zibotentan [Ligand Id: 3539] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628688 (ZD-4054, ZD4054, Zibotentan)
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • ETB receptor/Endothelin receptor ET-B in Human [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
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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]
ChEMBL Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting B 7.68 pIC50 21 nM IC50 Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
GtoPdb - - 8.3 pIC50 5 nM IC50 Br J Cancer (2005) 92: 2148-52 [PMID:15956965]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
ChEMBL Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting B 7 pIC50 >100 nM IC50 Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]

ChEMBL data shown on this page come from version 34:

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]