imiglitazar [Ligand Id: 2675] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL592054 (Imiglitazar, Tak-559, TAK-559)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
GtoPdb - - 7.17 pEC50 - - - Biochem Biophys Res Commun (2000) 278: 704-11 [PMID:11095972]
ChEMBL Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells F 8.1 pEC50 8 nM EC50 Bioorg Med Chem Lett (2008) 18: 6471-6475 [PMID:18976908]
ChEMBL Agonist activity at human full length PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by firefly luciferase assay F 8.3 pEC50 5 nM EC50 Bioorg Med Chem Lett (2010) 20: 1156-1161 [PMID:20022492]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells F 8.4 pEC50 4 nM EC50 Bioorg Med Chem Lett (2008) 18: 6471-6475 [PMID:18976908]
ChEMBL Agonist activity at human full length PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by firefly luciferase assay F 8.4 pEC50 4 nM EC50 Bioorg Med Chem Lett (2010) 20: 1156-1161 [PMID:20022492]

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]