Target Validation Information
TTD ID	T53585
Target Name	HMG-CoA reductase (HMGCR)
Type of Target	Successful
Drug Potency against Target	Atorvastatin	Drug Info	IC50 = 8.2 nM	[6]
	Fluvastatin	Drug Info	IC50 = 27.6 nM	[6]
	Lovastatin	Drug Info	IC50 = 24 nM	[7]
	Pravastatin	Drug Info	IC50 = 44.1 nM	[6]
	Rosuvastatin	Drug Info	IC50 = 5.4 nM	[6]
	Simvastatin	Drug Info	IC50 = 11.2 nM	[6]
	Teriflunomide	Drug Info	IC50 = 11 nM	[5]
	Cerivastatin	Drug Info	IC50 = 10 nM	[6]
	(E)-5-octadecen-7,9-diynoic acid	Drug Info	IC50 = 500 nM
	(E)-octadecan-9-ynoic acid	Drug Info	IC50 = 2000 nM
	(Z)-5-octadecen-7,9-diynoic acid	Drug Info	IC50 = 1500 nM
	(Z)-7-octedecan-9-ynoic acid	Drug Info	IC50 = 3000 nM
	3-(1,3 dodecadiynyl)-6-oxiranebutanoic acid	Drug Info	IC50 = 5000 nM
	3-Hydroxy-3-Methyl-Glutaric Acid	Drug Info	IC50 = 4000 nM	[1]
	6-hydroxy-7,9-octadecadiynoic acid	Drug Info	IC50 = 7000 nM
	7,9-octadecadiynoic acid	Drug Info	IC50 = 5000 nM
	7,9-tetradecadiynoic acid	Drug Info	IC50 = 3000 nM
	9-octadecynoic acid	Drug Info	IC50 = 5000 nM
	F(4-Fluoro)VAE	Drug Info	IC50 = 3800 nM	[3]
	GFPDGG	Drug Info	IC50 = 1500 nM	[3]
	GFPEGG	Drug Info	IC50 = 1700 nM	[3]
	GFPTGG	Drug Info	IC50 = 16900 nM	[3]
	GLPTGG	Drug Info	IC50 = 19400 nM	[3]
	PF-3052334	Drug Info	IC50 = 1.9 nM	[4]
	PITAVASTATIN CALCIUM	Drug Info	IC50 = 10550 nM	[2]
Action against Disease Model	Lovastatin	Drug Info	IC50 on sterol synthesis in h uMan myoblasts in culture: 19nM	[8]
	Pravastatin	Drug Info	IC50 on sterol synthesis in h uMan myoblasts in culture: 110nM	[8]
	Simvastatin	Drug Info	IC50 on sterol synthesis in h uMan myoblasts in culture: 4.0nM	[8]
References
REF 1	Molecular docking of the highly hypolipidemic agent alpha-asarone with the catalytic portion of HMG-CoA reductase. Bioorg Med Chem Lett. 2005 Feb 15;15(4):989-94.
REF 2	Synthesis and HMG CoA reductase inhibition of 4-thiophenyl quinolines as potential hypocholesterolemic agents. Bioorg Med Chem. 2007 Dec 15;15(24):7809-29.
REF 3	Binding effect and design of a competitive inhibitory peptide for HMG-CoA reductase through modeling of an active peptide backbone. Bioorg Med Chem. 2008 Feb 1;16(3):1309-18.
REF 4	Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylca... J Med Chem. 2008 Jan 10;51(1):31-45.
REF 5	Comparative pharmacology of rosuvastatin. Atheroscler Suppl. 2003 Mar;4(1):9-14.
REF 6	New lipid-lowering agents acting on LDL receptors. Curr Top Med Chem. 2005;5(3):233-42.
REF 7	Pravastatin inhibited the cholesterol synthesis in human hepatoma cell line Hep G2 less than simvastatin and lovastatin, which is reflected in the upregulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase and squalene synthase. Biochem Pharmacol. 1993 Jun 9;45(11):2203-8.
REF 8	Action of lovastatin, simvastatin, and pravastatin on sterol synthesis and their antiproliferative effect in cultured myoblasts from human striated muscle. Biochem Pharmacol. 1996 Nov 8;52(9):1387-92.

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