/j.bmcl.2010.06.062
90643803 111806 None 0 Mouse Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Mouse Functional pEC50 = 9.2 9.2 -1 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
1338 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 9.2 9.2 -2 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
1324 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
16154396 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
16197727 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
16197727.0 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
44285019 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
57514683 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
91898441 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
DB04931 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assayAgonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.3c00432
1324 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
16154396 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
16197727.0 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
44285019 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
57514683 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
91898441 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
DB04931 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960845e
1324 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
16154396 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
16197727.0 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
44285019 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
57514683 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
91898441 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
DB04931 302 None 19 Human Functional pEC50 = 9.1 9.1 -14 8
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm960840h
56669820 63715 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 4 0 4 6.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2 10.1016/j.bmcl.2010.06.062
CHEMBL1801147 63715 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 4 0 4 6.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2 10.1016/j.bmcl.2010.06.062
CHEMBL410763 215298 None 0 Mouse Functional pEC50 = 9.1 9.1 -21 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL412494 215457 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm0501432
CHEMBL3601426 214286 None 0 Human Functional pEC50 = 9.1 9.1 17 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
56676632 63699 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 5 1 3 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801118 63699 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 5 1 3 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1 10.1016/j.bmcl.2010.06.062
25129453 171869 None 0 Human Functional pEC50 = 9.1 9.1 15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
CHEMBL446757 171869 None 0 Human Functional pEC50 = 9.1 9.1 15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 677 11 3 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm800525p
49862750 15158 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 657 5 1 6 5.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1 10.1016/j.bmcl.2010.06.068
CHEMBL1209801 15158 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 657 5 1 6 5.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1 10.1016/j.bmcl.2010.06.068
CHEMBL3358537 214027 None 0 Mouse Functional pEC50 = 9.1 9.1 -3 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
1338 3807 None 36 Human Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 9.1 9.1 -2 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL3646889 214487 None 0 Human Functional pEC50 = 9.1 9.1 31 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O nan
118722940 116305 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358548 116305 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3646892 214490 None 0 Human Functional pEC50 = 9.1 9.1 25 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
56673302 63692 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C 10.1016/j.bmcl.2010.06.062
CHEMBL1801095 63692 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C 10.1016/j.bmcl.2010.06.062
1324 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16154396 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
16197727.0 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
44285019 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
57514683 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
91898441 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
DB04931 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b00251
CHEMBL5077095 216967 None 0 Human Functional pEC50 = 9.1 9.1 -25 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
16746686 18163 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 651 5 0 6 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL1269575 18163 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 651 5 0 6 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
25133210 169560 None 0 Human Functional pEC50 = 9.1 9.1 44 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
CHEMBL442829 169560 None 0 Human Functional pEC50 = 9.1 9.1 44 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1 10.1021/jm800525p
25131478 169611 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
CHEMBL443396 169611 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 574 10 5 6 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O 10.1021/jm800525p
44569176 172648 None 0 Human Functional pEC50 = 9.1 9.1 48 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
CHEMBL448410 172648 None 0 Human Functional pEC50 = 9.1 9.1 48 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.3 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1 10.1021/jm800525p
44275650 94107 None 0 Human Functional pEC50 = 9.1 9.1 -2 4
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL24892 94107 None 0 Human Functional pEC50 = 9.1 9.1 -2 4
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 953 15 12 10 -0.8 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1016/s0960-894x(03)00114-8
1324 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16154396 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
16197727.0 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
44285019 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
57514683 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
91898441 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
DB04931 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00641
1324 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16154396 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
16197727.0 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
44285019 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
57514683 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
91898441 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
DB04931 302 None 19 Mouse Functional pEC50 = 9.1 9.1 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b00860
10886436 119221 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
CHEMBL342954 119221 None 0 Mouse Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 588 8 2 6 4.6 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/acs.jmedchem.0c02041
44448660 95026 None 0 Rat Functional pEC50 = 9.1 9.1 4 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 95026 None 0 Rat Functional pEC50 = 9.1 9.1 4 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
56659466 63694 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.6 CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801097 63694 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.6 CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL427666 215825 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O 10.1021/jm0501432
CHEMBL264190 213067 None 0 Human Functional pEC50 = 9.0 9.0 -30 7
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL264536 213086 None 9 Mouse Functional pEC50 = 9.0 9.0 -20 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1021/jm010061n
127048118 173110 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 2236 54 25 25 -5.6 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL4518266 173110 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 2236 54 25 25 -5.6 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL5087859 217613 None 0 Human Functional pEC50 = 9.0 9.0 -4 3
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
56683301 63718 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801150 63718 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1 10.1016/j.bmcl.2010.06.062
172453477 196059 None 0 Human Functional pEC50 = 9.0 9.0 22 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1323 13 16 16 3.8 C[C@@H]1NC(=O)c2cc(NC(=S)Nc3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5416095 196059 None 0 Human Functional pEC50 = 9.0 9.0 22 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1323 13 16 16 3.8 C[C@@H]1NC(=O)c2cc(NC(=S)Nc3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
1324 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
16154396 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
16197727 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
16197727.0 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
44285019 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
57514683 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
91898441 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
CHEMBL441738 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
DB04931 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None None 10.1016/s0960-894x(02)00830-2
1338 3807 None 36 Human Functional pEC50 = 9 9.0 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 36 Human Functional pEC50 = 9 9.0 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 36 Human Functional pEC50 = 9 9.0 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
56679968 63716 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 639 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801148 63716 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 639 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1 10.1016/j.bmcl.2010.06.062
172453477 196059 None 0 Human Functional pEC50 = 9 9.0 22 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1323 13 16 16 3.8 C[C@@H]1NC(=O)c2cc(NC(=S)Nc3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5416095 196059 None 0 Human Functional pEC50 = 9 9.0 22 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 1323 13 16 16 3.8 C[C@@H]1NC(=O)c2cc(NC(=S)Nc3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
172457809 196344 None 0 Human Functional pEC50 = 9 9.0 1 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5421885 196344 None 0 Human Functional pEC50 = 9 9.0 1 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
70688853 76952 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070248 76952 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1495 39 18 16 -0.1 CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
1324 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
11571540 135278 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 910 22 9 7 3.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL372201 135278 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 910 22 9 7 3.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
11593230 161324 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 958 22 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1 10.1016/j.bmcl.2005.08.083
CHEMBL411817 161324 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 958 22 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1 10.1016/j.bmcl.2005.08.083
1324 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
16154396 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
16197727 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
16197727.0 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
44285019 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
57514683 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
91898441 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
CHEMBL441738 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
DB04931 302 None 19 Human Functional pEC50 = 9 9.0 -14 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None None 10.1016/s0960-894x(02)00459-6
11851038 140422 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL380691 140422 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL5076315 216916 None 0 Human Functional pEC50 = 9.0 9.0 -3 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL3287059 213757 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL502093 216637 None 0 Mouse Functional pEC50 = 9.0 9.0 2 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
CHEMBL3799094 214728 None 0 Human Functional pEC50 = 9.0 9.0 -8 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
56673305 63704 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 631 6 1 3 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF 10.1016/j.bmcl.2010.06.062
CHEMBL1801123 63704 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 631 6 1 3 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF 10.1016/j.bmcl.2010.06.062
56676639 63717 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801149 63717 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 4 0 3 7.4 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1 10.1016/j.bmcl.2010.06.062
49862736 15143 None 0 Human Functional pEC50 = 9.0 9.0 117 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 569 3 0 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209787 15143 None 0 Human Functional pEC50 = 9.0 9.0 117 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 569 3 0 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
1324 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16154396 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16197727 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
16197727.0 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
44285019 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
57514683 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
91898441 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
DB04931 302 None 19 Mouse Functional pEC50 = 9.0 9.0 -10 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None None 10.1021/acsmedchemlett.9b00198
46919520 15144 None 0 Rat Functional pEC50 = 9.0 9.0 2 6
Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15144 None 0 Rat Functional pEC50 = 9.0 9.0 2 6
Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
1324 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
1324 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 9.0 9.0 -14 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
168281421 191066 None 0 Human Functional pEC50 = 9.0 9.0 -10 3
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185945 191066 None 0 Human Functional pEC50 = 9.0 9.0 -10 3
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2430 43 34 31 -3.4 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
11158573 71143 None 0 Mouse Functional pEC50 = 8.9 8.9 -2 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL195439 71143 None 0 Mouse Functional pEC50 = 8.9 8.9 -2 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 783 25 9 7 2.1 CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
127047853 140080 None 0 Human Functional pEC50 = 8.9 8.9 -4 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL3799955 140080 None 0 Human Functional pEC50 = 8.9 8.9 -4 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1948 72 23 25 -2.1 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
56676614 63725 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 0 4 7.1 CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801218 63725 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 0 4 7.1 CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1 10.1016/j.bmcl.2010.06.062
25129107 173881 None 0 Human Functional pEC50 = 8.9 8.9 36 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
CHEMBL453734 173881 None 0 Human Functional pEC50 = 8.9 8.9 36 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 11 3 5 2.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N 10.1021/jm800525p
1324 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
1338 3807 None 36 Human Functional pEC50 = 8.9 8.9 -2 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 8.9 8.9 -2 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.9 8.9 -2 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL5077144 216973 None 0 Human Functional pEC50 = 8.9 8.9 -13 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5090946 217775 None 0 Human Functional pEC50 = 8.9 8.9 -4 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL322610 213693 None 0 Human Functional pEC50 = 8.9 8.9 -2 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL5091236 217789 None 0 Human Functional pEC50 = 8.9 8.9 -48 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44408287 75412 None 0 Human Functional pEC50 = 8.9 8.9 162 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL203911 75412 None 0 Human Functional pEC50 = 8.9 8.9 162 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 620 8 2 5 5.1 C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
56659467 63707 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 629 6 2 4 5.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO 10.1016/j.bmcl.2010.06.062
CHEMBL1801126 63707 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 629 6 2 4 5.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO 10.1016/j.bmcl.2010.06.062
25133556 188957 None 0 Human Functional pEC50 = 8.9 8.9 7 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
CHEMBL506762 188957 None 0 Human Functional pEC50 = 8.9 8.9 7 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1 10.1021/jm800525p
168276507 190374 None 0 Human Functional pEC50 = 8.9 8.9 -15 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5175487 190374 None 0 Human Functional pEC50 = 8.9 8.9 -15 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289457 191489 None 0 Human Functional pEC50 = 8.9 8.9 -7 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5192329 191489 None 0 Human Functional pEC50 = 8.9 8.9 -7 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
137638778 156850 None 0 Human Functional pEC50 = 8.9 8.9 11 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 156850 None 0 Human Functional pEC50 = 8.9 8.9 11 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
137633806 156572 None 0 Human Functional pEC50 = 8.9 8.9 10 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
CHEMBL4067491 156572 None 0 Human Functional pEC50 = 8.9 8.9 10 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1031 14 14 13 -2.0 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.7b00353
56662925 63697 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 5 1 3 7.0 CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801116 63697 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 5 1 3 7.0 CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL503229 216651 None 0 Human Functional pEC50 = 8.9 8.9 -1 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
134466953 156750 None 0 Mouse Functional pEC50 = 8.9 8.9 -4 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4069451 156750 None 0 Mouse Functional pEC50 = 8.9 8.9 -4 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1153 14 13 12 -1.3 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
1324 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 8.9 8.9 -14 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44310344 97382 None 0 Mouse Functional pEC50 = 8.9 8.9 -13 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
77231883 97382 None 0 Mouse Functional pEC50 = 8.9 8.9 -13 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL269274 97382 None 0 Mouse Functional pEC50 = 8.9 8.9 -13 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 4414 53 53 68 -9.9 CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4 10.1021/jm0303608
CHEMBL443071 216381 None 0 Human Functional pEC50 = 8.9 8.9 -1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL410404 215279 None 0 Mouse Functional pEC50 = 8.9 8.9 -11 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
10408 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
5329 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
9941379.0 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
CHEMBL2070241 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
DB11653 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.1c00095
10408 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
5329 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
9941379.0 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
CHEMBL2070241 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
DB11653 720 None 23 Human Functional pEC50 = 8.8 8.8 -1 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.2c00793
1338 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm049278i
9938402 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm049278i
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm049278i
CHEMBL3358533 214026 None 0 Mouse Functional pEC50 = 8.8 8.8 -3 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
49862745 15152 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 615 5 0 5 6.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C 10.1016/j.bmcl.2010.06.068
CHEMBL1209796 15152 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 615 5 0 5 6.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C 10.1016/j.bmcl.2010.06.068
90643803 111806 None 0 Human Functional pEC50 = 8.8 8.8 -3 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Human Functional pEC50 = 8.8 8.8 -3 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
1324 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 8.8 8.8 -14 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
1338 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.8 8.8 -2 8
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
172468014 196563 None 0 Human Functional pEC50 = 8.8 8.8 6 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 934 11 13 11 -0.4 C[C@H]1NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5426684 196563 None 0 Human Functional pEC50 = 8.8 8.8 6 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 934 11 13 11 -0.4 C[C@H]1NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5087814 217609 None 0 Human Functional pEC50 = 8.8 8.8 -4 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
16132144 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
16133793 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
44273719 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0490843
44415920 80402 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL214410 80402 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 644 12 4 6 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416060 81349 None 0 Human Functional pEC50 = 8.8 8.8 66 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL215895 81349 None 0 Human Functional pEC50 = 8.8 8.8 66 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 734 13 5 6 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
44415912 139313 None 0 Human Functional pEC50 = 8.8 8.8 23 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL378837 139313 None 0 Human Functional pEC50 = 8.8 8.8 23 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 575 11 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
56683299 63710 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 627 5 0 3 7.3 CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801142 63710 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 627 5 0 3 7.3 CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
134463477 159345 None 0 Mouse Functional pEC50 = 8.8 8.8 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4099127 159345 None 0 Mouse Functional pEC50 = 8.8 8.8 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 977 11 12 11 -1.9 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
101670969 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
16131138 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
44349184 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
53310908 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
91898438 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
CHEMBL438402 168999 None 21 Mouse Functional pEC50 = 8.8 8.8 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 1623 49 22 22 -4.3 CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C 10.1021/acs.jmedchem.0c02041
118722935 116300 None 0 Mouse Functional pEC50 = 8.8 8.8 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
CHEMBL3358543 116300 None 0 Mouse Functional pEC50 = 8.8 8.8 1 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1048 17 13 13 -0.7 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm501027w
42630327 155961 None 0 Human Functional pEC50 = 8.8 8.8 -6 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
CHEMBL4060381 155961 None 0 Human Functional pEC50 = 8.8 8.8 -6 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1119 32 19 14 -3.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O 10.1021/acs.jmedchem.8b00170
16007263 79827 None 0 Human Functional pEC50 = 8.8 8.8 23 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL211975 79827 None 0 Human Functional pEC50 = 8.8 8.8 23 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 557 11 4 5 1.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
56683300 63711 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 641 6 0 3 7.7 CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801143 63711 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 641 6 0 3 7.7 CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
25129109 188809 None 0 Human Functional pEC50 = 8.8 8.8 29 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
CHEMBL504349 188809 None 0 Human Functional pEC50 = 8.8 8.8 29 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 603 12 3 5 2.8 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC 10.1021/jm800525p
16132144 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
16133793 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
44273719 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.8 8.8 -8 8
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00053
168293710 192275 None 0 Human Functional pEC50 = 8.8 8.8 -19 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5203986 192275 None 0 Human Functional pEC50 = 8.8 8.8 -19 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2158 33 32 24 -2.3 CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
168289404 191421 None 0 Human Functional pEC50 = 8.8 8.8 -39 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5191309 191421 None 0 Human Functional pEC50 = 8.8 8.8 -39 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2134 33 32 28 -5.0 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
137635422 156000 None 0 Human Functional pEC50 = 8.7 8.7 30 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060816 156000 None 0 Human Functional pEC50 = 8.7 8.7 30 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1111 22 15 16 -2.3 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL264190 213067 None 0 Human Functional pEC50 = 8.7 8.7 -30 7
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
24848934 78983 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 655 11 1 6 4.2 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL2113004 78983 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 655 11 1 6 4.2 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1 10.1016/j.bmcl.2005.01.060
16132144 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
16133793 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
44273719 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.7 8.7 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm0492756
155531854 171751 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 2286 54 25 25 -4.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL4466007 171751 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 2286 54 25 25 -4.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
155563057 175402 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1680 54 21 19 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL4573190 175402 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1680 54 21 19 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
56662927 63709 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 6 2 4 6.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO 10.1016/j.bmcl.2010.06.062
CHEMBL1801141 63709 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 657 6 2 4 6.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO 10.1016/j.bmcl.2010.06.062
CHEMBL3287069 213766 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(O)c(I)c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.02.068
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2004.10.020
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2005.05.109
44456222 97978 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 97978 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
49862376 15046 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209319 15046 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1 10.1016/j.bmcl.2010.06.038
25133208 172097 None 0 Human Functional pEC50 = 8 8.0 4 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
CHEMBL447117 172097 None 0 Human Functional pEC50 = 8 8.0 4 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 615 11 3 5 3.1 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1 10.1021/jm800525p
145977650 163929 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4206406 163929 None 0 Human Functional pEC50 = 8 8.0 -2 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
1323 2688 None 38 Human Functional pEC50 = 8 8.0 -33 7
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
92432 2688 None 38 Human Functional pEC50 = 8 8.0 -33 7
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8 8.0 -33 7
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01620
11845272 80389 None 0 Human Functional pEC50 = 8 8.0 9 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL214347 80389 None 0 Human Functional pEC50 = 8 8.0 9 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1021/jm060384p
44275265 161384 None 0 Human Functional pEC50 = 8 8.0 14 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL412174 161384 None 0 Human Functional pEC50 = 8 8.0 14 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
90643802 111805 None 0 Human Functional pEC50 = 8 8.0 -14 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 8 8.0 -14 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 8 8.0 -5 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
11851038 140422 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL380691 140422 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
44409257 140673 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL381357 140673 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 690 15 7 6 1.6 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
44409338 168847 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL437132 168847 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 739 19 7 6 3.4 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL412358 215446 None 0 Human Functional pEC50 = 8 8.0 -10 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)N=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
44441684 94184 None 0 Human Functional pEC50 = 8 8.0 28 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249321 94184 None 0 Human Functional pEC50 = 8 8.0 28 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 571 7 3 5 3.1 CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 7
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
44448631 95123 None 0 Rat Functional pEC50 = 8.0 8.0 1 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95123 None 0 Rat Functional pEC50 = 8.0 8.0 1 4
Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL5081077 217205 None 0 Human Functional pEC50 = 8.0 8.0 -89 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168295726 192514 None 0 Human Functional pEC50 = 8.0 8.0 -117 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5207936 192514 None 0 Human Functional pEC50 = 8.0 8.0 -117 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2547 50 34 33 -2.8 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL589308 218289 None 0 Mouse Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)NCC(=O)N(CC(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)Cc1ccccc1 10.1016/j.bmc.2009.12.010
44394659 66975 None 0 Human Functional pEC50 = 8.0 8.0 53 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL186687 66975 None 0 Human Functional pEC50 = 8.0 8.0 53 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 754 19 9 7 1.5 N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11239907 133195 None 0 Mouse Functional pEC50 = 8.0 8.0 -18 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL370261 133195 None 0 Mouse Functional pEC50 = 8.0 8.0 -18 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 854 30 9 7 4.1 CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.0 8.0 -2 7
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
46228690 203949 None 0 Human Functional pEC50 = 7 7.0 -63 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 519 5 1 4 4.4 O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21 10.1016/j.bmc.2010.01.049
CHEMBL605115 203949 None 0 Human Functional pEC50 = 7 7.0 -63 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 519 5 1 4 4.4 O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21 10.1016/j.bmc.2010.01.049
137638218 156920 None 0 Mouse Functional pEC50 = 7 7.0 -2 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4071283 156920 None 0 Mouse Functional pEC50 = 7 7.0 -2 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 988 11 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
44373317 119722 None 0 Human Functional pEC50 = 7 7.0 2 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 787 22 9 9 0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL346930 119722 None 0 Human Functional pEC50 = 7 7.0 2 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 787 22 9 9 0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
16157270 215013 None 15 Human Functional pEC50 = 7 7.0 -162 6
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL405282 215013 None 15 Human Functional pEC50 = 7 7.0 -162 6
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
16157270 215013 None 15 Human Functional pEC50 = 7 7.0 -162 6
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
CHEMBL405282 215013 None 15 Human Functional pEC50 = 7 7.0 -162 6
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
71459896 78570 None 0 Human Functional pEC50 = 6 6.0 6 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 820 21 9 7 1.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL2112064 78570 None 0 Human Functional pEC50 = 6 6.0 6 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 820 21 9 7 1.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
44442998 93659 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 578 8 1 5 5.2 O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
CHEMBL246631 93659 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 578 8 1 5 5.2 O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
44443016 94141 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 566 9 1 5 5.4 COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/j.bmcl.2007.10.032
CHEMBL249064 94141 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 566 9 1 5 5.4 COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/j.bmcl.2007.10.032
CHEMBL3600921 214284 None 0 Human Functional pEC50 = 6 6.0 -7 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
11706338 204164 None 0 Human Functional pEC50 = 6 6.0 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL1237150 204164 None 0 Human Functional pEC50 = 6 6.0 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL1237166 204164 None 0 Human Functional pEC50 = 6 6.0 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL606399 204164 None 0 Human Functional pEC50 = 6 6.0 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
145966364 164215 None 0 Human Functional pEC50 = 6 6.0 -131 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4209913 164215 None 0 Human Functional pEC50 = 6 6.0 -131 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 865 11 12 9 -0.7 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL320157 213685 None 0 Mouse Functional pEC50 = 6 6.0 -1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
11851038 140422 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL380691 140422 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
44349170 116887 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 650 9 4 5 4.8 O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL337941 116887 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 650 9 4 5 4.8 O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
44348844 118267 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 665 11 2 6 4.0 CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
CHEMBL340908 118267 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 665 11 2 6 4.0 CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
CHEMBL381739 214752 None 0 Human Functional pEC50 = 5 5.0 -8 3
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O 10.1021/jm0510326
44305763 205544 None 0 Mouse Functional pEC50 = 4 4.0 -5 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL63850 205544 None 0 Mouse Functional pEC50 = 4 4.0 -5 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 490 11 5 4 3.1 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
164612768 184825 None 0 Mouse Functional pEC50 = 4 4.0 -165 3
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4850501 184825 None 0 Mouse Functional pEC50 = 4 4.0 -165 3
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 10 3 3 6.3 CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
164613353 184881 None 0 Mouse Functional pEC50 = 4 4.0 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 539 13 4 4 4.0 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
CHEMBL4851292 184881 None 0 Mouse Functional pEC50 = 4 4.0 - 1
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 539 13 4 4 4.0 CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O 10.1021/acs.jmedchem.0c02041
164613550 185235 None 0 Mouse Functional pEC50 = 4 4.0 -177 3
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4856539 185235 None 0 Mouse Functional pEC50 = 4 4.0 -177 3
Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 606 11 3 3 6.7 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
45487298 199798 None 0 Mouse Functional pEC50 = 5 5.0 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568965 199798 None 0 Mouse Functional pEC50 = 5 5.0 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 657 17 8 8 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
49862663 15128 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 613 3 0 5 7.0 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209705 15128 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 613 3 0 5 7.0 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44413576 78185 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 725 10 10 7 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL210399 78185 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 725 10 10 7 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL5091245 217790 None 0 Human Functional pEC50 = 7.0 7.0 -5 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
46228814 201832 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 617 10 2 6 4.9 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL590955 201832 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 617 10 2 6 4.9 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
137646617 157636 None 0 Human Functional pEC50 = 6.0 6.0 -2 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 157636 None 0 Human Functional pEC50 = 6.0 6.0 -2 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44433423 88758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 496 6 1 4 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL236110 88758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 496 6 1 4 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
44433423 88758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 496 6 1 4 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.06.088
CHEMBL236110 88758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 496 6 1 4 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.06.088
46885368 7958 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
CHEMBL1090484 7958 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 6 1 3 4.8 CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
44275312 141494 None 0 Human Functional pEC50 = 7.0 7.0 70 2
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL 1023 13 11 9 1.9 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL384036 141494 None 0 Human Functional pEC50 = 7.0 7.0 70 2
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL 1023 13 11 9 1.9 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
44394627 124148 None 0 Human Functional pEC50 = 7.0 7.0 7 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL363272 124148 None 0 Human Functional pEC50 = 7.0 7.0 7 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 757 20 8 6 2.1 CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46228726 202947 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL598643 202947 None 0 Human Functional pEC50 = 6.0 6.0 -3 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
137646617 157636 None 0 Human Functional pEC50 = 5.0 5.0 -2 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4080223 157636 None 0 Human Functional pEC50 = 5.0 5.0 -2 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46202892 7758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 538 3 1 3 5.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1 10.1021/jm9017866
CHEMBL1089107 7758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 538 3 1 3 5.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1 10.1021/jm9017866
CHEMBL1204062 7758 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 538 3 1 3 5.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1 10.1021/jm9017866
CHEMBL438596 216242 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
44413969 80261 None 0 Human Functional pEC50 = 5.0 5.0 -24 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
CHEMBL213752 80261 None 0 Human Functional pEC50 = 5.0 5.0 -24 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1 10.1021/jm060384p
44310258 159512 None 0 Mouse Functional pEC50 = 5.0 5.0 -4 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932908 159512 None 0 Mouse Functional pEC50 = 5.0 5.0 -4 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL410091 159512 None 0 Mouse Functional pEC50 = 5.0 5.0 -4 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44413968 80260 None 0 Human Functional pEC50 = 6.0 6.0 -57 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL213751 80260 None 0 Human Functional pEC50 = 6.0 6.0 -57 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL444493 216394 None 0 Human Functional pEC50 = 8.0 8.0 37 2
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
CHEMBL438596 216242 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
44405911 140594 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 994 20 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL381007 140594 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 994 20 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O 10.1016/j.bmcl.2005.08.083
1337 3424 None 5 Human Functional pEC50 = 8.0 8.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 5 Human Functional pEC50 = 8.0 8.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 5 Human Functional pEC50 = 8.0 8.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
9808720 64243 None 0 Human Functional pEC50 = 8.0 8.0 3 2
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL180892 64243 None 0 Human Functional pEC50 = 8.0 8.0 3 2
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.01.060
6918813 131439 None 2 Human Functional pEC50 = 8.0 8.0 77 4
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Functional pEC50 = 8.0 8.0 77 4
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL91957 218395 None 0 Human Functional pEC50 = 8.0 8.0 3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168278271 191224 None 0 Human Functional pEC50 = 8.0 8.0 -23 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5187932 191224 None 0 Human Functional pEC50 = 8.0 8.0 -23 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2167 35 34 26 -5.3 CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
137656521 159838 None 0 Human Functional pEC50 = 7.9 7.9 12 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4104927 159838 None 0 Human Functional pEC50 = 7.9 7.9 12 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1139 22 17 16 -3.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44322895 163465 None 0 Human Functional pEC50 = 7.9 7.9 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL419307 163465 None 0 Human Functional pEC50 = 7.9 7.9 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 811 21 10 8 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44442954 94352 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 526 8 2 5 4.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL250495 94352 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 526 8 2 5 4.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
24848995 118011 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm049278i
CHEMBL340355 118011 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm049278i
145973975 164752 None 0 Human Functional pEC50 = 7.0 7.0 -16 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216654 164752 None 0 Human Functional pEC50 = 7.0 7.0 -16 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 901 11 12 9 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
90643846 111831 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287353 111831 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
90643850 111834 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287357 111834 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44405802 72885 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 921 22 8 7 4.6 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL200270 72885 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 921 22 8 7 4.6 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44349055 16473 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 613 9 2 8 3.1 COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1 10.1016/s0960-894x(03)00796-0
CHEMBL123426 16473 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 613 9 2 8 3.1 COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1 10.1016/s0960-894x(03)00796-0
11295737 120277 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 544 7 2 4 4.6 CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL352063 120277 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 544 7 2 4 4.6 CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
24848995 118011 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL340355 118011 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
70695694 78445 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL2111251 78445 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
44397652 123701 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL361883 123701 None 0 Human Functional pEC50 = 7.0 7.0 14 2
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 620 10 2 7 6.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
44397461 126295 None 0 Human Functional pEC50 = 7.0 7.0 16 3
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365005 126295 None 0 Human Functional pEC50 = 7.0 7.0 16 3
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 606 10 2 7 5.6 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
44448661 95052 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254792 95052 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44442931 150478 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 536 8 1 4 5.4 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL395355 150478 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 536 8 1 4 5.4 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44443027 155110 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 579 9 1 5 5.5 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL401488 155110 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 579 9 1 5 5.5 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44433384 154800 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 564 7 1 4 6.2 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.079
CHEMBL399801 154800 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 564 7 1 4 6.2 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.079
44433384 154800 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 564 7 1 4 6.2 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL399801 154800 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 564 7 1 4 6.2 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL3287356 213774 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
137645898 158110 None 0 Mouse Functional pEC50 = 6.0 6.0 -27 2
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 797 10 9 8 -1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4085584 158110 None 0 Mouse Functional pEC50 = 6.0 6.0 -27 2
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 797 10 9 8 -1.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
155558348 175140 None 0 Mouse Functional pEC50 = 6.0 6.0 -61 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4567480 175140 None 0 Mouse Functional pEC50 = 6.0 6.0 -61 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 677 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
155566298 175897 None 0 Mouse Functional pEC50 = 6.0 6.0 -85 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4584189 175897 None 0 Mouse Functional pEC50 = 6.0 6.0 -85 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 683 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL343094 214156 None 0 Mouse Functional pEC50 = 6.0 6.0 -6 3
Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
44349006 114516 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 622 8 3 6 4.1 O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1 10.1016/s0960-894x(03)00796-0
CHEMBL333368 114516 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 622 8 3 6 4.1 O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1 10.1016/s0960-894x(03)00796-0
44397534 67289 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 621 10 2 8 5.1 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL188142 67289 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 621 10 2 8 5.1 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
44397698 126269 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 616 10 2 7 6.2 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL364992 126269 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 616 10 2 7 6.2 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
1337 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
1337 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
6918851 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
CHEMBL364346 3424 None 5 Human Functional pEC50 = 5.0 5.0 3 5
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F 10.1016/j.bmcl.2005.05.109
46885561 7814 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089487 7814 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44441646 154177 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398487 154177 None 0 Human Functional pEC50 = 7.0 7.0 10 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 611 9 2 7 3.7 Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
122184912 122624 None 0 Human Functional pEC50 = 6.0 6.0 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601430 122624 None 0 Human Functional pEC50 = 6.0 6.0 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
46203214 7863 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 472 3 1 5 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1 10.1021/jm9017866
CHEMBL1089831 7863 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 472 3 1 5 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1 10.1021/jm9017866
CHEMBL1204064 7863 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 472 3 1 5 3.6 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1 10.1021/jm9017866
CHEMBL430843 216082 None 0 Mouse Functional pEC50 = 5.0 5.0 -3 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
16038121 106760 None 0 Human Functional pEC50 = 6.0 6.0 -8 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 697 10 10 7 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL3143817 106760 None 0 Human Functional pEC50 = 6.0 6.0 -8 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 697 10 10 7 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
46885674 7961 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 442 3 1 3 4.3 CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1090487 7961 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 442 3 1 3 4.3 CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
137656033 158735 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1034 20 15 16 -3.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4092477 158735 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1034 20 15 16 -3.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL65339 218350 None 0 Mouse Functional pEC50 = 5.0 5.0 -1 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
90643825 111812 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 923 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287331 111812 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 923 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
44394657 127531 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL366040 127531 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 745 19 10 7 0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
137647538 158054 None 0 Human Functional pEC50 = 6.9 6.9 -891 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 158054 None 0 Human Functional pEC50 = 6.9 6.9 -891 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137638725 157071 None 0 Human Functional pEC50 = 6.9 6.9 3 3
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4073016 157071 None 0 Human Functional pEC50 = 6.9 6.9 3 3
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
90643844 111830 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 695 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287351 111830 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 695 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44372942 119821 None 0 Human Functional pEC50 = 5.9 5.9 -6 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 786 22 11 9 -1.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL347864 119821 None 0 Human Functional pEC50 = 5.9 5.9 -6 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 786 22 11 9 -1.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
45487417 199500 None 0 Mouse Functional pEC50 = 4.9 4.9 -27 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
CHEMBL567233 199500 None 0 Mouse Functional pEC50 = 4.9 4.9 -27 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 17 8 7 0.1 COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1 10.1016/j.bmcl.2009.07.025
46885559 7812 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089484 7812 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
73347133 89506 None 0 Human Functional pEC50 = 6.9 6.9 -7 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 960 13 10 9 0.9 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
CHEMBL2371903 89506 None 0 Human Functional pEC50 = 6.9 6.9 -7 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 960 13 10 9 0.9 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
44416122 80159 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213284 80159 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 576 11 4 5 1.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
56679964 63693 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.6 CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801096 63693 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.6 CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
25129105 177124 None 0 Human Functional pEC50 = 7.9 7.9 12 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
CHEMBL463047 177124 None 0 Human Functional pEC50 = 7.9 7.9 12 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1 10.1021/jm800525p
168273822 190679 None 0 Human Functional pEC50 = 7.9 7.9 -7 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5180152 190679 None 0 Human Functional pEC50 = 7.9 7.9 -7 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11328898 7962 None 25 Human Functional pEC50 = 7.9 7.9 85 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1090488 7962 None 25 Human Functional pEC50 = 7.9 7.9 85 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1204059 7962 None 25 Human Functional pEC50 = 7.9 7.9 85 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
122179552 121551 None 0 Mouse Functional pEC50 = 7.9 7.9 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
CHEMBL3582446 121551 None 0 Mouse Functional pEC50 = 7.9 7.9 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL 699 19 10 7 0.0 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12 10.1021/acsmedchemlett.5b00053
1338 3807 None 36 Human Functional pEC50 = 7.9 7.9 -2 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 7.9 7.9 -2 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 7.9 7.9 -2 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL438596 216242 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
CHEMBL184870 211510 None 0 Human Functional pEC50 = 7.9 7.9 3 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None C=CCNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11786860 66355 None 1 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185035 66355 None 1 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 614 9 4 6 3.4 CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
71454491 78984 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 615 10 1 6 3.2 CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL2113006 78984 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 615 10 1 6 3.2 CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2005.01.060
44441642 154494 None 0 Human Functional pEC50 = 7.9 7.9 75 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL398816 154494 None 0 Human Functional pEC50 = 7.9 7.9 75 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
162670951 182944 None 0 Human Functional pEC50 = 7.9 7.9 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Functional pEC50 = 7.9 7.9 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
137644225 158528 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1083 22 13 16 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4090425 158528 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1083 22 13 16 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL501679 216631 None 0 Mouse Functional pEC50 = 7.9 7.9 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
44277299 169535 None 0 Human Functional pEC50 = 6.9 6.9 8 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 864 23 9 8 1.7 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1 10.1016/s0960-894x(02)00830-2
CHEMBL442537 169535 None 0 Human Functional pEC50 = 6.9 6.9 8 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 864 23 9 8 1.7 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1 10.1016/s0960-894x(02)00830-2
145976863 163853 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4205548 163853 None 0 Human Functional pEC50 = 6.9 6.9 -6 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 879 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
90643838 111823 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 831 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287345 111823 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 831 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
1324 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16154396 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16197727 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
16197727.0 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
44285019 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
57514683 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
91898441 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
CHEMBL441738 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
DB04931 302 None 19 Mouse Functional pEC50 = 6.9 6.9 -10 8
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None None 10.1016/s0960-894x(03)00318-4
44397655 67328 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 627 10 2 8 5.7 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL188360 67328 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 627 10 2 8 5.7 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
10168556 63894 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 657 9 3 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.01.060
CHEMBL180366 63894 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 657 9 3 6 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.01.060
137641398 158408 None 0 Human Functional pEC50 = 6.9 6.9 -162 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4089162 158408 None 0 Human Functional pEC50 = 6.9 6.9 -162 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44448479 155461 None 0 Human Functional pEC50 = 6.9 6.9 9 3
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL403420 155461 None 0 Human Functional pEC50 = 6.9 6.9 9 3
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
44442977 93867 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 537 8 1 5 4.8 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL247636 93867 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 537 8 1 5 4.8 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44443020 94142 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 566 9 1 5 5.4 COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1 10.1016/j.bmcl.2007.10.032
CHEMBL249065 94142 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 566 9 1 5 5.4 COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1 10.1016/j.bmcl.2007.10.032
CHEMBL264190 213067 None 0 Human Functional pEC50 = 5.9 5.9 -30 7
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
71456245 79007 None 0 Human Functional pEC50 = 5.9 5.9 2 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113039 79007 None 0 Human Functional pEC50 = 5.9 5.9 2 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 608 9 2 6 6.2 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44394694 66333 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184895 66333 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 819 21 9 6 3.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 5.9 5.9 -117 6
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.5b00053
44394580 122214 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359701 122214 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 757 19 8 6 2.0 CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
46944097 71942 None 0 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 441 6 1 5 5.3 COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC nan
CHEMBL1971975 71942 None 0 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 441 6 1 5 5.3 COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC nan
CHEMBL3287059 213757 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
137644225 158528 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1083 22 13 16 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4090425 158528 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1083 22 13 16 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
45487296 199781 None 0 Mouse Functional pEC50 = 4.9 4.9 -10 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568836 199781 None 0 Mouse Functional pEC50 = 4.9 4.9 -10 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 635 18 8 7 0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL3287061 213759 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
46228764 202680 None 0 Human Functional pEC50 = 5.9 5.9 -35 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL596804 202680 None 0 Human Functional pEC50 = 5.9 5.9 -35 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
46885816 7908 None 0 Human Functional pEC50 = 6.9 6.9 28 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 436 4 1 3 4.4 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1090161 7908 None 0 Human Functional pEC50 = 6.9 6.9 28 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 436 4 1 3 4.4 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL2323800 211985 None 0 Mouse Functional pEC50 = 5.9 5.9 -79 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
45487411 199501 None 0 Mouse Functional pEC50 = 4.9 4.9 -46 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL567240 199501 None 0 Mouse Functional pEC50 = 4.9 4.9 -46 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44278193 168540 None 0 Human Functional pEC50 = 7.9 7.9 22 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 862 22 9 7 2.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1 10.1016/s0960-894x(02)00830-2
CHEMBL434966 168540 None 0 Human Functional pEC50 = 7.9 7.9 22 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 862 22 9 7 2.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1 10.1016/s0960-894x(02)00830-2
9808801 60829 None 0 Human Functional pEC50 = 7.9 7.9 29 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761871 60829 None 0 Human Functional pEC50 = 7.9 7.9 29 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 599 8 3 4 5.0 CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1 10.1016/j.bmcl.2011.02.090
10077258 15037 None 0 Human Functional pEC50 = 7.9 7.9 15 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15037 None 0 Human Functional pEC50 = 7.9 7.9 15 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
118735100 118864 None 0 Human Functional pEC50 = 7.9 7.9 26 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421677 118864 None 0 Human Functional pEC50 = 7.9 7.9 26 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 764 15 9 6 1.8 CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
162670951 182944 None 0 Human Functional pEC50 = 7.9 7.9 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791306 182944 None 0 Human Functional pEC50 = 7.9 7.9 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL3287329 213770 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287329 213770 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL451423 216431 None 0 Mouse Functional pEC50 = 7.9 7.9 1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
44373198 52182 None 0 Human Functional pEC50 = 7.9 7.9 7 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 848 22 10 8 0.1 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL158808 52182 None 0 Human Functional pEC50 = 7.9 7.9 7 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 848 22 10 8 0.1 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
10213106 72450 None 0 Human Functional pEC50 = 7.9 7.9 199 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 892 24 9 8 2.9 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL198772 72450 None 0 Human Functional pEC50 = 7.9 7.9 199 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 892 24 9 8 2.9 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1 10.1016/j.bmcl.2005.08.012
71449119 78999 None 0 Human Functional pEC50 = 7.9 7.9 117 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL2113028 78999 None 0 Human Functional pEC50 = 7.9 7.9 117 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 643 7 3 6 4.2 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1 10.1016/j.bmcl.2004.10.020
44323032 209062 None 0 Human Functional pEC50 = 7.9 7.9 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL89004 209062 None 0 Human Functional pEC50 = 7.9 7.9 -6 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 761 20 10 7 0.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11308957 69415 None 0 Mouse Functional pEC50 = 7.9 7.9 -6 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL193151 69415 None 0 Mouse Functional pEC50 = 7.9 7.9 -6 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 868 31 9 7 4.5 CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44448631 95123 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL255286 95123 None 0 Human Functional pEC50 = 7.9 7.9 -1 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44400428 125744 None 0 Mouse Functional pEC50 = 7.9 7.9 -16 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL364726 125744 None 0 Mouse Functional pEC50 = 7.9 7.9 -16 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 896 35 9 7 6.1 CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 7.9 7.9 -2 7
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
44394585 66787 None 0 Human Functional pEC50 = 7.9 7.9 61 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL185868 66787 None 0 Human Functional pEC50 = 7.9 7.9 61 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 755 20 9 6 2.1 C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL5077095 216967 None 0 Human Functional pEC50 = 7.9 7.9 -25 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL204310 211623 None 0 Human Functional pEC50 = 6.9 6.9 -64 4
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0510326
44278223 99189 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 878 23 9 8 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1 10.1016/s0960-894x(02)00830-2
CHEMBL281060 99189 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 878 23 9 8 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1 10.1016/s0960-894x(02)00830-2
44277301 100910 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 854 21 9 7 2.0 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL29349 100910 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 854 21 9 7 2.0 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1 10.1016/s0960-894x(02)00830-2
145972289 164615 None 0 Human Functional pEC50 = 6.9 6.9 -45 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4214826 164615 None 0 Human Functional pEC50 = 6.9 6.9 -45 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
90643806 111809 None 0 Human Functional pEC50 = 6.9 6.9 -12 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 6.9 6.9 -12 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
59149264 76830 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684624 76830 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929810 76830 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2069317 76830 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1946 57 23 26 -3.0 CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
46885862 8473 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 462 3 1 3 4.3 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1093857 8473 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 462 3 1 3 4.3 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL2323793 211978 None 0 Mouse Functional pEC50 = 6.9 6.9 -17 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
137644449 158384 None 0 Mouse Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4088980 158384 None 0 Mouse Functional pEC50 = 6.9 6.9 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1016 12 11 10 -0.7 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
44404528 72533 None 0 Human Functional pEC50 = 6.9 6.9 10 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 791 20 8 6 3.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL199037 72533 None 0 Human Functional pEC50 = 6.9 6.9 10 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 791 20 8 6 3.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44404528 72533 None 0 Human Functional pEC50 = 6.9 6.9 10 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 791 20 8 6 3.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL199037 72533 None 0 Human Functional pEC50 = 6.9 6.9 10 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 791 20 8 6 3.3 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.012
44448436 95655 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 577 6 1 3 6.6 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257770 95655 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 577 6 1 3 6.6 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44443015 94099 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 570 8 1 4 6.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL248862 94099 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 570 8 1 4 6.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44443031 154646 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 572 8 1 4 5.7 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL399112 154646 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 572 8 1 4 5.7 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL2323797 211982 None 0 Mouse Functional pEC50 = 5.9 5.9 -67 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1 10.1021/jm301253y
155555217 174441 None 0 Mouse Functional pEC50 = 5.9 5.9 -812 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4550976 174441 None 0 Mouse Functional pEC50 = 5.9 5.9 -812 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 775 16 8 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
162667982 182521 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 776 16 8 7 -0.1 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acsmedchemlett.0c00561
CHEMBL4785727 182521 None 0 Mouse Functional pEC50 = 5.9 5.9 - 1
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 776 16 8 7 -0.1 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acsmedchemlett.0c00561
11364343 119988 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 516 6 2 4 3.7 Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL349427 119988 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 516 6 2 4 3.7 Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL184968 211511 None 0 Human Functional pEC50 = 6.9 6.9 7 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None CCC(=O)OC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
145980198 166781 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4282109 166781 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 692 17 7 6 2.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
164622453 186196 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
CHEMBL4871577 186196 None 0 Mouse Functional pEC50 = 5.9 5.9 -2 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 601 12 3 3 6.2 CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2 10.1021/acs.jmedchem.0c02041
162669632 182671 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182671 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
44310243 169290 None 0 Mouse Functional pEC50 = 4.9 4.9 -2 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932909 169290 None 0 Mouse Functional pEC50 = 4.9 4.9 -2 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL440633 169290 None 0 Mouse Functional pEC50 = 4.9 4.9 -2 3
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL 1421 24 20 20 -4.6 C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
44394734 64578 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL181494 64578 None 0 Human Functional pEC50 = 6.9 6.9 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 791 19 9 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
162669632 182671 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4787753 182671 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL434357 216113 None 0 Human Functional pEC50 = 6.9 6.9 5 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None COP(=O)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC 10.1016/j.bmcl.2004.07.046
46232220 203511 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602652 203511 None 0 Mouse Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487407 199424 None 0 Mouse Functional pEC50 = 4.9 4.9 -8 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566545 199424 None 0 Mouse Functional pEC50 = 4.9 4.9 -8 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 17 8 7 0.1 COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
122184636 122501 None 0 Human Functional pEC50 = 6.9 6.9 -7 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600917 122501 None 0 Human Functional pEC50 = 6.9 6.9 -7 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44393888 127150 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 625 10 3 6 4.9 CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL365636 127150 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 625 10 3 6 4.9 CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44408253 140431 None 0 Human Functional pEC50 = 7.9 7.9 54 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
CHEMBL380727 140431 None 0 Human Functional pEC50 = 7.9 7.9 54 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 650 10 2 5 6.1 CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C 10.1016/j.bmcl.2005.11.095
52940633 18158 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 624 4 0 5 7.5 Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1 10.1016/j.bmcl.2010.09.049
CHEMBL1269570 18158 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 624 4 0 5 7.5 Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1 10.1016/j.bmcl.2010.09.049
11846669 80308 None 0 Human Functional pEC50 = 7.9 7.9 2 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL213956 80308 None 0 Human Functional pEC50 = 7.9 7.9 2 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 584 12 5 5 3.5 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
44413930 138735 None 0 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377620 138735 None 0 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
90643805 111808 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
90643802 111805 None 0 Human Functional pEC50 = 7.9 7.9 -14 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 7.9 7.9 -14 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
10325955 165366 None 0 Human Functional pEC50 = 7.9 7.9 112 2
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL423101 165366 None 0 Human Functional pEC50 = 7.9 7.9 112 2
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 582 8 2 6 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
11157584 168347 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 587 10 2 5 4.3 CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL433710 168347 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 587 10 2 5 4.3 CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44394730 132555 None 0 Human Functional pEC50 = 7.9 7.9 42 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL369770 132555 None 0 Human Functional pEC50 = 7.9 7.9 42 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 772 21 10 7 0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11181928 166252 None 0 Mouse Functional pEC50 = 7.8 7.8 -4 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL426282 166252 None 0 Mouse Functional pEC50 = 7.8 7.8 -4 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 797 26 9 7 2.5 CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3799094 214728 None 0 Mouse Functional pEC50 = 7.8 7.8 -12 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
44394660 67075 None 0 Human Functional pEC50 = 7.8 7.8 41 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL187167 67075 None 0 Human Functional pEC50 = 7.8 7.8 41 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 772 20 9 7 0.2 NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322958 107068 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL315356 107068 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 727 18 9 7 0.4 CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL3350396 213938 None 0 Human Functional pEC50 = 7.8 7.8 -60 4
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
44415972 79914 None 0 Human Functional pEC50 = 6.9 6.9 141 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
CHEMBL212332 79914 None 0 Human Functional pEC50 = 6.9 6.9 141 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 549 13 6 5 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1 10.1016/j.bmcl.2006.05.087
155556954 174652 None 0 Mouse Functional pEC50 = 6.9 6.9 -467 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4556149 174652 None 0 Mouse Functional pEC50 = 6.9 6.9 -467 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
11262020 120331 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 612 9 2 7 3.7 Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL352457 120331 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 612 9 2 7 3.7 Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
73351850 89553 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL2373212 89553 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
44433475 148977 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 514 7 1 4 5.2 CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.09.079
CHEMBL394160 148977 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 514 7 1 4 5.2 CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.09.079
CHEMBL502300 216640 None 0 Human Functional pEC50 = 5.9 5.9 -27 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
71459937 79006 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113038 79006 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44409206 140271 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL380437 140271 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 567 13 4 4 4.8 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL309213 213474 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
11214733 120360 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 530 7 2 4 4.0 CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL352677 120360 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 530 7 2 4 4.0 CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
122184914 122625 None 0 Human Functional pEC50 = 5.8 5.8 -51 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601432 122625 None 0 Human Functional pEC50 = 5.8 5.8 -51 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1144 17 9 11 1.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL359765 214267 None 0 Human Functional pEC50 = 6.8 6.8 -1 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44393822 124110 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 668 9 2 6 4.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL363074 124110 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 668 9 2 6 4.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
46203216 8478 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1093889 8478 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1204067 8478 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 460 4 1 3 4.1 CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
137658158 159811 None 0 Human Functional pEC50 = 6.8 6.8 -10 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159811 None 0 Human Functional pEC50 = 6.8 6.8 -10 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
45487406 199350 None 0 Mouse Functional pEC50 = 4.8 4.8 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL566150 199350 None 0 Mouse Functional pEC50 = 4.8 4.8 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 16 8 6 0.3 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
44408388 140410 None 0 Human Functional pEC50 = 7.8 7.8 36 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL380635 140410 None 0 Human Functional pEC50 = 7.8 7.8 36 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 646 8 2 5 5.6 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
49862376 15046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1 10.1016/j.bmcl.2010.06.038
CHEMBL1209319 15046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 624 8 0 6 5.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1 10.1016/j.bmcl.2010.06.038
44275192 168985 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL438286 168985 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
90643806 111809 None 0 Human Functional pEC50 = 7.8 7.8 -12 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 7.8 7.8 -12 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
59149255 76956 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70693082 76956 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929809 76956 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070252 76956 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1960 58 24 26 -2.5 CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
46885480 7756 None 0 Human Functional pEC50 = 7.8 7.8 4 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089103 7756 None 0 Human Functional pEC50 = 7.8 7.8 4 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 491 4 1 4 4.6 C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
46885621 7957 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1 10.1021/jm9017866
CHEMBL1090473 7957 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1 10.1021/jm9017866
CHEMBL1204057 7957 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 506 3 1 3 5.1 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1 10.1021/jm9017866
90643815 111782 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 707 15 8 6 1.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL3287066 111782 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 707 15 8 6 1.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
90643843 111829 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 809 13 5 6 2.6 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287350 111829 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 809 13 5 6 2.6 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287352 213773 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
44405879 141321 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 946 20 9 7 3.8 CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
CHEMBL382930 141321 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 946 20 9 7 3.8 CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
44405794 161940 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 975 21 10 7 4.0 CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
CHEMBL414670 161940 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 975 21 10 7 4.0 CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
10030530 17606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 552 10 1 4 4.8 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL125819 17606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 552 10 1 4 4.8 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.06.059
44393864 66217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 642 9 4 6 4.4 CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL184405 66217 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 642 9 4 6 4.4 CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
10030530 17606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 552 10 1 4 4.8 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
CHEMBL125819 17606 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 552 10 1 4 4.8 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
44413536 140016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 753 10 10 7 1.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL379959 140016 None 0 Human Functional pEC50 = 7.8 7.8 4 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 753 10 10 7 1.2 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
145971389 164728 None 0 Human Functional pEC50 = 6.8 6.8 -15 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4216242 164728 None 0 Human Functional pEC50 = 6.8 6.8 -15 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
44457043 97665 None 0 Mouse Functional pEC50 = 6.8 6.8 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL270923 97665 None 0 Mouse Functional pEC50 = 6.8 6.8 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 883 12 10 8 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
137654884 158689 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4092082 158689 None 0 Mouse Functional pEC50 = 6.8 6.8 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 840 9 10 9 -1.4 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
155542040 173181 None 0 Mouse Functional pEC50 = 6.8 6.8 -758 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4519837 173181 None 0 Mouse Functional pEC50 = 6.8 6.8 -758 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 654 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44394584 96623 None 0 Human Functional pEC50 = 6.8 6.8 5 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263047 96623 None 0 Human Functional pEC50 = 6.8 6.8 5 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11387898 56064 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 608 9 2 5 5.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL162493 56064 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 608 9 2 5 5.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
11237928 164966 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 532 7 3 5 2.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL422027 164966 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 532 7 3 5 2.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
44401313 12291 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1184856 12291 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL2028956 12291 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 571 8 4 5 3.3 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
44397633 126448 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 636 10 2 7 6.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL365051 126448 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 636 10 2 7 6.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
44442997 93975 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 576 8 1 4 6.3 O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
CHEMBL248205 93975 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 576 8 1 4 6.3 O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
CHEMBL320157 213685 None 0 Mouse Functional pEC50 = 5.8 5.8 -1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44447818 95463 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay
ChEMBL 613 6 2 5 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2008.01.125
CHEMBL256956 95463 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay
ChEMBL 613 6 2 5 5.1 Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2008.01.125
44441686 97297 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 545 8 3 5 2.7 CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL268722 97297 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 545 8 3 5 2.7 CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1 10.1016/j.bmcl.2006.11.084
11592389 201848 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 591 8 1 5 5.4 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591037 201848 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 591 8 1 5 5.4 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2010.01.049
45487404 199892 None 0 Mouse Functional pEC50 = 4.8 4.8 -3019 4
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569694 199892 None 0 Mouse Functional pEC50 = 4.8 4.8 -3019 4
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 18 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
122184575 122493 None 0 Human Functional pEC50 = 6.8 6.8 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600836 122493 None 0 Human Functional pEC50 = 6.8 6.8 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
122184909 122620 None 0 Human Functional pEC50 = 6.8 6.8 6 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3601427 122620 None 0 Human Functional pEC50 = 6.8 6.8 6 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1130 17 10 11 1.5 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44413879 138989 None 0 Human Functional pEC50 = 6.8 6.8 -50 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL378293 138989 None 0 Human Functional pEC50 = 6.8 6.8 -50 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 681 15 6 7 0.9 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
11851038 140422 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL380691 140422 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL433296 216097 None 0 Mouse Functional pEC50 = 6.8 6.8 -2 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
44394582 168477 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434544 168477 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 771 21 8 6 2.5 CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44448698 94985 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254351 94985 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 591 6 1 3 7.5 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
90643842 111827 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287349 111827 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
16132144 211738 None 29 Human Functional pEC50 = 6.8 6.8 -12 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 6.8 6.8 -12 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 6.8 6.8 -12 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 6.8 6.8 -12 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44441648 154781 None 0 Human Functional pEC50 = 6.8 6.8 41 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL399715 154781 None 0 Human Functional pEC50 = 6.8 6.8 41 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 605 8 2 8 2.9 Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
122184637 122502 None 0 Human Functional pEC50 = 5.8 5.8 -4 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600918 122502 None 0 Human Functional pEC50 = 5.8 5.8 -4 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
44413577 139613 None 0 Human Functional pEC50 = 5.8 5.8 -5 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 711 10 10 7 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL379531 139613 None 0 Human Functional pEC50 = 5.8 5.8 -5 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 711 10 10 7 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
46885325 8318 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 432 3 2 3 3.4 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
CHEMBL1092733 8318 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 432 3 2 3 3.4 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1 10.1021/jm9017866
44394626 65805 None 0 Human Functional pEC50 = 6.8 6.8 12 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL183476 65805 None 0 Human Functional pEC50 = 6.8 6.8 12 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 743 19 8 6 1.7 CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44310259 161794 None 0 Mouse Functional pEC50 = 4.8 4.8 1 2
Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
91932914 161794 None 0 Mouse Functional pEC50 = 4.8 4.8 1 2
Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL413465 161794 None 0 Mouse Functional pEC50 = 4.8 4.8 1 2
Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist
ChEMBL 1421 24 20 20 -4.6 C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0303608
CHEMBL413573 215535 None 0 Human Functional pEC50 = 7.8 7.8 -30 4
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
44408252 140756 None 0 Human Functional pEC50 = 7.8 7.8 30 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
CHEMBL381503 140756 None 0 Human Functional pEC50 = 7.8 7.8 30 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 605 8 3 4 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.11.095
44408189 168982 None 0 Human Functional pEC50 = 7.8 7.8 32 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
CHEMBL438259 168982 None 0 Human Functional pEC50 = 7.8 7.8 32 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 619 8 2 4 4.6 CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O 10.1016/j.bmcl.2005.11.095
10373417 100859 None 0 Human Functional pEC50 = 7.8 7.8 301 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 863 22 9 8 1.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1 10.1016/s0960-894x(02)00830-2
CHEMBL29317 100859 None 0 Human Functional pEC50 = 7.8 7.8 301 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 863 22 9 8 1.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1 10.1016/s0960-894x(02)00830-2
44444495 155005 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 595 10 1 5 5.2 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL400932 155005 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 595 10 1 5 5.2 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
9867330 97894 None 0 Human Functional pEC50 = 7.8 7.8 14 3
Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
CHEMBL272099 97894 None 0 Human Functional pEC50 = 7.8 7.8 14 3
Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells
ChEMBL 429 6 1 5 3.7 N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2007.11.109
44444495 155005 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 595 10 1 5 5.2 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.06.088
CHEMBL400932 155005 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 595 10 1 5 5.2 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.06.088
44444497 155102 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 571 9 2 5 4.3 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmcl.2007.06.088
CHEMBL401465 155102 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 571 9 2 5 4.3 CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmcl.2007.06.088
9960253 117013 None 0 Human Functional pEC50 = 7.8 7.8 25 2
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL338594 117013 None 0 Human Functional pEC50 = 7.8 7.8 25 2
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
71456236 78921 None 0 Human Functional pEC50 = 7.8 7.8 -31 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 814 24 10 9 -0.3 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL2112918 78921 None 0 Human Functional pEC50 = 7.8 7.8 -31 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 814 24 10 9 -0.3 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
6918813 131439 None 2 Human Functional pEC50 = 7.8 7.8 77 4
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL368876 131439 None 2 Human Functional pEC50 = 7.8 7.8 77 4
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44413535 96758 None 0 Human Functional pEC50 = 7.8 7.8 4 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 738 10 9 7 2.9 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL264120 96758 None 0 Human Functional pEC50 = 7.8 7.8 4 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 738 10 9 7 2.9 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
44322977 111632 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL328117 111632 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 714 18 11 8 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
168271237 190597 None 0 Human Functional pEC50 = 7.8 7.8 -69 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5179081 190597 None 0 Human Functional pEC50 = 7.8 7.8 -69 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2788 45 36 36 0.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
155563222 175395 None 0 Mouse Functional pEC50 = 6.8 6.8 -524 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4572994 175395 None 0 Mouse Functional pEC50 = 6.8 6.8 -524 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
155564058 175438 None 0 Mouse Functional pEC50 = 6.8 6.8 -794 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4574056 175438 None 0 Mouse Functional pEC50 = 6.8 6.8 -794 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 746 14 7 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
90643844 111830 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 695 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287351 111830 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 695 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44409140 141373 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL383256 141373 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 675 16 6 5 3.5 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
44405425 71884 None 0 Human Functional pEC50 = 6.8 6.8 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 669 10 3 5 4.5 NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1 10.1016/j.bmcl.2005.08.061
CHEMBL197020 71884 None 0 Human Functional pEC50 = 6.8 6.8 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 669 10 3 5 4.5 NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1 10.1016/j.bmcl.2005.08.061
44443033 93751 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1 10.1016/j.bmcl.2007.10.032
CHEMBL247010 93751 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1 10.1016/j.bmcl.2007.10.032
CHEMBL264190 213067 None 0 Human Functional pEC50 = 5.8 5.8 -30 7
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
155556466 174520 None 0 Mouse Functional pEC50 = 5.8 5.8 -2238 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4552764 174520 None 0 Mouse Functional pEC50 = 5.8 5.8 -2238 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 648 17 8 6 1.2 CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
44349151 18537 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 603 7 3 7 2.5 COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL127461 18537 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 603 7 3 7 2.5 COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
44413842 138464 None 0 Human Functional pEC50 = 5.8 5.8 -3 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377210 138464 None 0 Human Functional pEC50 = 5.8 5.8 -3 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44394010 125492 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 599 9 3 5 4.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL364577 125492 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 599 9 3 5 4.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
10188529 126849 None 0 Human Functional pEC50 = 6.8 6.8 19 3
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL365401 126849 None 0 Human Functional pEC50 = 6.8 6.8 19 3
Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
46228846 201849 None 0 Human Functional pEC50 = 6.8 6.8 8 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 567 9 1 6 4.3 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591041 201849 None 0 Human Functional pEC50 = 6.8 6.8 8 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 567 9 1 6 4.3 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
25133903 170661 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
CHEMBL445009 170661 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 596 11 3 6 3.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O 10.1021/jm800525p
CHEMBL420581 215711 None 0 Human Functional pEC50 = 5.8 5.8 -27 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
44394093 127306 None 0 Human Functional pEC50 = 6.8 6.8 3 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL365825 127306 None 0 Human Functional pEC50 = 6.8 6.8 3 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 881 19 9 6 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44456138 95406 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 8 2 6 4.4 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL256686 95406 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 8 2 6 4.4 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1 10.1016/j.bmcl.2007.10.115
145989222 167376 None 0 Human Functional pEC50 = 7.8 7.8 1 4
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4293365 167376 None 0 Human Functional pEC50 = 7.8 7.8 1 4
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 676 17 7 6 2.2 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44413932 137633 None 0 Human Functional pEC50 = 7.8 7.8 3 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL375440 137633 None 0 Human Functional pEC50 = 7.8 7.8 3 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 570 12 5 5 3.1 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1 10.1021/jm060384p
CHEMBL3287329 213770 None 0 Human Functional pEC50 = 7.8 7.8 1 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287064 213762 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O 10.1021/jm500064t
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 7.8 7.8 -2 7
Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2003.08.078
49862742 14976 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 601 4 0 5 6.1 CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL1208802 14976 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 601 4 0 5 6.1 CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 7.8 7.8 -2 7
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
137662147 159473 None 0 Human Functional pEC50 = 7.8 7.8 25 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 159473 None 0 Human Functional pEC50 = 7.8 7.8 25 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
11555886 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL404696 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
44443035 154506 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
CHEMBL398929 154506 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 584 9 1 5 5.5 COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F 10.1016/j.bmcl.2007.10.032
44444493 155220 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 581 9 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.06.088
CHEMBL402058 155220 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 581 9 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.06.088
CHEMBL432201 216094 None 0 Human Functional pEC50 = 6.8 6.8 6 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
57817730 76951 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70684622 76951 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929805 76951 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070247 76951 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1919 56 24 26 -3.5 CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
137648053 157631 None 0 Mouse Functional pEC50 = 6.8 6.8 -10 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4080169 157631 None 0 Mouse Functional pEC50 = 6.8 6.8 -10 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 934 12 11 10 -1.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.6b01707
44349093 168625 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 633 8 2 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
CHEMBL435410 168625 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 633 8 2 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
CHEMBL439128 216286 None 0 Human Functional pEC50 = 6.8 6.8 -52 3
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
10141778 116783 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
ChEMBL 500 9 2 6 3.2 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2003.09.036
CHEMBL337351 116783 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
ChEMBL 500 9 2 6 3.2 NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1 10.1016/j.bmcl.2003.09.036
46232228 203480 None 0 Mouse Functional pEC50 = 5.8 5.8 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602299 203480 None 0 Mouse Functional pEC50 = 5.8 5.8 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 8 8 1.0 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
171378343 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5423711 196422 None 0 Human Functional pEC50 = 6.8 6.8 -8 4
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 697 15 10 7 -0.2 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
45487413 199707 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568409 199707 None 0 Mouse Functional pEC50 = 4.8 4.8 -14 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 616 15 10 7 -0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O 10.1016/j.bmcl.2009.07.025
44358915 13082 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL1190181 13082 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL540320 13082 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
137653925 158699 None 0 Human Functional pEC50 = 5.8 5.8 -4 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4092141 158699 None 0 Human Functional pEC50 = 5.8 5.8 -4 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1742 21 20 21 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL263822 213049 None 0 Human Functional pEC50 = 6.8 6.8 -16 4
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm0510326
44393886 66380 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 585 9 3 5 4.2 CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185145 66380 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 585 9 3 5 4.2 CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44275264 156472 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL406636 156472 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O 10.1016/s0960-894x(03)00114-8
44441689 154507 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 569 7 3 6 1.8 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL398932 154507 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 569 7 3 6 1.8 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1 10.1016/j.bmcl.2006.11.084
15953838 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL188146 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL539306 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
11635265 202942 None 0 Human Functional pEC50 = 6.8 6.8 -12 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 543 7 1 4 4.8 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
CHEMBL598617 202942 None 0 Human Functional pEC50 = 6.8 6.8 -12 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 543 7 1 4 4.8 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
44335147 4594 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL102688 4594 None 0 Mouse Functional pEC50 = 5.8 5.8 -4 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL 711 16 9 7 -0.3 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1 10.1021/jm010524p
CHEMBL275303 213280 None 0 Human Functional pEC50 = 4.8 4.8 4 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
11555886 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.09.049
CHEMBL404696 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.09.049
10483153 60831 None 0 Human Functional pEC50 = 7.8 7.8 53 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761873 60831 None 0 Human Functional pEC50 = 7.8 7.8 53 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
44416014 80046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL212855 80046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 562 10 4 5 1.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O 10.1016/j.bmcl.2006.05.087
11555886 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.062
CHEMBL404696 155724 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 559 6 1 3 6.4 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.062
145976444 164058 None 0 Human Functional pEC50 = 7.8 7.8 -6 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4207858 164058 None 0 Human Functional pEC50 = 7.8 7.8 -6 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 889 11 12 9 -0.1 CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.8b00488
46885712 8073 None 0 Human Functional pEC50 = 7.8 7.8 63 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1091151 8073 None 0 Human Functional pEC50 = 7.8 7.8 63 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1204061 8073 None 0 Human Functional pEC50 = 7.8 7.8 63 4
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 488 3 1 3 4.9 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
46885417 8283 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 498 4 1 4 4.2 C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092573 8283 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 498 4 1 4 4.2 C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44456964 156782 None 0 Mouse Functional pEC50 = 7.8 7.8 1 3
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL406985 156782 None 0 Mouse Functional pEC50 = 7.8 7.8 1 3
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
16132144 211738 None 29 Human Functional pEC50 = 7.8 7.8 -12 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 7.8 7.8 -12 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 7.8 7.8 -12 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.8 7.8 -12 8
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
10145026 12273 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1 10.1016/j.bmcl.2005.02.068
CHEMBL1184727 12273 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1 10.1016/j.bmcl.2005.02.068
CHEMBL2028962 12273 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1 10.1016/j.bmcl.2005.02.068
44393885 124454 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 8 3 6 3.6 C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1 10.1016/j.bmcl.2004.06.059
CHEMBL363925 124454 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 8 3 6 3.6 C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1 10.1016/j.bmcl.2004.06.059
44390421 63927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 645 10 1 6 4.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL180544 63927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 645 10 1 6 4.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1 10.1016/j.bmcl.2005.01.060
44322923 209004 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88630 209004 None 0 Human Functional pEC50 = 7.8 7.8 -2 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 710 19 10 8 -0.5 N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
127047913 140011 None 0 Mouse Functional pEC50 = 7.7 7.7 -19 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3799563 140011 None 0 Mouse Functional pEC50 = 7.7 7.7 -19 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL370254 214626 None 2 Mouse Functional pEC50 = 7.7 7.7 -6 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm0490843
44394735 123382 None 0 Human Functional pEC50 = 7.7 7.7 34 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361578 123382 None 0 Human Functional pEC50 = 7.7 7.7 34 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44278071 100498 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 704 20 9 7 -0.6 CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29056 100498 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 704 20 9 7 -0.6 CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
49862426 15067 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 6 0 4 4.6 CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209383 15067 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 6 0 4 4.6 CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C 10.1016/j.bmcl.2010.06.038
15953838 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL188146 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL539306 67291 None 0 Human Functional pEC50 = 6.8 6.8 18 3
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL415200 215639 None 0 Mouse Functional pEC50 = 6.8 6.8 -20 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O 10.1021/jm030452x
1334 1501 None 4 Human Functional pEC50 = 6.8 6.8 -6 4
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
16133814 1501 None 4 Human Functional pEC50 = 6.8 6.8 -6 4
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.8 6.8 -6 4
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None None 10.1021/jm030119t
44442995 93705 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 562 8 1 4 5.9 O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
CHEMBL246837 93705 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 562 8 1 4 5.9 O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2007.10.032
11364326 66707 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185455 66707 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 515 6 3 3 5.2 C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
168285101 191753 None 0 Human Functional pEC50 = 6.7 6.7 -85 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5195937 191753 None 0 Human Functional pEC50 = 6.7 6.7 -85 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
45487415 199895 None 0 Mouse Functional pEC50 = 4.7 4.7 -218 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569697 199895 None 0 Mouse Functional pEC50 = 4.7 4.7 -218 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 603 16 9 7 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44413913 138760 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL377779 138760 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 672 16 6 7 0.2 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
137643023 158402 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1010 16 13 14 -1.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4089119 158402 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1010 16 13 14 -1.1 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44394787 166083 None 0 Human Functional pEC50 = 6.7 6.7 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL425348 166083 None 0 Human Functional pEC50 = 6.7 6.7 4 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 821 21 9 7 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
90643819 111783 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 688 13 6 6 1.8 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL3287070 111783 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 688 13 6 6 1.8 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
44441633 94583 None 0 Human Functional pEC50 = 6.7 6.7 18 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL251735 94583 None 0 Human Functional pEC50 = 6.7 6.7 18 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 546 7 2 4 5.2 N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44456137 155211 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 9 2 6 4.2 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmcl.2007.10.115
CHEMBL402017 155211 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 9 2 6 4.2 CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C 10.1016/j.bmcl.2007.10.115
49862377 15047 None 0 Human Functional pEC50 = 7.7 7.7 13 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
CHEMBL1209320 15047 None 0 Human Functional pEC50 = 7.7 7.7 13 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 654 9 0 6 6.2 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1 10.1016/j.bmcl.2010.06.038
49862425 15066 None 0 Human Functional pEC50 = 7.7 7.7 74 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209382 15066 None 0 Human Functional pEC50 = 7.7 7.7 74 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 9 0 5 4.0 CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
49862478 15081 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 7 0 5 4.0 CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209458 15081 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 570 7 0 5 4.0 CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
46885366 7853 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 456 5 1 3 4.4 CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
CHEMBL1089796 7853 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 456 5 1 3 4.4 CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
11787684 70298 None 0 Mouse Functional pEC50 = 7.7 7.7 -6 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL194217 70298 None 0 Mouse Functional pEC50 = 7.7 7.7 -6 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 811 27 9 7 2.9 CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
16132144 211738 None 29 Mouse Functional pEC50 = 7.7 7.7 -8 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
16133793 211738 None 29 Mouse Functional pEC50 = 7.7 7.7 -8 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
44273719 211738 None 29 Mouse Functional pEC50 = 7.7 7.7 -8 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 7.7 7.7 -8 8
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2009.07.025
137631599 156617 None 0 Human Functional pEC50 = 7.7 7.7 -16 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156617 None 0 Human Functional pEC50 = 7.7 7.7 -16 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
172446133 195506 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5405038 195506 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 964 12 12 12 -0.1 C[C@@H]1NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.2c01587
44443026 154892 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 593 9 2 5 5.4 CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1 10.1016/j.bmcl.2007.10.032
CHEMBL400263 154892 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 593 9 2 5 5.4 CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1 10.1016/j.bmcl.2007.10.032
90643802 111805 None 0 Human Functional pEC50 = 6.7 6.7 -14 4
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 6.7 6.7 -14 4
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
102096778 58823 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
51351277 58823 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
53322400 58823 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
91932360 58823 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL1688111 58823 None 0 Mouse Functional pEC50 = 6.7 6.7 -10 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL2323794 211979 None 0 Mouse Functional pEC50 = 6.7 6.7 -21 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
44349173 117054 None 0 Human Functional pEC50 = 6.7 6.7 3 3
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/s0960-894x(03)00796-0
CHEMBL338768 117054 None 0 Human Functional pEC50 = 6.7 6.7 3 3
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21 10.1016/s0960-894x(03)00796-0
44393821 66733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 650 11 2 6 4.5 CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185583 66733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 650 11 2 6 4.5 CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 6.7 6.7 -1 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
168285904 191779 None 0 Human Functional pEC50 = 6.7 6.7 -117 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5196407 191779 None 0 Human Functional pEC50 = 6.7 6.7 -117 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1347 15 14 15 1.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
44433380 88521 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 564 6 1 4 5.3 CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.09.079
CHEMBL234992 88521 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 564 6 1 4 5.3 CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.09.079
11341045 66187 None 0 Human Functional pEC50 = 5.7 5.7 -4 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
CHEMBL184275 66187 None 0 Human Functional pEC50 = 5.7 5.7 -4 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 501 6 3 3 5.0 O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1 10.1021/jm0400496
44349110 18558 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 559 7 3 5 3.4 CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL127574 18558 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 559 7 3 5 3.4 CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL264190 213067 None 0 Human Functional pEC50 = 6.7 6.7 -30 7
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
45487291 199829 None 0 Mouse Functional pEC50 = 4.7 4.7 -6 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569220 199829 None 0 Mouse Functional pEC50 = 4.7 4.7 -6 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
44448480 95611 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257616 95611 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 573 6 1 3 7.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2008.04.049
44409379 76549 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL206018 76549 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 757 19 6 5 4.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
137647538 158054 None 0 Human Functional pEC50 = 5.7 5.7 -891 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4084765 158054 None 0 Human Functional pEC50 = 5.7 5.7 -891 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL3287073 213768 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
49862662 15127 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 569 3 0 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209704 15127 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 569 3 0 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
44441639 94103 None 0 Human Functional pEC50 = 6.7 6.7 11 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248893 94103 None 0 Human Functional pEC50 = 6.7 6.7 11 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 532 7 2 4 4.8 N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
46232222 203512 None 0 Mouse Functional pEC50 = 5.7 5.7 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602653 203512 None 0 Mouse Functional pEC50 = 5.7 5.7 -3 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 8 8 0.2 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
90643804 111807 None 0 Human Functional pEC50 = 4.7 4.7 -8 4
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Human Functional pEC50 = 4.7 4.7 -8 4
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
122184634 122499 None 0 Human Functional pEC50 = 6.7 6.7 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600915 122499 None 0 Human Functional pEC50 = 6.7 6.7 -2 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1116 17 11 11 1.1 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
44456957 98091 None 0 Mouse Functional pEC50 = 5.7 5.7 -8 2
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 432 5 1 2 5.2 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21 10.1021/jm701303z
CHEMBL273044 98091 None 0 Mouse Functional pEC50 = 5.7 5.7 -8 2
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 432 5 1 2 5.2 O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21 10.1021/jm701303z
10373417 100859 None 0 Human Functional pEC50 = 8.7 8.7 301 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 863 22 9 8 1.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1 10.1016/s0960-894x(02)00830-2
CHEMBL29317 100859 None 0 Human Functional pEC50 = 8.7 8.7 301 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 863 22 9 8 1.4 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1 10.1016/s0960-894x(02)00830-2
137638778 156850 None 0 Human Functional pEC50 = 8.7 8.7 11 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4070639 156850 None 0 Human Functional pEC50 = 8.7 8.7 11 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1053 18 14 15 -2.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44447251 154888 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at MC4RAgonist activity at MC4R
ChEMBL 531 5 0 4 5.4 CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2007.11.128
CHEMBL400237 154888 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at MC4RAgonist activity at MC4R
ChEMBL 531 5 0 4 5.4 CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2007.11.128
127047913 140011 None 0 Human Functional pEC50 = 8.7 8.7 -4 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL3799563 140011 None 0 Human Functional pEC50 = 8.7 8.7 -4 4
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 962 35 12 13 -1.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
44415918 141636 None 0 Human Functional pEC50 = 8.7 8.7 -1 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL384774 141636 None 0 Human Functional pEC50 = 8.7 8.7 -1 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 754 16 6 7 0.9 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O 10.1016/j.bmcl.2006.05.087
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL None None None None 10.1016/j.ejmech.2018.04.021
44569175 188930 None 0 Human Functional pEC50 = 8.7 8.7 12 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
CHEMBL506272 188930 None 0 Human Functional pEC50 = 8.7 8.7 12 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 3 5 2.5 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1 10.1021/jm800525p
172445559 195459 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5404193 195459 None 0 Human Functional pEC50 = 8.7 8.7 -2 4
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 981 17 15 11 -0.5 CCCC[C@H](NC(C)=N)C(=O)N[C@@H]1NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.2c01794
73347133 89506 None 0 Human Functional pEC50 = 8.7 8.7 -7 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 960 13 10 9 0.9 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
CHEMBL2371903 89506 None 0 Human Functional pEC50 = 8.7 8.7 -7 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 960 13 10 9 0.9 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
44275656 159562 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1031 15 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL410148 159562 None 0 Human Functional pEC50 = 8.7 8.7 6 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1031 15 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL2070242 211642 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11753695 8395 None 6 Rat Functional pEC50 = 8.7 8.7 3 7
Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8395 None 6 Rat Functional pEC50 = 8.7 8.7 3 7
Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
1324 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16154396 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
16197727.0 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44285019 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
57514683 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
91898441 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
CHEMBL441738 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
DB04931 302 None 19 Human Functional pEC50 = 8.7 8.7 -14 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None None 10.1021/jm050780s
44405858 72886 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 896 21 9 7 4.2 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL200276 72886 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 896 21 9 7 4.2 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405833 133525 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 877 23 10 7 2.6 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL370665 133525 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 877 23 10 7 2.6 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405836 135277 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 882 21 9 7 2.5 NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL372200 135277 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 882 21 9 7 2.5 NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405860 136240 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 925 22 10 7 4.4 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL373259 136240 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 925 22 10 7 4.4 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
9919056 141156 None 0 Human Functional pEC50 = 8.7 8.7 1380 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 848 22 9 7 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL382511 141156 None 0 Human Functional pEC50 = 8.7 8.7 1380 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 848 22 9 7 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405793 159037 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 958 22 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1 10.1016/j.bmcl.2005.08.083
CHEMBL409588 159037 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 958 22 10 7 4.5 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1 10.1016/j.bmcl.2005.08.083
44405792 166205 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 940 23 10 7 4.1 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL425992 166205 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 940 23 10 7 4.1 CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405910 170559 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 910 22 9 7 3.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL444880 170559 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 910 22 9 7 3.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL200614 211567 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL None None None CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL434186 216112 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL None None None CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
11273288 12965 None 0 Human Functional pEC50 = 8.7 8.7 61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1189370 12965 None 0 Human Functional pEC50 = 8.7 8.7 61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL538567 12965 None 0 Human Functional pEC50 = 8.7 8.7 61 3
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
44404526 96545 None 0 Human Functional pEC50 = 8.7 8.7 346 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 878 23 9 8 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL262470 96545 None 0 Human Functional pEC50 = 8.7 8.7 346 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 878 23 9 8 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1 10.1016/j.bmcl.2005.08.012
9919056 141156 None 0 Human Functional pEC50 = 8.7 8.7 1380 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 848 22 9 7 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL382511 141156 None 0 Human Functional pEC50 = 8.7 8.7 1380 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 848 22 9 7 2.5 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL3644320 214420 None 0 Human Functional pEC50 = 8.7 8.7 30 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O nan
CHEMBL3646886 214484 None 0 Human Functional pEC50 = 8.7 8.7 39 2
cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.
ChEMBL None None None CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5083551 217358 None 0 Human Functional pEC50 = 8.7 8.7 -10 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
1338 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
9938402 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2005.11.095
1338 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
9938402 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2007.11.109
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL None None None None 10.1021/ml500436s
44448629 167561 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL429854 167561 None 0 Human Functional pEC50 = 8.7 8.7 -3 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 619 6 1 3 7.0 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1 10.1016/j.bmcl.2008.04.049
46911588 63689 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 7.0 CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801092 63689 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 7.0 CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
1323 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
92432 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.7 8.7 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2011.03.019
44358565 30034 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 588 8 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1 10.1016/j.bmcl.2003.09.026
CHEMBL138901 30034 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 588 8 2 6 5.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1 10.1016/j.bmcl.2003.09.026
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm049579s
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm030111j
1338 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
1338 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.7 8.7 -2 8
Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
118722929 116296 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
CHEMBL3358538 116296 None 0 Mouse Functional pEC50 = 8.7 8.7 -2 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O 10.1021/jm501027w
10101361 155793 None 0 Human Functional pEC50 = 8.7 8.7 1 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL405174 155793 None 0 Human Functional pEC50 = 8.7 8.7 1 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 717 16 8 6 2.4 CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL5078687 217068 None 0 Human Functional pEC50 = 8.7 8.7 -4 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168271934 190194 None 0 Human Functional pEC50 = 8.7 8.7 -26 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5172738 190194 None 0 Human Functional pEC50 = 8.7 8.7 -26 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2229 37 32 26 -3.7 C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O 10.1021/acs.jmedchem.2c00793
52943061 18155 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 610 4 0 5 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1 10.1016/j.bmcl.2010.09.049
CHEMBL1269568 18155 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 610 4 0 5 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1 10.1016/j.bmcl.2010.09.049
44416135 80215 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
CHEMBL213566 80215 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at human MC4RAgonist activity at human MC4R
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1016/j.bmcl.2006.05.087
44416135 80215 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
CHEMBL213566 80215 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 561 10 5 5 1.1 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O 10.1021/jm800525p
16132144 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
16133793 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
44273719 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.7 8.7 -12 8
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm9017866
118722925 116293 None 0 Mouse Functional pEC50 = 8.7 8.7 -3 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL3358534 116293 None 0 Mouse Functional pEC50 = 8.7 8.7 -3 3
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
ChEMBL 1052 34 13 11 1.6 CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O 10.1021/jm501027w
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 7
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1323 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
92432 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL None None None None 10.1016/j.bmcl.2006.07.015
137662147 159473 None 0 Human Functional pEC50 = 8.6 8.6 25 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4100598 159473 None 0 Human Functional pEC50 = 8.6 8.6 25 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1051 19 15 15 -3.0 C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
52945472 18156 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 624 4 0 5 7.5 Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1 10.1016/j.bmcl.2010.09.049
CHEMBL1269569 18156 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 624 4 0 5 7.5 Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1 10.1016/j.bmcl.2010.09.049
56676635 63708 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 1 4 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801127 63708 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 669 5 1 4 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1 10.1016/j.bmcl.2010.06.062
11845450 138556 None 0 Human Functional pEC50 = 8.6 8.6 -51 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL377465 138556 None 0 Human Functional pEC50 = 8.6 8.6 -51 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44408286 140755 None 0 Human Functional pEC50 = 8.6 8.6 117 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
CHEMBL381501 140755 None 0 Human Functional pEC50 = 8.6 8.6 117 4
Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation
ChEMBL 634 8 2 5 5.5 CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.11.095
52941830 18162 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 637 4 0 5 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
CHEMBL1269574 18162 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 637 4 0 5 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C 10.1016/j.bmcl.2010.09.049
90643802 111805 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL2115441 211727 None 0 Human Functional pEC50 = 8.6 8.6 -8 4
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
10078903 68041 None 0 Mouse Functional pEC50 = 8.6 8.6 -7 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191303 68041 None 0 Mouse Functional pEC50 = 8.6 8.6 -7 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 769 24 9 7 1.8 CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
16132144 211738 None 29 Mouse Functional pEC50 = 8.6 8.6 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
16133793 211738 None 29 Mouse Functional pEC50 = 8.6 8.6 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
44273719 211738 None 29 Mouse Functional pEC50 = 8.6 8.6 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.6 8.6 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm701303z
CHEMBL5085972 217492 None 0 Human Functional pEC50 = 8.6 8.6 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.1c00095
CHEMBL5090670 217767 None 0 Human Functional pEC50 = 8.6 8.6 3 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
49862665 15130 None 0 Human Functional pEC50 = 8.6 8.6 128 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 585 5 1 5 5.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209707 15130 None 0 Human Functional pEC50 = 8.6 8.6 128 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 585 5 1 5 5.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
90643804 111807 None 0 Human Functional pEC50 = 8.6 8.6 -8 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Human Functional pEC50 = 8.6 8.6 -8 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
16132144 211738 None 29 Human Functional pEC50 = 8.6 8.6 -12 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 8.6 8.6 -12 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 8.6 8.6 -12 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.6 8.6 -12 8
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
90643841 111826 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287348 111826 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL5087839 217610 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
44418430 83287 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
CHEMBL218748 83287 None 0 Human Functional pEC50 = 8.6 8.6 -1 3
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
ChEMBL 334 4 0 2 3.1 O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1 10.1016/j.bmcl.2006.07.015
25133209 173455 None 0 Human Functional pEC50 = 8.6 8.6 19 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
CHEMBL452710 173455 None 0 Human Functional pEC50 = 8.6 8.6 19 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 589 12 3 5 2.4 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC 10.1021/jm800525p
46919520 15144 None 0 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15144 None 0 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
90643804 111807 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Mouse Functional pEC50 = 8.6 8.6 -2 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL5094168 217969 None 0 Human Functional pEC50 = 8.6 8.6 -134 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
137637656 156329 None 0 Human Functional pEC50 = 8.6 8.6 40 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 156329 None 0 Human Functional pEC50 = 8.6 8.6 40 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
44448660 95026 None 0 Human Functional pEC50 = 8.6 8.6 -4 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL254589 95026 None 0 Human Functional pEC50 = 8.6 8.6 -4 4
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1 10.1016/j.bmcl.2008.04.049
1323 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
92432 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.6 8.6 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b00488
90643806 111809 None 0 Human Functional pEC50 = 8.6 8.6 -12 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 8.6 8.6 -12 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL448536 216421 None 0 Mouse Functional pEC50 = 8.6 8.6 1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm070461w
CHEMBL393075 214922 None 0 Human Functional pEC50 = 8.5 8.5 -7 4
Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1016/j.bmcl.2007.02.020
168270124 190064 None 0 Human Functional pEC50 = 8.5 8.5 -20 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5170533 190064 None 0 Human Functional pEC50 = 8.5 8.5 -20 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2096 33 32 24 -3.6 CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm0510326
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL None None None None 10.1021/jm060768f
56683296 63700 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 627 5 1 3 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C 10.1016/j.bmcl.2010.06.062
CHEMBL1801119 63700 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 627 5 1 3 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C 10.1016/j.bmcl.2010.06.062
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None None 10.1021/jm801300c
49862751 15159 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 677 5 0 5 6.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1 10.1016/j.bmcl.2010.06.068
CHEMBL1209802 15159 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 677 5 0 5 6.8 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1 10.1016/j.bmcl.2010.06.068
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL None None None None 10.1021/acs.jmedchem.5b01285
90643804 111807 None 0 Human Functional pEC50 = 8.5 8.5 -8 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Human Functional pEC50 = 8.5 8.5 -8 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 8.5 8.5 -5 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
90643803 111806 None 0 Human Functional pEC50 = 8.5 8.5 -3 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Human Functional pEC50 = 8.5 8.5 -3 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
16132144 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
16133793 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
44273719 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/j.bmcl.2015.09.046
16132144 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44393824 122418 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 659 13 3 5 5.7 CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL359976 122418 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 659 13 3 5 5.7 CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2004.06.059
1338 3807 None 36 Rat Functional pEC50 = 8.5 8.5 2 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
9938402 3807 None 36 Rat Functional pEC50 = 8.5 8.5 2 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL339053 3807 None 36 Rat Functional pEC50 = 8.5 8.5 2 8
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm025539h
CHEMBL410217 215268 None 0 Human Functional pEC50 = 8.5 8.5 2 3
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
44277696 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
CHEMBL29582 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00830-2
44456027 155560 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 599 10 1 5 5.0 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.10.115
CHEMBL403967 155560 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 599 10 1 5 5.0 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.10.115
44413938 139026 None 0 Human Functional pEC50 = 7.7 7.7 10 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378446 139026 None 0 Human Functional pEC50 = 7.7 7.7 10 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 662 15 4 5 3.9 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 7.7 7.7 -5 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL2323795 211980 None 0 Mouse Functional pEC50 = 7.7 7.7 -39 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
90643826 111813 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287333 111813 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
44277696 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL29582 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.083
44409339 75022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL203252 75022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 723 19 6 5 3.7 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1 10.1016/j.bmcl.2005.12.005
CHEMBL78565 218370 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
44394693 96651 None 0 Human Functional pEC50 = 7.7 7.7 2 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL263234 96651 None 0 Human Functional pEC50 = 7.7 7.7 2 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 805 20 9 6 2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44373177 119895 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 804 22 10 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL348511 119895 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 804 22 10 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
44372933 119977 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL349298 119977 None 0 Human Functional pEC50 = 7.7 7.7 1 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
44277696 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL29582 101259 None 0 Human Functional pEC50 = 7.7 7.7 1 4
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 770 22 10 8 -0.7 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.012
CHEMBL411400 215343 None 0 Mouse Functional pEC50 = 7.7 7.7 -141 5
Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O 10.1021/jm030452x
44323031 168181 None 0 Human Functional pEC50 = 7.7 7.7 -39 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL432565 168181 None 0 Human Functional pEC50 = 7.7 7.7 -39 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 775 21 10 7 1.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
71452720 79002 None 0 Human Functional pEC50 = 7.7 7.7 34 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL2113031 79002 None 0 Human Functional pEC50 = 7.7 7.7 34 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44322812 112445 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL329586 112445 None 0 Human Functional pEC50 = 7.7 7.7 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 711 19 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11491374 67641 None 0 Mouse Functional pEC50 = 7.7 7.7 -21 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL190366 67641 None 0 Mouse Functional pEC50 = 7.7 7.7 -21 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 840 29 9 7 3.7 CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL501592 216629 None 0 Human Functional pEC50 = 6.7 6.7 -38 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
CHEMBL501642 216630 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
CHEMBL509582 218036 None 0 Human Functional pEC50 = 6.7 6.7 6 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
44405832 133653 None 0 Human Functional pEC50 = 6.7 6.7 14 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 909 21 8 7 2.7 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
CHEMBL371215 133653 None 0 Human Functional pEC50 = 6.7 6.7 14 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 909 21 8 7 2.7 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
11272336 57210 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 517 6 3 5 3.0 Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL164969 57210 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 517 6 3 5 3.0 Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44397657 124190 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 624 10 2 7 5.8 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL363384 124190 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 624 10 2 7 5.8 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL438235 216220 None 0 Human Functional pEC50 = 6.7 6.7 -10 3
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C 10.1021/jm030119t
CHEMBL446185 216405 None 0 Human Functional pEC50 = 5.7 5.7 -5 3
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm0510326
71459937 79006 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113038 79006 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44349226 117047 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 601 10 1 6 2.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
CHEMBL338747 117047 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 601 10 1 6 2.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
11845444 80098 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL213026 80098 None 0 Human Functional pEC50 = 4.7 4.7 -11 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44413970 139102 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL378571 139102 None 0 Human Functional pEC50 = 4.7 4.7 -50 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 587 14 5 6 1.3 NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL2323792 211977 None 0 Mouse Functional pEC50 = 4.7 4.7 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL438596 216242 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
118735103 118867 None 0 Human Functional pEC50 = 6.7 6.7 -1 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421680 118867 None 0 Human Functional pEC50 = 6.7 6.7 -1 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 698 15 8 9 -0.8 CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
90643833 111819 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287340 111819 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL566764 218243 None 0 Mouse Functional pEC50 = 4.7 4.7 -2 2
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None CC(=O)N/C(=C\c1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2009.07.025
90643819 111783 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 688 13 6 6 1.8 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL3287070 111783 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 688 13 6 6 1.8 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
44393889 66368 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 667 11 3 5 5.5 CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL185094 66368 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 667 11 3 5 5.5 CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44393877 122319 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 10 4 6 3.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL359777 122319 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 10 4 6 3.5 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL3287064 213762 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O 10.1021/jm500064t
46885524 7806 None 0 Human Functional pEC50 = 7.7 7.7 186 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1089462 7806 None 0 Human Functional pEC50 = 7.7 7.7 186 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL1204054 7806 None 0 Human Functional pEC50 = 7.7 7.7 186 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 458 5 1 5 3.6 CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C 10.1021/jm9017866
CHEMBL264190 213067 None 0 Mouse Functional pEC50 = 7.7 7.7 -2 7
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
16132144 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16132144 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.7 7.7 -12 8
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL3287356 213774 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
44394691 122969 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL360598 122969 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
11753667 57194 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 596 8 2 6 4.0 Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL164857 57194 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 596 8 2 6 4.0 Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44441643 154890 None 0 Human Functional pEC50 = 7.7 7.7 43 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400252 154890 None 0 Human Functional pEC50 = 7.7 7.7 43 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 591 8 2 7 3.9 Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
44323034 208988 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL88537 208988 None 0 Human Functional pEC50 = 7.7 7.7 -1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 729 21 11 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11263053 68042 None 0 Mouse Functional pEC50 = 7.7 7.7 -29 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL191304 68042 None 0 Mouse Functional pEC50 = 7.7 7.7 -29 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 896 33 9 7 5.3 CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL88185 218386 None 0 Human Functional pEC50 = 7.7 7.7 4 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44444508 155172 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 9 2 5 5.7 CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL401853 155172 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 9 2 5 5.7 CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL526334 218171 None 0 Human Functional pEC50 = 6.7 6.7 -1 2
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm801300c
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 6.7 6.7 -5 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL2323529 211969 None 0 Mouse Functional pEC50 = 6.7 6.7 -2 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
11261324 58151 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 547 7 2 6 3.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL167780 58151 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 547 7 2 6 3.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
44397569 122972 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 636 10 2 7 6.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL360602 122972 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 636 10 2 7 6.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL3600842 214279 None 0 Human Functional pEC50 = 5.7 5.7 -7 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O 10.1021/acs.jmedchem.5b00102
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 5.7 5.7 -117 6
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
44349008 114393 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 646 10 4 7 3.1 CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL333071 114393 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 646 10 4 7 3.1 CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
137659949 159225 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3926 63 56 62 -18.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O 10.1021/acs.jmedchem.8b00251
CHEMBL4097903 159225 None 0 Human Functional pEC50 = 4.7 4.7 -1 2
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3926 63 56 62 -18.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O 10.1021/acs.jmedchem.8b00251
52943061 18155 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 610 4 0 5 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1 10.1016/j.bmcl.2010.09.049
CHEMBL1269568 18155 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 610 4 0 5 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1 10.1016/j.bmcl.2010.09.049
CHEMBL50056 216607 None 1 Mouse Functional pEC50 = 5.7 5.7 -117 6
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
16725558 155759 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL404905 155759 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 575 6 1 3 6.9 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1 10.1016/j.bmcl.2008.04.049
90643847 111832 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287354 111832 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL2369131 212052 None 0 Mouse Functional pEC50 = 4.7 4.7 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
44441682 154738 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 529 8 3 5 2.1 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1 10.1016/j.bmcl.2006.11.084
CHEMBL399474 154738 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 529 8 3 5 2.1 CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1 10.1016/j.bmcl.2006.11.084
168295131 192351 None 0 Human Functional pEC50 = 6.7 6.7 -14 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5205283 192351 None 0 Human Functional pEC50 = 6.7 6.7 -14 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1135 17 13 12 2.2 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL3600920 214283 None 0 Human Functional pEC50 = 5.7 5.7 -8 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
52918026 60828 None 0 Human Functional pEC50 = 7.7 7.7 63 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
CHEMBL1761870 60828 None 0 Human Functional pEC50 = 7.7 7.7 63 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 571 6 3 4 4.2 C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1 10.1016/j.bmcl.2011.02.090
11753695 8395 None 6 Mouse Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1093304 8395 None 6 Mouse Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
11753695 8395 None 6 Mouse Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093304 8395 None 6 Mouse Functional pEC50 = 7.7 7.7 -10 7
Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
90643847 111832 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287354 111832 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
44409104 76552 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
CHEMBL206033 76552 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 582 12 5 5 2.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2005.12.005
44322957 208669 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL86573 208669 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 753 19 10 7 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL5075506 216867 None 0 Human Functional pEC50 = 7.6 7.6 -676 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL5091236 217789 None 0 Human Functional pEC50 = 7.6 7.6 -48 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44442972 153107 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 538 8 1 6 4.2 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL397562 153107 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 538 8 1 6 4.2 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
145948912 167583 None 0 Human Functional pEC50 = 6.7 6.7 -8 4
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
CHEMBL4299454 167583 None 0 Human Functional pEC50 = 6.7 6.7 -8 4
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
ChEMBL 1170 17 14 11 0.7 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.5b01285
46885622 8461 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 3 4.7 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1093801 8461 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 3 4.7 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL2323785 211970 None 0 Mouse Functional pEC50 = 6.7 6.7 -35 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
CHEMBL500516 216605 None 0 Mouse Functional pEC50 = 6.7 6.7 1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
44405913 132804 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 859 21 8 7 3.1 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL369915 132804 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 859 21 8 7 3.1 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44349134 117387 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 679 12 2 6 4.4 CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
CHEMBL339708 117387 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 679 12 2 6 4.4 CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
90643833 111819 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287340 111819 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
46232225 203539 None 0 Mouse Functional pEC50 = 5.7 5.7 -6 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL602852 203539 None 0 Mouse Functional pEC50 = 5.7 5.7 -6 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 849 12 8 8 0.6 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
90643828 111815 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287335 111815 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
90643834 111820 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287341 111820 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
118735102 118866 None 0 Human Functional pEC50 = 6.6 6.6 -6 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
CHEMBL3421679 118866 None 0 Human Functional pEC50 = 6.6 6.6 -6 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
ChEMBL 707 15 8 6 1.1 CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O 10.1021/ml500436s
10348630 30204 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL139042 30204 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
45487295 199830 None 0 Mouse Functional pEC50 = 4.6 4.6 -13 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569221 199830 None 0 Mouse Functional pEC50 = 4.6 4.6 -13 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 617 18 8 7 0.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O 10.1016/j.bmcl.2009.07.025
137660671 159311 None 0 Human Functional pEC50 = 6.6 6.6 -812 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 159311 None 0 Human Functional pEC50 = 6.6 6.6 -812 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137656489 159804 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4104402 159804 None 0 Mouse Functional pEC50 = 7.6 7.6 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1125 13 13 12 -1.2 C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/acs.jmedchem.6b01707
CHEMBL195468 211561 None 0 Mouse Functional pEC50 = 7.6 7.6 -7 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL None None None CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
44394583 122411 None 0 Human Functional pEC50 = 7.6 7.6 6 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359927 122411 None 0 Human Functional pEC50 = 7.6 7.6 6 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 771 18 8 6 2.4 CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44442956 94401 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 526 8 2 5 4.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL250701 94401 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 526 8 2 5 4.1 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44397658 125493 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 10 2 7 6.1 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL364582 125493 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 10 2 7 6.1 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
155567399 176070 None 0 Mouse Functional pEC50 = 5.6 5.6 -501 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4588429 176070 None 0 Mouse Functional pEC50 = 5.6 5.6 -501 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 769 19 9 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL3287073 213768 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL432895 216096 None 2 Mouse Functional pEC50 = 5.6 5.6 -1 4
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
45487288 199812 None 0 Mouse Functional pEC50 = 4.6 4.6 -18 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569076 199812 None 0 Mouse Functional pEC50 = 4.6 4.6 -18 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 623 16 8 6 0.4 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O 10.1016/j.bmcl.2009.07.025
45487286 199797 None 0 Mouse Functional pEC50 = 4.6 4.6 -41 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL568940 199797 None 0 Mouse Functional pEC50 = 4.6 4.6 -41 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 631 16 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
44358660 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL435697 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL544851 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
44305790 102895 None 0 Mouse Functional pEC50 = 4.6 4.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL305559 102895 None 0 Mouse Functional pEC50 = 4.6 4.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44305704 205795 None 0 Mouse Functional pEC50 = 4.6 4.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
CHEMBL64954 205795 None 0 Mouse Functional pEC50 = 4.6 4.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 407 10 5 3 2.4 NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1 10.1016/s0960-894x(03)00318-4
44396986 67453 None 0 Human Functional pEC50 = 6.6 6.6 20 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
CHEMBL188966 67453 None 0 Human Functional pEC50 = 6.6 6.6 20 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 568 7 3 4 4.3 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1 10.1016/j.bmcl.2005.05.109
44278194 99424 None 0 Human Functional pEC50 = 7.6 7.6 8 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 848 22 9 7 1.9 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL282533 99424 None 0 Human Functional pEC50 = 7.6 7.6 8 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 848 22 9 7 1.9 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1 10.1016/s0960-894x(02)00830-2
24873537 146149 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL391902 146149 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 538 6 1 5 4.8 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2007.09.079
CHEMBL2370964 212426 None 0 Human Functional pEC50 = 7.6 7.6 -74 4
Agonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c01295
90643830 111817 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 787 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287337 111817 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 787 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44349019 114501 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
CHEMBL333283 114501 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
44322986 106153 None 0 Human Functional pEC50 = 7.6 7.6 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL313377 106153 None 0 Human Functional pEC50 = 7.6 7.6 -3 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 713 19 9 7 0.1 CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL2370964 212426 None 0 Human Functional pEC50 = 7.6 7.6 -74 4
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
16132144 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
16133793 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
44273719 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.7b00353
CHEMBL5087814 217609 None 0 Human Functional pEC50 = 7.6 7.6 -4 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
10098133 15021 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 518 7 1 4 4.9 CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL1209191 15021 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 518 7 1 4 4.9 CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1 10.1016/j.bmcl.2010.06.038
CHEMBL2323790 211975 None 0 Mouse Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
24882615 97545 None 0 Mouse Functional pEC50 = 6.6 6.6 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
CHEMBL270270 97545 None 0 Mouse Functional pEC50 = 6.6 6.6 -5 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 371 6 2 3 3.1 NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O 10.1021/jm701303z
11157584 168347 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 587 10 2 5 4.3 CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL433710 168347 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 587 10 2 5 4.3 CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44358660 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL435697 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL544851 168662 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
122184577 122495 None 0 Human Functional pEC50 = 5.6 5.6 -19 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL3600838 122495 None 0 Human Functional pEC50 = 5.6 5.6 -19 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL 1102 17 12 11 0.8 CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
CHEMBL105113 210925 None 0 Mouse Functional pEC50 = 5.6 5.6 -1 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
44349111 117550 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 679 10 2 6 4.2 CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
CHEMBL339979 117550 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 679 10 2 6 4.2 CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
44397651 66972 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 670 10 2 7 7.2 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL186675 66972 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 670 10 2 7 7.2 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1 10.1016/j.bmcl.2005.06.033
46885560 7813 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089485 7813 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
44448628 155207 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL402009 155207 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL430489 216081 None 0 Mouse Functional pEC50 = 4.6 4.6 -2 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
137631599 156617 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4067967 156617 None 0 Human Functional pEC50 = 6.6 6.6 -16 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1694 20 20 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
90643848 111833 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287355 111833 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
137660671 159311 None 0 Human Functional pEC50 = 5.6 5.6 -812 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4098785 159311 None 0 Human Functional pEC50 = 5.6 5.6 -812 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1708 20 19 21 -2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
137658158 159811 None 0 Human Functional pEC50 = 5.6 5.6 -10 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4104465 159811 None 0 Human Functional pEC50 = 5.6 5.6 -10 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1714 21 22 21 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
16132144 211738 None 29 Mouse Functional pEC50 = 5.6 5.6 -8 8
Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
16133793 211738 None 29 Mouse Functional pEC50 = 5.6 5.6 -8 8
Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
44273719 211738 None 29 Mouse Functional pEC50 = 5.6 5.6 -8 8
Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 5.6 5.6 -8 8
Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(03)00318-4
44413880 77975 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
CHEMBL209587 77975 None 0 Human Functional pEC50 = 6.6 6.6 -10 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 639 14 6 7 0.7 NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1021/jm060384p
16132144 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00830-2
16133793 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00830-2
44273719 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00830-2
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00830-2
10257242 15036 None 0 Human Functional pEC50 = 7.6 7.6 39 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209252 15036 None 0 Human Functional pEC50 = 7.6 7.6 39 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 560 7 0 4 5.1 CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
10077258 15037 None 0 Human Functional pEC50 = 7.6 7.6 15 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
CHEMBL1209253 15037 None 0 Human Functional pEC50 = 7.6 7.6 15 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 596 8 0 5 4.5 CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O 10.1016/j.bmcl.2010.06.038
25132867 172601 None 0 Human Functional pEC50 = 7.6 7.6 15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL448337 172601 None 0 Human Functional pEC50 = 7.6 7.6 15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 623 11 2 5 3.9 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1 10.1021/jm800525p
CHEMBL2371888 212605 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL None None None CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(C)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
71452716 78924 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL2112920 78924 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL322610 213693 None 0 Mouse Functional pEC50 = 7.6 7.6 -2 4
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
16132144 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00459-6
16133793 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00459-6
44273719 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00459-6
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1016/s0960-894x(02)00459-6
71452716 78924 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL2112920 78924 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation
ChEMBL 781 22 9 8 -0.0 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O 10.1016/s0960-894x(02)01052-1
CHEMBL508501 217431 None 0 Human Functional pEC50 = 6.6 6.6 36 2
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/jm801300c
CHEMBL438596 216242 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
CHEMBL438596 216242 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
90643848 111833 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287355 111833 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 714 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44358630 28322 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 588 10 2 7 5.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL137452 28322 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 588 10 2 7 5.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL541866 28322 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 588 10 2 7 5.5 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL443590 216386 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
CHEMBL311175 213557 None 0 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
11845630 139601 None 0 Human Functional pEC50 = 6.6 6.6 4 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379490 139601 None 0 Human Functional pEC50 = 6.6 6.6 4 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N 10.1021/jm060384p
44394009 124417 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 571 9 3 5 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL363684 124417 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 571 9 3 5 3.7 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44413881 137680 None 0 Human Functional pEC50 = 6.6 6.6 4 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
CHEMBL375559 137680 None 0 Human Functional pEC50 = 6.6 6.6 4 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 707 15 6 7 1.9 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N 10.1021/jm060384p
46885324 8212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 432 3 2 3 3.4 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1092210 8212 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 432 3 2 3 3.4 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
45487287 200105 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL570903 200105 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 633 17 8 8 -0.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
46886010 7876 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 3 4.7 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
CHEMBL1089892 7876 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 3 4.7 CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1 10.1021/jm9017866
137649543 157412 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1025 18 12 15 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4077331 157412 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1025 18 12 15 -1.5 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
155549760 173981 None 0 Mouse Functional pEC50 = 7.6 7.6 -66 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4539621 173981 None 0 Mouse Functional pEC50 = 7.6 7.6 -66 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
1338 3807 None 36 Human Functional pEC50 = 7.6 7.6 -2 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
9938402 3807 None 36 Human Functional pEC50 = 7.6 7.6 -2 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL339053 3807 None 36 Human Functional pEC50 = 7.6 7.6 -2 8
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1021/jm050780s
CHEMBL2310901 211957 None 0 Human Functional pEC50 = 7.6 7.6 -4 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm049579s
CHEMBL5087859 217613 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44322959 156166 None 0 Human Functional pEC50 = 7.6 7.6 -13 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL406276 156166 None 0 Human Functional pEC50 = 7.6 7.6 -13 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 727 21 9 7 0.6 CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
11423083 96892 None 0 Mouse Functional pEC50 = 7.6 7.6 -26 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL265236 96892 None 0 Mouse Functional pEC50 = 7.6 7.6 -26 3
In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor
ChEMBL 882 32 9 7 4.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm0490843
CHEMBL3287327 213769 None 0 Human Functional pEC50 = 6.6 6.6 -5 4
Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155539948 172989 None 0 Mouse Functional pEC50 = 6.6 6.6 -131 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4515666 172989 None 0 Mouse Functional pEC50 = 6.6 6.6 -131 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 705 20 11 7 -0.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL138771 211213 None 0 Mouse Functional pEC50 = 6.6 6.6 1 3
Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells
ChEMBL None None None CC(=O)N(CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
44358705 96678 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL263461 96678 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 602 10 2 7 5.9 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2003.09.026
1334 1501 None 4 Human Functional pEC50 = 6.6 6.6 -6 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
16133814 1501 None 4 Human Functional pEC50 = 6.6 6.6 -6 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
CHEMBL437050 1501 None 4 Human Functional pEC50 = 6.6 6.6 -6 4
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm000211e
49789765 67253 None 0 Human Functional pEC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 363 4 1 5 4.7 COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1 nan
CHEMBL1879413 67253 None 0 Human Functional pEC50 = 4.6 4.6 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 363 4 1 5 4.7 COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1 nan
CHEMBL3600841 214278 None 0 Human Functional pEC50 = 6.6 6.6 -1 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
11845276 80084 None 0 Human Functional pEC50 = 6.6 6.6 2 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
CHEMBL212976 80084 None 0 Human Functional pEC50 = 6.6 6.6 2 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 605 14 4 4 4.9 N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1 10.1021/jm060384p
1334 1501 None 4 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
16133814 1501 None 4 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL437050 1501 None 4 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
90643838 111823 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 831 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287345 111823 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 831 10 3 5 4.1 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
44456304 155344 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 10 1 5 4.7 CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.10.115
CHEMBL402787 155344 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 609 10 1 5 4.7 CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.10.115
56676633 63702 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 641 6 1 3 7.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C 10.1016/j.bmcl.2010.06.062
CHEMBL1801121 63702 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 641 6 1 3 7.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C 10.1016/j.bmcl.2010.06.062
16132144 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
16133793 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44273719 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
CHEMBL214332 211738 None 29 Human Functional pEC50 = 7.6 7.6 -12 8
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm050780s
44394736 123383 None 0 Human Functional pEC50 = 7.6 7.6 25 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL361579 123383 None 0 Human Functional pEC50 = 7.6 7.6 25 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 797 19 9 7 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44390424 63948 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 645 10 1 6 4.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmcl.2005.01.060
CHEMBL180635 63948 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 645 10 1 6 4.8 CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmcl.2005.01.060
137660993 159541 None 0 Human Functional pEC50 = 7.6 7.6 -63 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 159541 None 0 Human Functional pEC50 = 7.6 7.6 -63 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44433448 88518 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 500 6 1 4 4.9 CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.079
CHEMBL234983 88518 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA
ChEMBL 500 6 1 4 4.9 CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.09.079
44433448 88518 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 500 6 1 4 4.9 CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL234983 88518 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 500 6 1 4 4.9 CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
145966716 164400 None 0 Human Functional pEC50 = 6.6 6.6 -70 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4212209 164400 None 0 Human Functional pEC50 = 6.6 6.6 -70 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 887 11 12 9 -0.3 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL2070254 211644 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
155567887 176152 None 0 Mouse Functional pEC50 = 6.6 6.6 1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4590532 176152 None 0 Mouse Functional pEC50 = 6.6 6.6 1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 676 19 10 7 -1.1 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
164623811 186006 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL4868636 186006 None 0 Mouse Functional pEC50 = 6.6 6.6 -1 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
ChEMBL 614 11 4 4 6.2 CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N 10.1021/acs.jmedchem.0c02041
CHEMBL438596 216242 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
44391940 12254 None 0 Human Functional pEC50 = 6.6 6.6 21 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1184624 12254 None 0 Human Functional pEC50 = 6.6 6.6 21 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL2145456 12254 None 0 Human Functional pEC50 = 6.6 6.6 21 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 614 8 4 6 2.1 C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44405366 71985 None 0 Human Functional pEC50 = 6.6 6.6 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 643 12 3 5 4.7 NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1 10.1016/j.bmcl.2005.08.061
CHEMBL197327 71985 None 0 Human Functional pEC50 = 6.6 6.6 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 643 12 3 5 4.7 NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1 10.1016/j.bmcl.2005.08.061
11375764 66710 None 0 Human Functional pEC50 = 5.6 5.6 -38 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL185469 66710 None 0 Human Functional pEC50 = 5.6 5.6 -38 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 515 6 3 3 5.2 C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1 10.1021/jm0400496
CHEMBL414778 215616 None 0 Human Functional pEC50 = 5.6 5.6 -478 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
90643850 111834 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287357 111834 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 711 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44359589 31487 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
CHEMBL140324 31487 None 0 Mouse Functional pEC50 = 4.6 4.6 -3 3
Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells
ChEMBL 685 20 4 7 1.4 CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1 10.1016/j.bmcl.2003.08.078
51350911 58821 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53322399 58821 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932357 58821 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688109 58821 None 0 Mouse Functional pEC50 = 5.6 5.6 -5 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
11156852 65706 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL183434 65706 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 531 7 3 5 2.9 NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
44394078 161811 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 611 10 3 6 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL413556 161811 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 611 10 3 6 4.3 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
90643834 111820 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287341 111820 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
56669816 63698 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 5 1 3 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1 10.1016/j.bmcl.2010.06.062
CHEMBL1801117 63698 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 625 5 1 3 7.1 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1 10.1016/j.bmcl.2010.06.062
25133907 176829 None 0 Human Functional pEC50 = 7.6 7.6 5 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460138 176829 None 0 Human Functional pEC50 = 7.6 7.6 5 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 518 9 2 4 3.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
162672255 182977 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
90643823 111784 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 696 18 9 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O 10.1021/jm500064t
CHEMBL3287074 111784 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 696 18 9 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O 10.1021/jm500064t
44323033 107208 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL316259 107208 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 747 19 10 7 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
162672255 182977 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4791788 182977 None 0 Human Functional pEC50 = 7.6 7.6 1 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1100 18 14 11 0.6 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL5077144 216973 None 0 Human Functional pEC50 = 7.6 7.6 -13 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44441645 94180 None 0 Human Functional pEC50 = 7.5 7.5 63 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL249277 94180 None 0 Human Functional pEC50 = 7.5 7.5 63 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 605 12 2 7 4.4 CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
137637656 156329 None 0 Human Functional pEC50 = 7.5 7.5 40 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4064777 156329 None 0 Human Functional pEC50 = 7.5 7.5 40 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL 1045 20 14 15 -2.2 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
145988867 167199 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4289983 167199 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 660 17 7 6 1.7 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
133053557 163801 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4204975 163801 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 851 11 12 9 -1.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
90643824 111811 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 842 11 3 7 3.4 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287330 111811 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 842 11 3 7 3.4 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
90643828 111815 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287335 111815 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 806 12 6 6 1.5 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
44405378 140652 None 0 Human Functional pEC50 = 6.6 6.6 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 655 10 3 5 4.1 NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1 10.1016/j.bmcl.2005.08.061
CHEMBL381197 140652 None 0 Human Functional pEC50 = 6.6 6.6 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 655 10 3 5 4.1 NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1 10.1016/j.bmcl.2005.08.061
44305956 102816 None 0 Mouse Functional pEC50 = 5.6 5.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
CHEMBL305132 102816 None 0 Mouse Functional pEC50 = 5.6 5.6 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 490 11 5 4 2.9 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00318-4
44441636 94065 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL248701 94065 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 520 9 2 4 4.8 CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
11512024 202941 None 0 Human Functional pEC50 = 6.6 6.6 -5 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
CHEMBL598616 202941 None 0 Human Functional pEC50 = 6.6 6.6 -5 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
46885326 8213 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 450 3 2 3 3.5 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1 10.1021/jm9017866
CHEMBL1092211 8213 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 450 3 2 3 3.5 C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1 10.1021/jm9017866
46228813 203906 None 0 Human Functional pEC50 = 5.5 5.5 -16 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 538 8 1 6 3.9 COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL604911 203906 None 0 Human Functional pEC50 = 5.5 5.5 -16 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 538 8 1 6 3.9 COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
49862378 15048 None 0 Human Functional pEC50 = 7.5 7.5 45 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
CHEMBL1209321 15048 None 0 Human Functional pEC50 = 7.5 7.5 45 4
Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation
ChEMBL 534 8 0 4 4.6 CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C 10.1016/j.bmcl.2010.06.038
11170774 158456 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay
ChEMBL 1180 19 13 12 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4089689 158456 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay
ChEMBL 1180 19 13 12 -0.4 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
137656180 159120 None 0 Mouse Functional pEC50 = 7.5 7.5 -13 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL4096678 159120 None 0 Mouse Functional pEC50 = 7.5 7.5 -13 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay
ChEMBL 1005 12 12 11 -2.0 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/acs.jmedchem.6b01707
CHEMBL2096759 211667 None 0 Human Functional pEC50 = 7.5 7.5 -7 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44391927 13996 None 0 Human Functional pEC50 = 7.5 7.5 57 3
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL1196971 13996 None 0 Human Functional pEC50 = 7.5 7.5 57 3
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL3216393 13996 None 0 Human Functional pEC50 = 7.5 7.5 57 3
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 557 7 3 5 2.9 CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1 10.1016/j.bmcl.2004.10.020
CHEMBL187125 211514 None 0 Human Functional pEC50 = 7.5 7.5 30 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)Nc1ccco1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL89270 218389 None 0 Human Functional pEC50 = 7.5 7.5 1 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL None None None NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1 10.1016/s0960-894x(03)00552-3
73353216 89510 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL2372046 89510 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
11181804 128574 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm049278i
CHEMBL366706 128574 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm049278i
CHEMBL2323789 211974 None 0 Mouse Functional pEC50 = 6.5 6.5 -147 3
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm301253y
73353216 89510 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/j.bmcl.2005.08.012
CHEMBL2372046 89510 None 0 Human Functional pEC50 = 6.5 6.5 5 2
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/j.bmcl.2005.08.012
11237444 127532 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
CHEMBL366042 127532 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release
ChEMBL 503 8 4 3 5.4 CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1 10.1021/jm0400496
11845813 139891 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
CHEMBL379879 139891 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 473 10 3 4 3.0 NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1 10.1021/jm060384p
11847312 79793 None 0 Human Functional pEC50 = 6.5 6.5 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL211798 79793 None 0 Human Functional pEC50 = 6.5 6.5 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 613 12 6 6 1.8 N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1 10.1021/jm060384p
CHEMBL3287338 213771 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
73353216 89510 None 0 Human Functional pEC50 = 5.5 5.5 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL2372046 89510 None 0 Human Functional pEC50 = 5.5 5.5 5 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 806 20 9 7 0.9 CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1 10.1016/s0960-894x(02)00830-2
90643802 111805 None 0 Human Functional pEC50 = 6.5 6.5 -14 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 6.5 6.5 -14 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL275303 213280 None 0 Human Functional pEC50 = 6.5 6.5 4 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
25128749 178575 None 0 Human Functional pEC50 = 8.5 8.5 37 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
CHEMBL466380 178575 None 0 Human Functional pEC50 = 8.5 8.5 37 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 560 10 2 4 3.2 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O 10.1021/jm800525p
73348634 89505 None 0 Human Functional pEC50 = 8.5 8.5 1 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 975 13 10 9 0.8 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
CHEMBL2371902 89505 None 0 Human Functional pEC50 = 8.5 8.5 1 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 975 13 10 9 0.8 CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O 10.1016/s0960-894x(03)00114-8
90643806 111809 None 0 Human Functional pEC50 = 8.5 8.5 -12 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 8.5 8.5 -12 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
44405681 71817 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 896 21 9 7 2.9 C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL196773 71817 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 896 21 9 7 2.9 C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O 10.1016/j.bmcl.2005.08.083
44405826 141358 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 848 21 9 7 2.5 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL383143 141358 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 848 21 9 7 2.5 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
44405857 159039 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 944 21 10 7 4.9 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O 10.1016/j.bmcl.2005.08.083
CHEMBL409589 159039 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 944 21 10 7 4.9 N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O 10.1016/j.bmcl.2005.08.083
44401522 12788 None 0 Human Functional pEC50 = 8.5 8.5 97 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL1188041 12788 None 0 Human Functional pEC50 = 8.5 8.5 97 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
CHEMBL534928 12788 None 0 Human Functional pEC50 = 8.5 8.5 97 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 4 5 3.5 CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1 10.1016/j.bmcl.2005.02.068
44404522 72315 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 862 22 9 7 2.8 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL198309 72315 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 862 22 9 7 2.8 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.08.012
168284256 191055 None 0 Human Functional pEC50 = 8.5 8.5 -64 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5185775 191055 None 0 Human Functional pEC50 = 8.5 8.5 -64 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2383 48 33 31 -4.2 CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
16132144 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
16133793 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
44273719 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.5 8.5 -8 8
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm010061n
137659790 159416 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
CHEMBL4099889 159416 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
1323 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
92432 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
CHEMBL430239 2688 None 38 Human Functional pEC50 = 8.5 8.5 -33 7
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00353
49862749 15157 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 641 5 0 5 6.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1 10.1016/j.bmcl.2010.06.068
CHEMBL1209800 15157 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 641 5 0 5 6.6 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1 10.1016/j.bmcl.2010.06.068
CHEMBL3287327 213769 None 0 Mouse Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL5094215 217971 None 0 Human Functional pEC50 = 8.5 8.5 -15 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
137637026 156015 None 0 Human Functional pEC50 = 8.5 8.5 28 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4060937 156015 None 0 Human Functional pEC50 = 8.5 8.5 28 3
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1052 20 15 14 -1.4 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
11215553 8396 None 0 Human Functional pEC50 = 8.5 8.5 60 2
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093305 8396 None 0 Human Functional pEC50 = 8.5 8.5 60 2
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
145964017 164136 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
CHEMBL4208874 164136 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
ChEMBL 915 11 12 9 0.5 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.8b00488
90643803 111806 None 0 Human Functional pEC50 = 8.5 8.5 -3 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Human Functional pEC50 = 8.5 8.5 -3 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL438596 216242 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
44441641 94354 None 0 Human Functional pEC50 = 8.5 8.5 69 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL250508 94354 None 0 Human Functional pEC50 = 8.5 8.5 69 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 603 8 2 7 4.0 Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
16172929 215461 None 14 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None None 10.1021/jm0501432
CHEMBL412536 215461 None 14 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
ChEMBL None None None None 10.1021/jm0501432
11215553 8396 None 0 Human Functional pEC50 = 8.5 8.5 60 2
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1093305 8396 None 0 Human Functional pEC50 = 8.5 8.5 60 2
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
49862747 15154 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 615 6 1 5 6.1 CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL1209798 15154 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 615 6 1 5 6.1 CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL2371712 212568 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
CHEMBL413260 215519 None 0 Human Functional pEC50 = 8.5 8.5 5 2
Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm960845e
CHEMBL5075712 216882 None 0 Human Functional pEC50 = 8.5 8.5 -102 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
90643805 111808 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
90643808 111810 None 0 Human Functional pEC50 = 8.5 8.5 -14 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111810 None 0 Human Functional pEC50 = 8.5 8.5 -14 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
16132144 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
16133793 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
44273719 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
CHEMBL214332 211738 None 29 Human Functional pEC50 = 8.5 8.5 -12 8
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm201489a
CHEMBL501394 216625 None 0 Mouse Functional pEC50 = 8.5 8.5 2 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
46919520 15144 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 6
Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL1209788 15144 None 0 Mouse Functional pEC50 = 8.5 8.5 -3 6
Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 597 4 0 5 6.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N 10.1016/j.bmcl.2010.06.068
CHEMBL5090285 217743 None 0 Human Functional pEC50 = 8.5 8.5 -1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
90643805 111808 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Human Functional pEC50 = 8.5 8.5 1 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
168272660 190542 None 0 Human Functional pEC50 = 8.5 8.5 -28 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
CHEMBL5178164 190542 None 0 Human Functional pEC50 = 8.5 8.5 -28 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 2202 33 32 24 -2.1 CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.2c00793
127047475 139836 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
132991507 139836 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3798421 139836 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL 1630 54 21 19 -1.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.5b01894
CHEMBL3287338 213771 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3349030 213864 None 0 Human Functional pEC50 = 8.4 8.4 -1 3
Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O 10.1021/jm000211e
1338 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2003.09.036
9938402 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2003.09.036
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/j.bmcl.2003.09.036
44413914 139605 None 0 Human Functional pEC50 = 8.4 8.4 -12 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL379508 139605 None 0 Human Functional pEC50 = 8.4 8.4 -12 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 652 15 5 6 2.6 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
16132144 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
16133793 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
44273719 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.9b00198
44456222 97978 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
CHEMBL272538 97978 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 637 10 1 6 5.0 Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmcl.2007.10.115
11296600 123009 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
CHEMBL360716 123009 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm049278i
56679956 63721 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 675 4 0 3 7.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801214 63721 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 675 4 0 3 7.7 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1 10.1016/j.bmcl.2010.06.062
49862746 15153 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 601 5 1 5 5.7 CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL1209797 15153 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 601 5 1 5 5.7 CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
90643802 111805 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
11296600 123009 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 123009 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL5091245 217790 None 0 Human Functional pEC50 = 8.4 8.4 -5 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
44441644 154928 None 0 Human Functional pEC50 = 8.4 8.4 66 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL400456 154928 None 0 Human Functional pEC50 = 8.4 8.4 66 3
Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production
ChEMBL 577 9 2 7 3.5 CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2006.11.084
CHEMBL322610 213693 None 0 Mouse Functional pEC50 = 8.4 8.4 -2 4
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
46885711 8072 None 0 Human Functional pEC50 = 7.5 7.5 123 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
CHEMBL1091150 8072 None 0 Human Functional pEC50 = 7.5 7.5 123 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 504 3 1 3 5.4 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1 10.1021/jm9017866
155543031 173284 None 0 Mouse Functional pEC50 = 7.5 7.5 -50 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4522298 173284 None 0 Mouse Functional pEC50 = 7.5 7.5 -50 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
44394692 66235 None 0 Human Functional pEC50 = 7.5 7.5 17 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL184466 66235 None 0 Human Functional pEC50 = 7.5 7.5 17 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
71459938 79012 None 0 Human Functional pEC50 = 7.5 7.5 4 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113043 79012 None 0 Human Functional pEC50 = 7.5 7.5 4 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
44393823 124041 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 676 9 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL362880 124041 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 676 9 2 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
44405450 72543 None 0 Human Functional pEC50 = 6.5 6.5 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 581 11 2 5 3.1 CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.08.061
CHEMBL199061 72543 None 0 Human Functional pEC50 = 6.5 6.5 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 581 11 2 5 3.1 CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1 10.1016/j.bmcl.2005.08.061
CHEMBL427205 215813 None 0 Human Functional pEC50 = 5.5 5.5 -21 3
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O 10.1021/jm0510326
155565321 175680 None 0 Mouse Functional pEC50 = 5.5 5.5 -100 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
CHEMBL4579448 175680 None 0 Mouse Functional pEC50 = 5.5 5.5 -100 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 718 13 5 6 0.7 CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C 10.1021/acs.jmedchem.9b00053
168274920 190372 None 0 Human Functional pEC50 = 6.5 6.5 -102 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5175444 190372 None 0 Human Functional pEC50 = 6.5 6.5 -102 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL321870 213691 None 0 Mouse Functional pEC50 = 6.5 6.5 -5 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
51350799 58818 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53323763 58818 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932356 58818 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688105 58818 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
44358698 30932 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 574 8 2 7 5.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1 10.1016/j.bmcl.2003.09.026
CHEMBL139803 30932 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R
ChEMBL 574 8 2 7 5.0 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1 10.1016/j.bmcl.2003.09.026
56676634 63705 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 5 1 3 7.5 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F 10.1016/j.bmcl.2010.06.062
CHEMBL1801124 63705 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 5 1 3 7.5 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F 10.1016/j.bmcl.2010.06.062
168272615 190496 None 0 Human Functional pEC50 = 6.5 6.5 -60 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5177494 190496 None 0 Human Functional pEC50 = 6.5 6.5 -60 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
137655905 158920 None 0 Human Functional pEC50 = 5.5 5.5 -74 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4094606 158920 None 0 Human Functional pEC50 = 5.5 5.5 -74 4
Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method
ChEMBL 1666 20 22 21 -3.9 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
44444507 94226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 9 2 5 5.7 CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL249571 94226 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 9 2 5 5.7 CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
25132524 176863 None 0 Human Functional pEC50 = 7.5 7.5 7 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
CHEMBL460349 176863 None 0 Human Functional pEC50 = 7.5 7.5 7 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 504 8 2 4 2.7 CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1 10.1021/jm800525p
44394690 124715 None 0 Human Functional pEC50 = 7.5 7.5 14 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL364119 124715 None 0 Human Functional pEC50 = 7.5 7.5 14 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 792 19 9 7 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44394658 168440 None 0 Human Functional pEC50 = 7.5 7.5 5 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL434329 168440 None 0 Human Functional pEC50 = 7.5 7.5 5 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 758 18 10 7 0.0 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
162672691 183307 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183307 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL5076315 216916 None 0 Human Functional pEC50 = 7.5 7.5 -3 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
90643837 111822 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 750 11 3 7 3.4 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287344 111822 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 750 11 3 7 3.4 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
155562237 175813 None 0 Mouse Functional pEC50 = 5.5 5.5 -1548 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4582276 175813 None 0 Mouse Functional pEC50 = 5.5 5.5 -1548 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 692 15 8 7 0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O 10.1021/acs.jmedchem.9b00053
9852256 175471 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4574756 175471 None 0 Mouse Functional pEC50 = 5.5 5.5 -7 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 632 15 8 7 0.3 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
45487300 199815 None 0 Mouse Functional pEC50 = 4.5 4.5 -10 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569086 199815 None 0 Mouse Functional pEC50 = 4.5 4.5 -10 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 605 15 8 8 -0.6 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O 10.1016/j.bmcl.2009.07.025
44413537 139634 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 739 10 10 7 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
CHEMBL379627 139634 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells
ChEMBL 739 10 10 7 0.8 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmcl.2006.04.050
172468874 197097 None 0 Human Functional pEC50 = 6.5 6.5 -6 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 863 11 12 10 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.2c01587
CHEMBL5438629 197097 None 0 Human Functional pEC50 = 6.5 6.5 -6 2
Agonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assayAgonist activity at human MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
ChEMBL 863 11 12 10 0.1 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2cc(N)ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/acs.jmedchem.2c01587
46228845 201844 None 0 Human Functional pEC50 = 4.5 4.5 -39 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 551 9 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591026 201844 None 0 Human Functional pEC50 = 4.5 4.5 -39 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 551 9 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
46228848 201855 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 551 8 0 6 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591061 201855 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 551 8 0 6 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
46228849 201867 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 595 10 0 7 4.8 CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21 10.1016/j.bmc.2010.01.049
CHEMBL591123 201867 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 595 10 0 7 4.8 CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21 10.1016/j.bmc.2010.01.049
46228847 201869 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 620 11 1 7 6.0 O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL591132 201869 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 620 11 1 7 6.0 O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1 10.1016/j.bmc.2010.01.049
46228842 201872 None 0 Human Functional pEC50 = 4.5 4.5 -38 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 592 8 1 6 4.3 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591194 201872 None 0 Human Functional pEC50 = 4.5 4.5 -38 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 592 8 1 6 4.3 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1 10.1016/j.bmc.2010.01.049
46228844 201873 None 0 Human Functional pEC50 = 4.5 4.5 -26 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 587 10 1 7 4.3 COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591195 201873 None 0 Human Functional pEC50 = 4.5 4.5 -26 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 587 10 1 7 4.3 COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
46228888 201943 None 0 Human Functional pEC50 = 4.5 4.5 -8 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 481 6 1 4 3.2 CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
CHEMBL591717 201943 None 0 Human Functional pEC50 = 4.5 4.5 -8 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 481 6 1 4 3.2 CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1 10.1016/j.bmc.2010.01.049
46228763 202642 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL596602 202642 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 525 7 1 4 4.6 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
46228659 202849 None 0 Human Functional pEC50 = 4.5 4.5 -20 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 537 8 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL598010 202849 None 0 Human Functional pEC50 = 4.5 4.5 -20 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 537 8 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
46228850 202883 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 544 9 2 6 3.9 O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL598208 202883 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 544 9 2 6 3.9 O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1 10.1016/j.bmc.2010.01.049
46228725 202913 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL598442 202913 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
46228841 202981 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 503 8 0 4 4.8 COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL598831 202981 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 503 8 0 4 4.8 COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
46228843 204102 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 543 8 1 5 4.6 COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL605970 204102 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 543 8 1 5 4.6 COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
11706338 204164 None 0 Human Functional pEC50 = 4.5 4.5 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL1237150 204164 None 0 Human Functional pEC50 = 4.5 4.5 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL1237166 204164 None 0 Human Functional pEC50 = 4.5 4.5 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
CHEMBL606399 204164 None 0 Human Functional pEC50 = 4.5 4.5 -33 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 523 7 2 5 4.2 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1 10.1016/j.bmc.2010.01.049
11846673 80025 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL212766 80025 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 515 11 3 4 3.1 CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
137643385 158223 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1069 21 13 16 -1.8 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
CHEMBL4087072 158223 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
ChEMBL 1069 21 13 16 -1.8 CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O 10.1021/acs.jmedchem.7b00353
90643836 111821 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287343 111821 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 803 17 10 7 -0.7 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
56666397 63695 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 5 1 3 7.0 CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801098 63695 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 5 1 3 7.0 CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
162672691 183307 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4795842 183307 None 0 Human Functional pEC50 = 7.5 7.5 4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
46885415 8281 None 0 Human Functional pEC50 = 7.5 7.5 10 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1092571 8281 None 0 Human Functional pEC50 = 7.5 7.5 10 3
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 468 4 1 3 4.5 C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL432201 216094 None 0 Human Functional pEC50 = 7.5 7.5 6 4
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm500064t
44444432 94457 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 491 6 0 5 4.4 CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.06.088
CHEMBL250976 94457 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 491 6 0 5 4.4 CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.06.088
44397356 66938 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 634 10 1 7 6.4 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL186557 66938 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 634 10 1 7 6.4 COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1 10.1016/j.bmcl.2005.06.033
44431512 146012 None 0 Human Functional pEC50 = 5.5 5.5 -87 4
Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL391796 146012 None 0 Human Functional pEC50 = 5.5 5.5 -87 4
Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation
ChEMBL 1038 14 12 10 0.9 CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O 10.1016/j.bmcl.2007.02.020
CHEMBL3287352 213773 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
51351024 58819 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53318435 58819 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932358 58819 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688106 58819 None 0 Mouse Functional pEC50 = 5.5 5.5 -13 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
11685018 203149 None 0 Human Functional pEC50 = 6.5 6.5 -204 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 519 5 1 4 4.4 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21 10.1016/j.bmc.2010.01.049
CHEMBL599867 203149 None 0 Human Functional pEC50 = 6.5 6.5 -204 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 519 5 1 4 4.4 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21 10.1016/j.bmc.2010.01.049
11627577 203648 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL603468 203648 None 0 Human Functional pEC50 = 5.5 5.5 -4 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 507 7 1 4 4.5 CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1 10.1016/j.bmc.2010.01.049
CHEMBL438596 216242 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
ChEMBL None None None CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm050780s
CHEMBL80803 218375 None 0 Human Functional pEC50 = 5.5 5.5 -9 2
Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor
ChEMBL None None None CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O 10.1016/s0960-894x(02)00459-6
10123761 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL283214 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/s0960-894x(02)00830-2
44275121 96539 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1022 13 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL262437 96539 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1022 13 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
11851038 140422 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
CHEMBL380691 140422 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
ChEMBL 497 6 0 5 5.2 CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1021/jm050780s
11636019 72384 None 0 Human Functional pEC50 = 7.5 7.5 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 655 10 3 5 4.3 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
CHEMBL198535 72384 None 0 Human Functional pEC50 = 7.5 7.5 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 655 10 3 5 4.3 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
49862739 15147 None 0 Human Functional pEC50 = 7.5 7.5 23 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 583 6 0 4 7.3 CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1 10.1016/j.bmcl.2010.06.068
CHEMBL1209791 15147 None 0 Human Functional pEC50 = 7.5 7.5 23 2
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 583 6 0 4 7.3 CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1 10.1016/j.bmcl.2010.06.068
44401585 13768 None 0 Human Functional pEC50 = 6.5 6.5 19 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL1195347 13768 None 0 Human Functional pEC50 = 6.5 6.5 19 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
CHEMBL554368 13768 None 0 Human Functional pEC50 = 6.5 6.5 19 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 585 8 3 5 3.6 CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C 10.1016/j.bmcl.2005.02.068
46232227 201626 None 0 Mouse Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589517 201626 None 0 Mouse Functional pEC50 = 5.5 5.5 -6 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 863 12 9 8 0.7 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
137660993 159541 None 0 Human Functional pEC50 = 6.5 6.5 -63 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4101216 159541 None 0 Human Functional pEC50 = 6.5 6.5 -63 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1680 20 21 21 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
46228660 202850 None 0 Human Functional pEC50 = 6.5 6.5 -21 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 537 8 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL598011 202850 None 0 Human Functional pEC50 = 6.5 6.5 -21 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 537 8 1 5 4.5 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
90643808 111810 None 0 Human Functional pEC50 = 5.5 5.5 -14 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111810 None 0 Human Functional pEC50 = 5.5 5.5 -14 4
Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
11341811 120188 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 546 7 3 5 3.5 C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
CHEMBL351161 120188 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 546 7 3 5 3.5 C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1021/jm0304109
44393863 127620 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 642 9 4 6 4.4 CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL366321 127620 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 642 9 4 6 4.4 CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL439691 216309 None 0 Human Functional pEC50 = 7.5 7.5 -5 3
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
44391938 11750 None 0 Human Functional pEC50 = 7.5 7.5 20 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL1181567 11750 None 0 Human Functional pEC50 = 7.5 7.5 20 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
CHEMBL2145455 11750 None 0 Human Functional pEC50 = 7.5 7.5 20 2
Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
ChEMBL 599 9 3 5 3.9 CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1 10.1016/j.bmcl.2004.10.020
44397220 167400 None 0 Human Functional pEC50 = 7.5 7.5 28 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL429387 167400 None 0 Human Functional pEC50 = 7.5 7.5 28 3
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
ChEMBL 582 7 2 4 4.7 CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2 10.1016/j.bmcl.2005.05.109
CHEMBL438030 216205 None 0 Human Functional pEC50 = 7.5 7.5 -21 3
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O 10.1021/jm030119t
CHEMBL204864 211625 None 0 Human Functional pEC50 = 6.5 6.5 -12 4
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
ChEMBL None None None CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O 10.1021/jm0510326
44455893 155728 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 651 10 1 5 5.5 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1 10.1016/j.bmcl.2007.10.115
CHEMBL404706 155728 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production
ChEMBL 651 10 1 5 5.5 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1 10.1016/j.bmcl.2007.10.115
CHEMBL409636 215233 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/jm030119t
44349228 18822 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 538 9 0 4 4.4 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
CHEMBL127861 18822 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 538 9 0 4 4.4 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
44305770 205252 None 0 Mouse Functional pEC50 = 5.5 5.5 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL62228 205252 None 0 Mouse Functional pEC50 = 5.5 5.5 1 3
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
ChEMBL 448 9 5 4 2.2 NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1 10.1016/s0960-894x(03)00318-4
CHEMBL431242 216085 None 0 Mouse Functional pEC50 = 4.5 4.5 -1 3
Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010524p
46885713 7801 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 495 3 1 4 4.7 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1 10.1021/jm9017866
CHEMBL1089442 7801 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 495 3 1 4 4.7 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1 10.1021/jm9017866
44278195 98860 None 0 Human Functional pEC50 = 7.5 7.5 35 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 834 21 9 7 1.6 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL27848 98860 None 0 Human Functional pEC50 = 7.5 7.5 35 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 834 21 9 7 1.6 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1 10.1016/s0960-894x(02)00830-2
10123761 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/s0960-894x(02)00830-2
CHEMBL283214 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/s0960-894x(02)00830-2
44275119 169123 None 0 Human Functional pEC50 = 7.5 7.5 37 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1033 15 11 10 1.2 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL439361 169123 None 0 Human Functional pEC50 = 7.5 7.5 37 2
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1033 15 11 10 1.2 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O 10.1016/s0960-894x(03)00114-8
10123761 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
CHEMBL283214 99547 None 0 Human Functional pEC50 = 7.5 7.5 15 2
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 898 21 9 7 2.1 CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1 10.1016/j.bmcl.2005.08.083
CHEMBL185869 211512 None 0 Human Functional pEC50 = 7.5 7.5 6 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL None None None CCOC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL3600843 214280 None 0 Human Functional pEC50 = 7.5 7.5 -4 4
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
ChEMBL None None None CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.5b00102
51350673 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
53317148 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
91932362 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
CHEMBL1688104 58817 None 0 Mouse Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
ChEMBL 1635 23 20 21 -1.8 C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm101425m
25022598 95083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay
ChEMBL 613 6 2 5 5.1 Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2008.01.125
CHEMBL255007 95083 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay
ChEMBL 613 6 2 5 5.1 Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1 10.1016/j.bmcl.2008.01.125
CHEMBL500743 216612 None 0 Human Functional pEC50 = 5.5 5.5 -22 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O 10.1021/jm801300c
44456958 97457 None 0 Mouse Functional pEC50 = 4.5 4.5 -10 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
CHEMBL269837 97457 None 0 Mouse Functional pEC50 = 4.5 4.5 -10 3
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
ChEMBL 308 4 1 2 2.8 CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21 10.1021/jm701303z
49862744 15151 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 629 5 1 5 5.6 CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
CHEMBL1209795 15151 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release
ChEMBL 629 5 1 5 5.6 CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.068
11613741 201738 None 0 Human Functional pEC50 = 6.5 6.5 -223 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 555 8 1 5 4.7 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
CHEMBL590281 201738 None 0 Human Functional pEC50 = 6.5 6.5 -223 2
Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay
ChEMBL 555 8 1 5 4.7 COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1 10.1016/j.bmc.2010.01.049
16172929 215461 None 14 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
CHEMBL412536 215461 None 14 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL None None None None 10.1021/jm500064t
11181804 128574 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL366706 128574 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 641 11 3 6 4.8 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
145988152 167140 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
CHEMBL4288909 167140 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay
ChEMBL 720 17 7 6 2.3 CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.ejmech.2018.04.021
44413828 139380 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
CHEMBL379168 139380 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 632 12 5 5 4.0 N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1 10.1021/jm060384p
90661465 77191 None 0 Human Functional pEC50 = 7.4 7.4 46 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2028958 77191 None 0 Human Functional pEC50 = 7.4 7.4 46 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
CHEMBL2078649 77191 None 0 Human Functional pEC50 = 7.4 7.4 46 2
Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
ChEMBL 693 9 5 6 4.0 CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O 10.1016/j.bmcl.2005.02.068
44393809 66199 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 589 11 4 6 2.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL184325 66199 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor
ChEMBL 589 11 4 6 2.9 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1 10.1016/j.bmcl.2004.06.059
CHEMBL438920 216270 None 0 Human Functional pEC50 = 7.4 7.4 -12 4
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON 10.1021/jm049579s
168295644 192421 None 0 Human Functional pEC50 = 6.4 6.4 1 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
CHEMBL5206336 192421 None 0 Human Functional pEC50 = 6.4 6.4 1 4
Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis
ChEMBL 1106 17 13 12 1.5 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c01848
11375529 120215 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL351400 120215 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 502 6 2 4 3.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL427629 215818 None 0 Human Functional pEC50 = 6.4 6.4 -2 3
Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O 10.1021/jm030119t
44405365 71970 None 0 Human Functional pEC50 = 6.4 6.4 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 641 10 3 5 4.6 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
CHEMBL197278 71970 None 0 Human Functional pEC50 = 6.4 6.4 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 641 10 3 5 4.6 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
46203213 7960 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1 10.1021/jm9017866
CHEMBL1090486 7960 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1 10.1021/jm9017866
CHEMBL1204058 7960 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 471 3 1 4 4.2 C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1 10.1021/jm9017866
137659790 159416 None 0 Human Functional pEC50 = 5.4 5.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL4099889 159416 None 0 Human Functional pEC50 = 5.4 5.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL 1728 21 21 21 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.8b00170
CHEMBL5077811 217004 None 0 Human Functional pEC50 = 5.4 5.4 -87 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O 10.1021/acs.jmedchem.1c00095
46885863 8474 None 0 Human Functional pEC50 = 6.4 6.4 41 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1093858 8474 None 0 Human Functional pEC50 = 6.4 6.4 41 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 446 3 1 3 3.8 C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
25128751 173688 None 0 Human Functional pEC50 = 7.4 7.4 23 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
CHEMBL453300 173688 None 0 Human Functional pEC50 = 7.4 7.4 23 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 629 11 2 6 4.0 CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1 10.1021/jm800525p
25128748 190100 None 0 Human Functional pEC50 = 7.4 7.4 8 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
CHEMBL517108 190100 None 0 Human Functional pEC50 = 7.4 7.4 8 3
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 490 7 2 4 2.3 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O 10.1021/jm800525p
44577510 188843 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
CHEMBL504986 188843 None 0 Human Functional pEC50 = 7.4 7.4 -4 4
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 893 12 11 11 0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701181n
44275191 81920 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL216474 81920 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).
ChEMBL 1066 13 11 9 1.6 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
11330869 120044 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 599 8 2 5 4.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL349886 120044 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 599 8 2 5 4.4 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
44349470 16940 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 589 11 1 5 4.9 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
CHEMBL125308 16940 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor
ChEMBL 589 11 1 5 4.9 CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2003.10.056
44405426 135862 None 0 Human Functional pEC50 = 7.4 7.4 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 669 11 3 5 4.7 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
CHEMBL373037 135862 None 0 Human Functional pEC50 = 7.4 7.4 - 1
cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R
ChEMBL 669 11 3 5 4.7 O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1 10.1016/j.bmcl.2005.08.061
46884748 8398 None 0 Human Functional pEC50 = 7.4 7.4 16 2
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL1093307 8398 None 0 Human Functional pEC50 = 7.4 7.4 16 2
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.02.058
CHEMBL3350327 213929 None 0 Mouse Functional pEC50 = 5.4 5.4 2 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
45487410 199894 None 0 Mouse Functional pEC50 = 5.4 5.4 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL569696 199894 None 0 Mouse Functional pEC50 = 5.4 5.4 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 655 16 8 6 1.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O 10.1016/j.bmcl.2009.07.025
44448477 95610 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 577 6 1 3 6.6 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257615 95610 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 577 6 1 3 6.6 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1 10.1016/j.bmcl.2008.04.049
162643435 181773 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181773 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
162643435 181773 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
CHEMBL4776340 181773 None 0 Human Functional pEC50 = 6.4 6.4 -4 2
Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL 1150 18 14 11 1.8 CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O 10.1021/acs.jmedchem.0c01620
46885416 8282 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 472 6 1 4 3.6 COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
CHEMBL1092572 8282 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 472 6 1 4 3.6 COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1 10.1021/jm9017866
90643830 111817 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 787 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL3287337 111817 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 787 10 4 6 2.2 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O 10.1021/jm500064t
CHEMBL2304250 211945 None 0 Mouse Functional pEC50 = 4.4 4.4 -6 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O 10.1021/jm0492756
44409337 170564 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
CHEMBL444883 170564 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist potency at MC4 receptorAgonist potency at MC4 receptor
ChEMBL 721 19 7 6 3.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1 10.1016/j.bmcl.2005.12.005
44349019 114501 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 2
In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
CHEMBL333283 114501 None 0 Mouse Functional pEC50 = 7.4 7.4 -1 2
In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)
ChEMBL 583 8 2 7 3.1 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1 10.1016/s0960-894x(03)00796-0
44394581 122215 None 0 Human Functional pEC50 = 7.4 7.4 12 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL359702 122215 None 0 Human Functional pEC50 = 7.4 7.4 12 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 755 19 9 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322987 96785 None 0 Human Functional pEC50 = 7.4 7.4 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL264306 96785 None 0 Human Functional pEC50 = 7.4 7.4 -8 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 713 20 9 7 0.2 CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
44322788 157475 None 0 Human Functional pEC50 = 7.4 7.4 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL407825 157475 None 0 Human Functional pEC50 = 7.4 7.4 -5 3
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 699 19 9 7 -0.2 CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
90643841 111826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287348 111826 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 828 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
155563055 175399 None 0 Mouse Functional pEC50 = 6.4 6.4 -75 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
CHEMBL4573041 175399 None 0 Mouse Functional pEC50 = 6.4 6.4 -75 3
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
ChEMBL 686 18 9 7 0.5 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.9b00053
9960253 117013 None 0 Human Functional pEC50 = 6.4 6.4 25 2
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
CHEMBL338594 117013 None 0 Human Functional pEC50 = 6.4 6.4 25 2
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 595 8 3 6 2.8 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/s0960-894x(03)00796-0
44349133 117348 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 665 11 2 6 3.8 CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
CHEMBL339545 117348 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 665 11 2 6 3.8 CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/s0960-894x(03)00796-0
137634090 156390 None 0 Human Functional pEC50 = 5.4 5.4 -2 5
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
CHEMBL4065418 156390 None 0 Human Functional pEC50 = 5.4 5.4 -2 5
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
ChEMBL 3980 69 56 64 -22.2 CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2 10.1021/acs.jmedchem.8b00251
155512534 169795 None 0 Mouse Functional pEC50 = 5.4 5.4 -42 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
CHEMBL4437801 169795 None 0 Mouse Functional pEC50 = 5.4 5.4 -42 3
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
ChEMBL 642 16 7 6 1.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acsmedchemlett.9b00198
46232221 201625 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
CHEMBL589516 201625 None 0 Mouse Functional pEC50 = 5.4 5.4 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay
ChEMBL 835 12 9 8 -0.1 N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2009.12.010
45487290 199236 None 0 Mouse Functional pEC50 = 4.4 4.4 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
CHEMBL565474 199236 None 0 Mouse Functional pEC50 = 4.4 4.4 -12 3
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL 579 17 9 7 -1.2 N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O 10.1016/j.bmcl.2009.07.025
11846844 140166 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL380051 140166 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 678 15 5 6 3.6 CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
44405823 72992 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 907 21 8 7 4.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
CHEMBL200668 72992 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation
ChEMBL 907 21 8 7 4.9 CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1 10.1016/j.bmcl.2005.08.083
11421919 120045 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 585 8 2 5 4.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
CHEMBL349887 120045 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
ChEMBL 585 8 2 5 4.0 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1 10.1021/jm0304109
44394654 124040 None 0 Human Functional pEC50 = 7.4 7.4 9 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL362879 124040 None 0 Human Functional pEC50 = 7.4 7.4 9 3
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 775 20 8 7 1.7 CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44442978 153165 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 537 8 1 5 4.8 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
CHEMBL397607 153165 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release
ChEMBL 537 8 1 5 4.8 CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1 10.1016/j.bmcl.2007.10.032
44444448 94116 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 523 6 1 5 4.0 CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.06.088
CHEMBL248964 94116 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 523 6 1 5 4.0 CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2007.06.088
CHEMBL105113 210925 None 0 Mouse Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
ChEMBL None None None CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm800291b
15953833 79005 None 0 Human Functional pEC50 = 6.4 6.4 8 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
CHEMBL2113037 79005 None 0 Human Functional pEC50 = 6.4 6.4 8 4
Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay
ChEMBL 622 9 2 6 6.6 COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.033
46865980 8470 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1093846 8470 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 470 3 1 3 4.8 C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
25131477 178806 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL468252 178806 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay
ChEMBL 547 10 2 5 2.2 CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O 10.1021/jm800525p
CHEMBL5075506 216867 None 0 Human Functional pEC50 = 6.4 6.4 -676 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2 10.1021/acs.jmedchem.1c00095
168296647 192584 None 0 Human Functional pEC50 = 6.4 6.4 -213 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
CHEMBL5208830 192584 None 0 Human Functional pEC50 = 6.4 6.4 -213 4
Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay
ChEMBL 1319 15 14 15 0.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O 10.1021/acs.jmedchem.2c00793
49792705 67524 None 0 Human Functional pEC50 = 5.4 5.4 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 422 4 1 4 5.5 CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12 nan
CHEMBL1894685 67524 None 0 Human Functional pEC50 = 5.4 5.4 - 1
PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)
ChEMBL 422 4 1 4 5.5 CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12 nan
90643803 111806 None 0 Human Functional pEC50 = 8.4 8.4 -3 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287323 111806 None 0 Human Functional pEC50 = 8.4 8.4 -3 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 898 18 9 7 0.4 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
46885558 7811 None 0 Human Functional pEC50 = 8.4 8.4 151 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
CHEMBL1089483 7811 None 0 Human Functional pEC50 = 8.4 8.4 151 2
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 492 4 1 5 4.0 C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1 10.1021/jm9017866
46885483 8333 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 510 4 1 5 4.1 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1092861 8333 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 510 4 1 5 4.1 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
CHEMBL1204053 8333 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
ChEMBL 510 4 1 5 4.1 C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1 10.1021/jm9017866
15603023 98017 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL272660 98017 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 849 12 10 8 0.0 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
15602927 157974 None 0 Mouse Functional pEC50 = 8.4 8.4 1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
CHEMBL408398 157974 None 0 Mouse Functional pEC50 = 8.4 8.4 1 4
Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells
ChEMBL 835 12 10 8 -0.4 N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701093y
16132144 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
16133793 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
44273719 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
CHEMBL214332 211738 None 29 Mouse Functional pEC50 = 8.4 8.4 -8 8
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acs.jmedchem.5b01894
44275263 162020 None 0 Human Functional pEC50 = 8.4 8.4 478 2
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL 1022 13 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
CHEMBL415341 162020 None 0 Human Functional pEC50 = 8.4 8.4 478 2
Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation
ChEMBL 1022 13 11 9 1.5 CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O 10.1016/s0960-894x(03)00114-8
1338 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
9938402 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
CHEMBL339053 3807 None 36 Human Functional pEC50 = 8.4 8.4 -2 8
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
ChEMBL 588 8 2 6 4.6 O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl 10.1016/s0960-894x(03)00796-0
44390411 63917 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 609 8 2 6 2.8 CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
CHEMBL180487 63917 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor
ChEMBL 609 8 2 6 2.8 CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O 10.1016/j.bmcl.2005.01.060
44404523 135449 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 882 22 9 7 3.1 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.08.012
CHEMBL372785 135449 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
ChEMBL 882 22 9 7 3.1 CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.08.012
10408 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
5329 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
9941379.0 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
CHEMBL2070241 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
DB11653 720 None 23 Human Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL None None None CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C 10.1021/acs.jmedchem.8b00170
171378344 195064 None 0 Human Functional pEC50 = 8.4 8.4 12 3
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 765 15 10 7 0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
CHEMBL5395890 195064 None 0 Human Functional pEC50 = 8.4 8.4 12 3
Agonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysisAgonist activity at human MC4R stably overexpressing in HEK293 cells assessed as intracellular acumulation of cAMP level incubated for 30 mins measured by microbeta 2 microplate counter analysis
ChEMBL 765 15 10 7 0.8 CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CNC1=O 10.1021/acs.jmedchem.2c01794
90643804 111807 None 0 Human Functional pEC50 = 8.4 8.4 -8 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287324 111807 None 0 Human Functional pEC50 = 8.4 8.4 -8 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 839 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
52944242 18160 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 609 4 1 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1 10.1016/j.bmcl.2010.09.049
CHEMBL1269572 18160 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor
ChEMBL 609 4 1 4 6.9 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1 10.1016/j.bmcl.2010.09.049
56683297 63706 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 5 1 3 7.5 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F 10.1016/j.bmcl.2010.06.062
CHEMBL1801125 63706 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 667 5 1 3 7.5 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F 10.1016/j.bmcl.2010.06.062
90643808 111810 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111810 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
90643827 111814 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287334 111814 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 920 15 7 6 1.9 CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL5092761 217878 None 0 Human Functional pEC50 = 8.4 8.4 -295 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2 10.1021/acs.jmedchem.1c00095
56676631 63690 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 7.0 CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1801093 63690 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 613 4 0 3 7.0 CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
56659468 63713 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 661 4 0 3 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1 10.1016/j.bmcl.2010.06.062
CHEMBL1801145 63713 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 661 4 0 3 7.3 Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1 10.1016/j.bmcl.2010.06.062
44413931 78044 None 0 Human Functional pEC50 = 8.4 8.4 9 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
CHEMBL209789 78044 None 0 Human Functional pEC50 = 8.4 8.4 9 3
Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells
ChEMBL 643 16 5 6 1.9 CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N 10.1021/jm060384p
90643806 111809 None 0 Human Functional pEC50 = 8.4 8.4 -12 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287326 111809 None 0 Human Functional pEC50 = 8.4 8.4 -12 4
Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 728 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
90643805 111808 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Mouse Functional pEC50 = 8.4 8.4 -1 4
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL307457 213440 None 0 Mouse Functional pEC50 = 8.4 8.4 -10 3
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm010061n
CHEMBL5080489 217177 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2 10.1021/acs.jmedchem.1c00095
90643808 111810 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287328 111810 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 747 16 7 8 1.2 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
90643805 111808 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287325 111808 None 0 Human Functional pEC50 = 8.4 8.4 1 4
Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 917 20 11 7 -0.3 CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1021/jm500064t
90643802 111805 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
CHEMBL3287322 111805 None 0 Human Functional pEC50 = 8.4 8.4 -14 4
Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL 820 14 5 8 1.9 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1021/jm500064t
44448590 95652 None 0 Human Functional pEC50 = 8.3 8.3 25 3
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
CHEMBL257759 95652 None 0 Human Functional pEC50 = 8.3 8.3 25 3
Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release
ChEMBL 571 7 1 4 6.3 CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1 10.1016/j.bmcl.2008.04.049
11753695 8395 None 6 Human Functional pEC50 = 8.3 8.3 -3 7
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
CHEMBL1093304 8395 None 6 Human Functional pEC50 = 8.3 8.3 -3 7
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
ChEMBL 599 4 1 3 6.7 CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21 10.1016/j.bmcl.2010.06.062
24180493 155214 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 10 2 5 5.7 CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
CHEMBL402043 155214 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 635 10 2 5 5.7 CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.06.088
44394623 141625 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
CHEMBL384720 141625 None 0 Human Functional pEC50 = 8.3 8.3 1 2
Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor
ChEMBL 936 26 11 8 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/j.bmcl.2004.07.046
44322896 168075 None 0 Human Functional pEC50 = 8.3 8.3 1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
CHEMBL431801 168075 None 0 Human Functional pEC50 = 8.3 8.3 1 2
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
ChEMBL 789 22 10 7 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1016/s0960-894x(03)00552-3
155551699 175244 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1680 54 21 19 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
CHEMBL4569886 175244 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay
ChEMBL 1680 54 21 19 -0.0 CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b00238
57817763 76955 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
70690940 76955 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
91929808 76955 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
CHEMBL2070251 76955 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin
ChEMBL 1988 59 26 26 -3.2 CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O 10.1021/jm201489a
11296600 123009 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.03.053
CHEMBL360716 123009 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2005.03.053
11296600 123009 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
CHEMBL360716 123009 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor
ChEMBL 628 9 4 6 3.8 CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1 10.1016/j.bmcl.2004.06.059
11753695 8395 None 6 Human Functional pEC50 = 8.3 8.3 -3 7
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation <