Ro 46-8443 [Ligand Id: 1011] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628620 (Ro-468443)
  • 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 radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes B 5.17 pIC50 6800 nM IC50 Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
ChEMBL Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1 B 7.16 pIC50 69 nM IC50 Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
GtoPdb - - 7.2 pIC50 69 nM IC50 FEBS Lett (1996) 383: 37-41 [PMID:8612786]

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]