GSK0660 [Ligand Id: 3441] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL592652 (GSK0660)
  • 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-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
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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 Displacement of [3H]GW2433 from human PPARalpha receptor by ligand displacement assay B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 1857-1861 [PMID:20128594]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Binding affinity to PPAR-delta (unknown origin) by TR-FRET assay B 8.33 pKi 4.65 nM Ki J Med Chem (2020) 63: 16012-16027 [PMID:33325691]
ChEMBL Antagonist activity at human PPARdelta ligand binding domain-mediated transcriptional activity in CV1 cells by Gal4 chimera reporter assay B 6.5 pIC50 316.23 nM IC50 J. Med. Chem. (2010) 53: 1857-1861 [PMID:20128594]
GtoPdb - - 6.5 pIC50 300 nM IC50 Mol Endocrinol (2008) 22: 523-9 [PMID:17975020]
ChEMBL Inhibition of human PPARdelta receptor by ligand displacement assay B 6.8 pIC50 158.49 nM IC50 J. Med. Chem. (2010) 53: 1857-1861 [PMID:20128594]
ChEMBL Binding affinity to N-terminal hexa-histidine tagged and fluorescein-labeled human PPAR-beta/delta (164 to 441 residues) expressed in Escherichia coli BL21-DE3 incubated for 1 hr by fluorescence anisotropy B 6.81 pIC50 155 nM IC50 Eur. J. Med. Chem. (2015) 94: 229-236 [PMID:25768705]
ChEMBL Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assay B 5.27 pEC50 5400 nM EC50 Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
ChEMBL Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assay B 5.36 pEC50 4340 nM EC50 J Med Chem (2020) 63: 16012-16027 [PMID:33325691]
ChEMBL Antagonist at PPARdelta LBD (unknown origin) assessed as increase in recruitment of coactivator peptide C33 cotreated with PPARdelta agonist GW501516 by TR-FRET assay B 5.4 pEC50 4000 nM EC50 Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Displacement of fluormone Pan-PPAR Green from mouse recombinant GST-tagged PPARbeta/delta LBD after 60 mins by TR-FRET assay B 6.52 pIC50 >=300 nM IC50 J. Med. Chem. (2012) 55: 2858-2868 [PMID:22369181]
ChEMBL Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis F 7.32 pIC50 48 nM IC50 J. Med. Chem. (2012) 55: 2858-2868 [PMID:22369181]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Inhibition of human PPARgamma receptor by ligand displacement assay B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 1857-1861 [PMID:20128594]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]