Target Validation Information
TTD ID	T64795
Target Name	Voltage-gated calcium channel alpha Cav3.1 (CACNA1G)
Type of Target	Successful
Drug Potency against Target	Ethosuximide	Drug Info	IC50 = 7000 nM	[8]
	Methsuximide	Drug Info	IC50 = 1100000 nM	[8]
	Trimethadione	Drug Info	IC50 = 369000 nM	[9]
	Verapamil	Drug Info	IC50 = 250 nM	[10]
	Cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamide	Drug Info	IC50 = 1010 nM	[2]
	KKHT-10318	Drug Info	IC50 = 2460 nM	[3]
	KKHT-10608	Drug Info	IC50 = 16870 nM	[3]
	KKHT-10609	Drug Info	IC50 = 9230 nM	[3]
	KKHT-10618	Drug Info	IC50 = 2080 nM	[3]
	KKHT-11018	Drug Info	IC50 = 3380 nM	[3]
	KKHT-20718	Drug Info	IC50 = 3720 nM	[3]
	KKHT-20818	Drug Info	IC50 = 1520 nM	[3]
	KKHT-20918	Drug Info	IC50 = 1950 nM	[3]
	KYS-05001	Drug Info	IC50 = 1160 nM	[6]
	KYS-05040	Drug Info	IC50 = 14400 nM	[1]
	KYS-05050	Drug Info	IC50 = 130 nM	[4]
	KYS-05055	Drug Info	IC50 = 350 nM	[7]
	KYS-05056	Drug Info	IC50 = 380 nM	[7]
	KYS-05057	Drug Info	IC50 = 630 nM	[7]
	KYS-05064	Drug Info	IC50 = 960 nM	[5]
	KYS-05065	Drug Info	IC50 = 1040 nM	[7]
	KYS-05077	Drug Info	IC50 = 4200 nM	[4]
	KYS-05080	Drug Info	IC50 = 260 nM	[7]
	KYS-05090	Drug Info	IC50 = 41 nM	[7]
References
REF 1	3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.
REF 2	Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8.
REF 3	Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. Bioorg Med Chem. 2007 Jan 1;15(1):365-73.
REF 4	Synthesis and biological evaluation of novel T-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5.
REF 5	3D pharmacophore based virtual screening of T-type calcium channel blockers. Bioorg Med Chem. 2007 Jan 15;15(2):1091-105.
REF 6	Discovery of potent T-type calcium channel blocker. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3.
REF 7	T-type Ca2+ channel blockers suppress the growth of human cancer cells. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901.
REF 8	Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. J Bioenerg Biomembr. 2003 Dec;35(6):577-98.
REF 9	Evidence for involvement of the astrocytic benzodiazepine receptor in the mechanism of action of convulsant and anticonvulsant drugs. Life Sci. 1988;43(6):477-84.
REF 10	Specific calcium antagonist binding sites in brain. Life Sci. 1982 Oct 11;31(15):1575-85.

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