mitoglitazone [Ligand Id: 11303] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL146624 (CAY-10415, J730.386F, Mitoglitazone, MSD-9, MSDC-0160, PNU-91325, U-91325) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| mitochondrial pyruvate carrier 2/Mitochondrial pyruvate carrier 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295686] [GtoPdb: 3023] [UniProtKB: O95563] | ||||||||
| ChEMBL | Displacement of photoprobe from MPC2 (unknown origin) | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| mitochondrial pyruvate carrier 2 in Mouse [GtoPdb: 3023] [UniProtKB: Q9D023] | ||||||||
| GtoPdb | - | - | 5.89 | pIC50 | 1300 | nM | IC50 | Proc Natl Acad Sci U S A (2013) 110: 5422-7 [PMID:23513224] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Competitive displacement of fluorescently labelled PPAR tracer ligand from GST-tagged human PPARgamma ligand binding domain after 1 hr in dark by TR-FRET competitive binding assay | B | 4.65 | pIC50 | 22300 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| ChEMBL | Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay | B | 6.18 | pEC50 | 657 | nM | EC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| mitochondrial pyruvate carrier 1 in Mouse [GtoPdb: 3022] [UniProtKB: P63030] | ||||||||
| GtoPdb | - | - | 5.89 | pIC50 | 1300 | nM | IC50 | Proc Natl Acad Sci U S A (2013) 110: 5422-7 [PMID:23513224] |
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]
