FR139317 [Ligand Id: 998] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL352396
  • 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 - - 7.9 pIC50 12.6 nM IC50 Br J Pharmacol (1995) 115: 191-7 [PMID:7647976]
ChEMBL Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand. B 8.28 pIC50 5.3 nM IC50 Bioorg Med Chem Lett (1995) 5: 917-922
Sialin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630859] [GtoPdb: 1006] [UniProtKB: Q9NRA2]
ChEMBL Inhibition of human recombinant-Sialin expressed in HEK293 cells assessed as reduction in [3H]Neu5Ac uptake at 30 to 300 uM incubated for 15 mins by liquid scintillation counting method B 4.7 pKi 20000 nM Ki J Med Chem (2020) 63: 8231-8249 [PMID:32608236]

ChEMBL data shown on this page come from version 32:

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]