GSK0660 [Ligand Id: 3441] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL592652 (GSK0660) |
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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 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]
