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

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ChEMBL ligand: CHEMBL539423 (Filspari, 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 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]