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ChEMBL ligand: CHEMBL1477 (Baycol, Cerivastatin, Lipobay) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035] | ||||||||
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.24 | pKi | 5.7 | nM | Ki | Biochemistry (2005) 44: 11741-8 [PMID:16128575] |
GtoPdb | Inhibition of HMG-CoA reductase | - | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1027-32 [PMID:15686906] |
ChEMBL | Inhibitory concentration against 3-hydroxy-3-methylglutaryl-CoA reductase | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1027-1032 [PMID:15686906] |
ChEMBL | DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) | B | 10.07 | pIC50 | 0.09 | nM | IC50 | DrugMatrix in vitro pharmacology data |
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639] | ||||||||
ChEMBL | Inhibition of HMGR in rat hepatic microsomes assessed as conversion of [14C]HMG-CoA to [14C]mevalonic acid | B | 8.01 | pIC50 | 9.8 | nM | IC50 | J Med Chem (2008) 51: 2722-2733 [PMID:18412317] |
GtoPdb | in vitro inhibition of cholesterol synthesis | - | 8.45 | pIC50 | 3.54 | nM | IC50 | Am J Cardiol (2001) 87: 28B-32B [PMID:11256847] |
ChEMBL | Inhibition of rat microsomal HMG-CoA reductase assessed as inhibition of cholesterol synthesis after 30 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem (2007) 15: 5576-5589 [PMID:17560788] |
ChEMBL | Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2008) 51: 31-45 [PMID:18072721] |
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]