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ChEMBL ligand: CHEMBL1144 (C10AA03, Pravachol, Pravastatin, Pravator) |
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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 | - | 6.99 | pKi | 103 | nM | Ki | Biochemistry (2005) 44: 11741-8 [PMID:16128575] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 5.86 | pIC50 | 1370 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1285-8 [PMID:11392538] |
ChEMBL | Inhibition of human HMGR catalytic domain using 800 uM HMG-CoA as substrate measured every 20 secs for 10 mins | B | 6.4 | pIC50 | 400 | nM | IC50 | J Nat Prod (2016) 79: 1500-1507 [PMID:27228159] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1992) 35: 2095-103 [PMID:1597859] |
ChEMBL | Tested in vitro for the inhibition of HMG-CoA reductase from partially purified microsomal preparations. | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1992) 35: 2095-2103 [PMID:1597859] |
ChEMBL | DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) | B | 8.25 | pIC50 | 5.59 | 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 | 7.5 | pIC50 | 31.6 | nM | IC50 | J Med Chem (2008) 51: 2722-2733 [PMID:18412317] |
ChEMBL | Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 31-45 [PMID:18072721] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 31-45 [PMID:18072721] |
GtoPdb | in vitro inhibition of cholesterol synthesis | - | 8.16 | pIC50 | 6.93 | nM | IC50 | Am J Cardiol (2001) 87: 28B-32B [PMID:11256847] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1993) 36: 3658-62 [PMID:8246234] |
GtoPdb | In vitro inhibition of HMG-CoA reductase | - | 8.38 | pEC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1285-8 [PMID:11392538] |
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] | ||||||||
ChEMBL | Inhibition of rat Oat1 expressed in pig LLC-PK11 cells | B | 4.28 | pKi | 52000 | nM | Ki | Bioorg Med Chem (2011) 19: 3320-3340 [PMID:21571536] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells | F | 4.86 | pIC50 | 13700 | nM | IC50 | J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells | F | 4.81 | pIC50 | 15600 | nM | IC50 | J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359] |
squalene monooxygenase/Squalene monooxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3592] [GtoPdb: 2433] [UniProtKB: Q14534] | ||||||||
ChEMBL | In vitro inhibitory activity against pig liver microsomal squalene epoxidase | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 3207-3216 [PMID:7650673] |
ChEMBL data shown on this page come from version 32:
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]