GW409544 [Ligand Id: 2656] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL410478 (GW409544)
  • 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]
ChEMBL Binding affinity for human peroxisome proliferator activated receptor alpha B 8.7 pKi 2 nM Ki J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
GtoPdb - - 8.7 pIC50 - - - J Med Chem (2004) 47: 4118-27 [PMID:15293980];
Proc Natl Acad Sci USA (2001) 98: 13919-24 [PMID:11698662]
ChEMBL Agonist activity at human PPAR-alpha B 6.62 pEC50 240 nM EC50 Bioorg Med Chem Lett (2014) 24: 2267-2272 [PMID:24745969]
ChEMBL Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay F 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2010) 20: 2605-2608 [PMID:20299214]
ChEMBL Agonist activity at human PPARalpha F 8.64 pEC50 2.3 nM EC50 Bioorg Med Chem (2008) 16: 3800-3808 [PMID:18272370]
ChEMBL Agonist activity at GAL4-fused human PPARalpha LBD B 8.64 pEC50 2.3 nM EC50 Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329]
ChEMBL Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay B 8.7 pEC50 2 nM EC50 J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Binding affinity for human peroxisome proliferator activated receptor gamma B 9 pKi 1 nM Ki J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
ChEMBL Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay F 8.57 pEC50 2.7 nM EC50 Bioorg Med Chem Lett (2010) 20: 2605-2608 [PMID:20299214]
GtoPdb - - 9.55 pEC50 - - - J Med Chem (2004) 47: 4118-27 [PMID:15293980];
Proc Natl Acad Sci USA (2001) 98: 13919-24 [PMID:11698662]
ChEMBL Agonist activity at human PPARgamma F 9.55 pEC50 0.28 nM EC50 Bioorg Med Chem (2008) 16: 3800-3808 [PMID:18272370]
ChEMBL Agonist activity at GAL4-fused human PPARgamma LBD B 9.55 pEC50 0.28 nM EC50 Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329]
ChEMBL Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay B 9.7 pEC50 0.2 nM EC50 J Med Chem (2004) 47: 4118-4127 [PMID:15293980]

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]