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 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]