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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL370152
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
There should be some charts here, you may need to enable JavaScript!
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 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]