sparsentan [Ligand Id: 8448] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL539423 (PS-433540, PS433540, RE-021, Sparsentan)
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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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 - - 8.03 pKi 9.3 nM Ki J Med Chem (2005) 48: 6523-43 [PMID:16220969]
ChEMBL Inhibitory concentration against endothelin receptor type A B 8.03 pKi 9.3 nM Ki J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Binding affinity to ETA receptor B 8.03 pKi 9.3 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Inhibitory concentration against angiotensin II receptor, type 1 B 9.1 pKi 0.8 nM Ki J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Binding affinity to AT1 receptor B 9.1 pKi 0.8 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
GtoPdb - - 9.1 pKi 0.8 nM Ki J Med Chem (2005) 48: 6523-43 [PMID:16220969]

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]