T0070907 [Ligand Id: 3444] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL510698 |
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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 | Agonist activity at human PPARalpha expressed in CHO cells co-expressing GAL4-NHR-LBD assessed as transcriptional activation preincubated for 6 hrs followed by luciferin addition by luminescence method | B | 5.53 | pIC50 | 2950 | nM | IC50 | Bioorg Med Chem (2023) 78: 117130-117130 [PMID:36542958] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Antagonist activity at human PPARdelta assessed as effect on TIPP-703-induced activity | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4774-4778 [PMID:23891183] |
| ChEMBL | Inverse agonist activity at human PPARdelta expressed in CHO cells co-expressing GAL4-NHR-LBD assessed as transcriptional repression preincubated for 6 hrs followed by luciferin addition by luminescence method | B | 5.3 | pIC50 | >5000 | nM | IC50 | Bioorg Med Chem (2023) 78: 117130-117130 [PMID:36542958] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | J Biol Chem (2002) 277: 19649-57 [PMID:11877444] |
| ChEMBL | Antagonist activity at human PPARgamma receptor expressed in Saccharomyces cerevisiae AH109 co-transfected with mouse CBP assessed as inhibition of rosiglitazone-induced LBD-CBP interaction by alpha-galactosidase based yeast two hybrid assay | F | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2008) 43: 2699-2716 [PMID:18329752] |
| ChEMBL | Antagonist activity at PPAR gamma LBD (203 to 476 residues) (unknown origin) expressed in HEK293T cells co-transfected with pCMV-GAL4-PPARgamma-LBD-SV40-Renilla-luciferase assessed as reduction of rosiglitazone induced PPAR-gamma activation incubated for 24 hrs by dural-luciferase reporter assay | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2024) 67: 15738-15755 [PMID:39185622] |
| ChEMBL | Inverse agonist activity at human PPARgamma expressed in CHO cells co-expressing GAL4-NHR-LBD assessed as transcriptional repression preincubated for 6 hrs followed by luciferin addition by luminescence method | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Bioorg Med Chem (2023) 78: 117130-117130 [PMID:36542958] |
| ChEMBL | Inhibition of PPARgamma (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2024) 15: 1430-1432 [PMID:39291000] |
ChEMBL data shown on this page come from version 36:
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]
