AD-5061 [Ligand Id: 2663] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL59132 (AD-7057)
  • 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 towards human peroxidase proliferator activated receptor alpha (hPPARalpha) B 5.39 pIC50 4086 nM IC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
GtoPdb - - 5.6 pIC50 - - - Biochem Biophys Res Commun (2000) 278: 704-11 [PMID:11095972];
Eur J Pharmacol (2004) 495: 17-26 [PMID:15219816]
ChEMBL Binding affinity at human PPAR alpha B 6.11 pEC50 771 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 In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) B 8.37 pKi 4.27 nM Ki J Med Chem (1998) 41: 5020-5036 [PMID:9836620]
GtoPdb - - 7.7 pIC50 - - - Biochem Biophys Res Commun (2000) 278: 704-11 [PMID:11095972];
Eur J Pharmacol (2004) 495: 17-26 [PMID:15219816]
ChEMBL Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma) B 7.85 pIC50 14 nM IC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
ChEMBL Binding affinity at human PPAR gamma B 8.1 pEC50 8 nM EC50 J Med Chem (2001) 44: 2061-2064 [PMID:11405642]
ChEMBL Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells F 8.5 pEC50 3.16 nM EC50 J Med Chem (1998) 41: 5020-5036 [PMID:9836620]

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]