bremelanotide [Ligand Id: 10408] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2070241 (PT-141, Bremelanotide)
  • MC1 receptor/Melanocortin receptor 1 in Human [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
1 CHEMBL2070241_lig_chart_1 Melanocortin receptor 1 Human
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
2 CHEMBL2070241_lig_chart_2 Melanocortin receptor 3 Human
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
3 CHEMBL2070241_lig_chart_3 Melanocortin receptor 4 Human
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
4 CHEMBL2070241_lig_chart_4 Melanocortin receptor 5 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MC1 receptor/Melanocortin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
GtoPdb Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC1 receptor. - 8.19 pKi 6.4 nM Ki J. Med. Chem. (2012) 55: 1969-77 [PMID:22335602]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin B 8.19 pKi 6.4 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay B 8.72 pKi 1.91 nM Ki J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
ChEMBL Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method B 10.02 pEC50 0.1 nM EC50 J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
ChEMBL Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay B 6.72 pKi 190.55 nM Ki J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin B 7.28 pKi 53 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
GtoPdb Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC3 receptor. - 7.28 pKi 53 nM Ki J. Med. Chem. (2012) 55: 1969-77 [PMID:22335602]
ChEMBL Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method B 8.62 pEC50 2.4 nM EC50 J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay B 7.61 pKi 24.55 nM Ki J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
GtoPdb Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC4 receptor. - 9.6 pKi 0.25 nM Ki J. Med. Chem. (2012) 55: 1969-77 [PMID:22335602]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin B 9.6 pKi 0.25 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method B 8.39 pEC50 4.07 nM EC50 J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
ChEMBL Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method B 9.61 pEC50 0.25 nM EC50 J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
ChEMBL Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin F 9.7 pEC50 0.2 nM EC50 J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin B 7.77 pKi 17 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
GtoPdb Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC5 receptor. - 7.77 pKi 17 nM Ki J. Med. Chem. (2012) 55: 1969-77 [PMID:22335602]
ChEMBL Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay B 6.71 pIC50 194.98 nM IC50 J Med Chem (2018) 61: 3674-3684 [PMID:29605997]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]