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 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]