endothelin-1 [Ligand Id: 989] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3775234
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
GtoPdb - - 8.5 pIC50 - - - Br J Pharmacol (1995) 115: 191-7 [PMID:7647976]
ChEMBL Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells B 10.64 pIC50 0.02 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method B 10.64 pIC50 0.02 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]