nTzDpa [Ligand Id: 2699] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL370152
  • 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 Inhibitory concentration against human peroxisome proliferator activated receptor alpha in SPA assay B 4.82 pIC50 >15000 nM IC50 Bioorg Med Chem Lett (2005) 15: 5035-5038 [PMID:16153845]
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 to human PPARgamma (unknown origin) by competitive TR-FRET assay B 7.54 pKd 29 nM Kd J Med Chem (2013) 56: 1535-1543 [PMID:23286787]
GtoPdb - - 6.5 pIC50 - - - Mol Endocrinol (2003) 17: 662-76 [PMID:12554792]
ChEMBL Inhibitory concentration against human peroxisome proliferator activated receptor gamma in SPA assay B 7.59 pIC50 26 nM IC50 Bioorg Med Chem Lett (2005) 15: 5035-5038 [PMID:16153845]
ChEMBL Activity at human PPARgamma transfected in HEK293 cells assessed as transactivation activity by luciferase reporter gene assay B 7.24 pEC50 57 nM EC50 J Med Chem (2015) 58: 5381-5394 [PMID:25734377]
ChEMBL Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assay F 7.26 pEC50 55 nM EC50 Bioorg Med Chem Lett (2005) 15: 5035-5038 [PMID:16153845]

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]