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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 |
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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 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]