cerivastatin [Ligand Id: 2950] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
