pravastatin [Ligand Id: 2953] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1144 (C10AA03, Pravachol, Pravastatin, Pravator)
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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  • Organic anion transporter 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
  • Organic anion transporter 3/Solute carrier family 22 member 8 in Rat [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7]
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  • squalene monooxygenase/Squalene monooxygenase in Human [ChEMBL: CHEMBL3592] [GtoPdb: 2433] [UniProtKB: Q14534]
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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 - 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 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]