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 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]