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

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ChEMBL ligand: CHEMBL2070241
  • MC1 receptor in Human [GtoPdb: 282] [UniProtKB: Q01726]
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  • MC3 receptor in Human [GtoPdb: 284] [UniProtKB: P41968]
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  • MC4 receptor in Human [GtoPdb: 285] [UniProtKB: P32245]
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  • MC5 receptor in Human [GtoPdb: 286] [UniProtKB: P33032]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MC1 receptor in Human [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]
MC3 receptor in Human [GtoPdb: 284] [UniProtKB: P41968]
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]
MC4 receptor in Human [GtoPdb: 285] [UniProtKB: P32245]
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];
Obstet Gynecol (2019) 134: 899-908 [PMID:31599840]
MC5 receptor in Human [GtoPdb: 286] [UniProtKB: P33032]
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 data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]