LY-465608 [Ligand Id: 2659] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL25259
  • 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 6.77 pKi 170 nM Ki J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
ChEMBL Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha) B 6.76 pIC50 174 nM IC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
GtoPdb - - 6.8 pIC50 - - - J Med Chem (2001) 44: 2061-4 [PMID:11405642];
J Med Chem (2004) 47: 2422-5 [PMID:15115385]
ChEMBL Agonistic activity for Peroxisome proliferator activated receptor alpha F 6.82 pEC50 150 nM EC50 J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay B 6.82 pEC50 150 nM EC50 J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
ChEMBL Binding affinity at human PPAR alpha B 6.83 pEC50 149.5 nM EC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
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 6.26 pKi 550 nM Ki J Med Chem (2004) 47: 4118-4127 [PMID:15293980]
GtoPdb - - 6.26 pIC50 - - - J Med Chem (2001) 44: 2061-4 [PMID:11405642]
ChEMBL Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma) B 6.26 pIC50 548 nM IC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
ChEMBL Binding affinity at human PPAR gamma B 6.05 pEC50 882 nM EC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
ChEMBL Agonistic activity for human Peroxisome proliferator activated receptor gamma F 6.06 pEC50 880 nM EC50 J Med Chem (2003) 46: 1306-1317 [PMID:12672231]
ChEMBL Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay B 6.06 pEC50 880 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]