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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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H don H acc LogP Smiles DOI
1324 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
16154396 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
16197727 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
44285019 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
57514683 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
91898441 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL441738 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
DB04931 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
1324 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 288 15 MC4R MC4 receptor Human 10.8 pEC50 = 10.8 Functional
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 206567 0 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 206972 0 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 288 15 MC4R MC4 receptor Human 10.7 pEC50 = 10.7 Functional
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 170411 0 MC4R MC4 receptor Human 10.5 pEC50 = 10.5 Functional
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 170411 0 MC4R MC4 receptor Human 10.5 pEC50 = 10.5 Functional
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 76330 0 MC4R MC4 receptor Human 10.4 pEC50 = 10.4 Functional
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 76330 0 MC4R MC4 receptor Human 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Human 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Human 10.4 pEC50 = 10.4 Functional
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 2527 44 MC4R MC4 receptor Human 10.4 pEC50 = 10.4 Functional
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 115499 0 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Functional
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 115499 0 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Functional
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
1323 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
92432 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
CHEMBL430239 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL None None None None 10.1021/ml500340z
118722937 115495 0 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Functional
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 115495 0 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Functional
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
1323 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
92432 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL430239 2527 44 MC4R MC4 receptor Mouse 10.3 pEC50 = 10.3 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
1323 2527 44 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
92432 2527 44 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
CHEMBL430239 2527 44 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm0303103
118722933 115492 0 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 115492 0 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 174289 0 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Functional
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 174289 0 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Functional
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 206710 0 MC4R MC4 receptor Human 10.2 pEC50 = 10.2 Functional
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 203662 0 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 115502 0 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 115502 0 MC4R MC4 receptor Mouse 10.2 pEC50 = 10.2 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
92432 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL430239 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
1323 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Functional
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 2527 44 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Functional
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 80940 0 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Functional
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 80940 0 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Functional
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
44327392 141062 0 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL 1025 21 12 12 -0.6 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/jm0104872
CHEMBL386583 141062 0 MC4R MC4 receptor Mouse 10.1 pEC50 = 10.1 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL 1025 21 12 12 -0.6 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/jm0104872
1324 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 288 15 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 115490 0 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 115490 0 MC4R MC4 receptor Mouse 10.0 pEC50 = 10.0 Functional
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 206511 0 MC4R MC4 receptor Human 10.0 pEC50 = 10 Functional
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 17787 0 MC4R MC4 receptor Human 10.0 pEC50 = 10.0 Functional
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 17787 0 MC4R MC4 receptor Human 10.0 pEC50 = 10.0 Functional
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 203786 0 MC4R MC4 receptor Human 10.0 pEC50 = 10.0 Functional
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 206198 0 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
16154396 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
16197727 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
44285019 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
57514683 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
91898441 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
DB04931 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm800291b
1324 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
16154396 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
16197727 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
44285019 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
57514683 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
91898441 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
DB04931 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 None 10.1021/jm500064t
90643803 111012 0 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 111012 0 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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
118722926 115487 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115487 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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
CHEMBL2369959 203263 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
118722931 115491 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115491 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115496 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115496 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115500 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115500 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115501 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 115501 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Human 9.9 pEC50 = 9.9 Functional
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 135660 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 135660 0 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16154396 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
16197727 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
44285019 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
57514683 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
91898441 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
DB04931 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R
ChEMBL None None None None 10.1016/j.bmcl.2009.07.025
1324 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 288 15 MC4R MC4 receptor Mouse 9.9 pEC50 = 9.9 Functional
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 76331 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 76331 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 76331 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 76331 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 135660 0 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Functional
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 135660 0 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Functional
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 204221 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
16154396 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
16197727 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
44285019 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
57514683 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
91898441 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
DB04931 288 15 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm049010r
57646441 76329 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 76329 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Functional
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 202359 0 MC4R MC4 receptor Mouse 9.8 pEC50 = 9.8 Functional
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
CHEMBL217305 202896 0 MC4R MC4 receptor Human 9.8 pEC50 = 9.8 Binding
Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 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]2CCCN2C1=O 10.1016/s0960-894x(03)00412-8
CHEMBL2369484 203150 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 205537 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 115488 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 115488 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 204825 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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
CHEMBL415165 206688 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Binding
Effective concentration against human melanocortin-4 receptor Effective concentration against human melanocortin-4 receptor
ChEMBL None None None None 10.1021/jm0501432
1324 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 138475 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 138475 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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
137653739 157871 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 ADMET
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 1632 51 23 21 -3.6 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)CN[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.7b01295
CHEMBL4093140 157871 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 ADMET
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 1632 51 23 21 -3.6 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)CN[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.7b01295
10408 682 19 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 682 19 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 682 19 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 682 19 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 682 19 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 206054 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 203815 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16154396 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
16197727 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
44285019 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
57514683 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
91898441 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
DB04931 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm020296e
90643808 111016 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 111016 0 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16154396 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16197727 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
44285019 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
57514683 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
91898441 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
DB04931 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor
ChEMBL None None None None 10.1021/jm0303608
16132144 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against 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 10.1021/jm0303103
16133793 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against 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 10.1021/jm0303103
44273719 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against 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 10.1021/jm0303103
CHEMBL214332 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Binding
Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against 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 10.1021/jm0303103
16132144 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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 202802 28 MC4R MC4 receptor Human 9.7 pEC50 = 9.7 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
16154396 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
16197727 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
44285019 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
57514683 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
91898441 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
DB04931 288 15 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.
ChEMBL None None None None 10.1021/jm0104872
118722936 115494 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 115494 0 MC4R MC4 receptor Mouse 9.7 pEC50 = 9.7 Functional
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 17784 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 17784 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 203894 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 111011 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 111011 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 205542 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 682 19 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 682 19 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 682 19 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 682 19 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 682 19 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 63146 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 63146 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 206217 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 111013 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 111013 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 204132 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 202359 0 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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
CHEMBL2369963 203267 0 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)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)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
1324 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 288 15 MC4R MC4 receptor Mouse 9.6 pEC50 = 9.6 Functional
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 204252 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 207502 0 MC4R MC4 receptor Human 9.6 pEC50 = 9.6 Functional
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 114776 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 114776 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 111014 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 111014 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 118049 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 118049 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 118051 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 118051 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 79305 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 79305 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 205867 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 204441 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 205533 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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
CHEMBL3358542 205083 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
16154396 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
16197727 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
44285019 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
57514683 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
91898441 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
DB04931 288 15 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor
ChEMBL None None None None 10.1021/jm010061n
CHEMBL429236 207028 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 80542 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 80542 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 155171 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 155171 0 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 123203 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 123203 0 MC4R MC4 receptor Mouse 9.5 pEC50 = 9.5 Functional
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 2527 44 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 2527 44 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 2527 44 MC4R MC4 receptor Human 9.5 pEC50 = 9.5 Functional
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 206688 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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
CHEMBL2369967 203271 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=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)NC1=O 10.1021/jm049010r
56666386 63147 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 63147 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 63138 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 63138 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 206678 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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
1324 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 207502 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 111015 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 111015 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 288 15 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 205543 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 206514 12 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 206514 12 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 62913 1 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 62913 1 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 205888 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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
CHEMBL444219 207439 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 204824 0 MC4R MC4 receptor Human 9.4 pEC50 = 9.4 Functional
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 204248 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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 206069 0 MC4R MC4 receptor Mouse 9.4 pEC50 = 9.4 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 202708 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 123203 0 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 123203 0 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 140645 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 140645 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 166629 0 MC4R MC4 receptor Rat 9.3 pEC50 = 9.3 Functional
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 166629 0 MC4R MC4 receptor Rat 9.3 pEC50 = 9.3 Functional
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 205535 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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
CHEMBL365913 205557 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Binding
Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells
ChEMBL None None None CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)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/jm0490033
1324 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 206612 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 288 15 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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
CHEMBL264132 204121 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 191026 0 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 191026 0 MC4R MC4 receptor Mouse 9.3 pEC50 = 9.3 Functional
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 206663 0 MC4R MC4 receptor Human 9.3 pEC50 = 9.3 Functional
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 138955 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 138955 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 138955 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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
CHEMBL2369975 203279 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369982 203286 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL428801 206984 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 115497 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Functional
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 115497 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Functional
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 63773 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63773 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63136 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63136 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 14796 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 14796 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 2527 44 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 2527 44 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 2527 44 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63773 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63773 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 30886 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 30886 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 205536 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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
CHEMBL2369971 203275 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL2369960 203264 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
CHEMBL412523 206513 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 266 23 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 202802 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 202802 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 202802 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 202802 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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
CHEMBL2369983 203287 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 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](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
127046235 138843 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 138843 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 206950 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 206137 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Functional
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
CHEMBL2369964 203268 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Binding
Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)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)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049010r
56662904 63148 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 63148 0 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 111012 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Functional
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 111012 0 MC4R MC4 receptor Mouse 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 3572 28 MC4R MC4 receptor Human 9.2 pEC50 = 9.2 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63139 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63139 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 206351 0 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 206510 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 205340 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63123 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63123 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 170927 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 170927 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 14799 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 14799 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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
1324 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16154396 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
16197727 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
44285019 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
57514683 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
91898441 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL441738 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
DB04931 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 ADMET
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00301
CHEMBL3358537 205082 0 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 3572 28 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 3572 28 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 3572 28 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 205541 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 115498 0 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 115498 0 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 205544 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63116 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 63116 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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
16746686 17786 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 17786 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 168617 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 168617 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 168668 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 168668 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 171703 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 171703 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 93381 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 93381 0 MC4R MC4 receptor Human 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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 288 15 MC4R MC4 receptor Mouse 9.1 pEC50 = 9.1 Functional
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
44448660 94291 0 MC4R MC4 receptor Rat 9.1 pEC50 = 9.1 Functional
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 94291 0 MC4R MC4 receptor Rat 9.1 pEC50 = 9.1 Functional
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 63118 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63118 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 206876 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 204123 1 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 204142 0 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 172163 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 172163 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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
56683301 63142 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63142 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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
1324 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 3572 28 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 3572 28 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 3572 28 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 63140 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 63140 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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
70688853 76333 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 76333 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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
CHEMBL372201 134424 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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
CHEMBL411817 160405 0 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9 Functional
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 139539 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 139539 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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
CHEMBL3287059 204812 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 207573 0 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 205781 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63128 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63128 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63141 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 63141 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 14784 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 14784 0 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Mouse 9.0 pEC50 = 9.0 Functional
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 14785 0 MC4R MC4 receptor Rat 9.0 pEC50 = 9.0 Functional
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 14785 0 MC4R MC4 receptor Rat 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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 288 15 MC4R MC4 receptor Human 9.0 pEC50 = 9.0 Functional
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