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 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]