Target Validation Information
Target ID T64795
Target Name Voltage-dependent T-type calcium channel alpha-1G subunit
Target Type
Successful
Drug Potency against Target KKHT-10318 Drug Info IC50 = 2460 nM [528476]
Ethosuximide Drug Info IC50 = 7000 nM [552415]
KYS-05090 Drug Info IC50 = 41 nM [529566]
KYS-05001 Drug Info IC50 = 1160 nM [529044]
KYS-05065 Drug Info IC50 = 1040 nM [529566]
KYS-05055 Drug Info IC50 = 350 nM [529566]
KYS-05057 Drug Info IC50 = 630 nM [529566]
KKHT-10618 Drug Info IC50 = 2080 nM [528476]
KKHT-10609 Drug Info IC50 = 9230 nM [528476]
KKHT-11018 Drug Info IC50 = 3380 nM [528476]
KKHT-20918 Drug Info IC50 = 1950 nM [528476]
KKHT-10608 Drug Info IC50 = 16870 nM [528476]
KYS-05064 Drug Info IC50 = 960 nM [528504]
KYS-05080 Drug Info IC50 = 260 nM [529566]
KYS-05056 Drug Info IC50 = 380 nM [529566]
KYS-05050 Drug Info IC50 = 130 nM [528495]
KYS-05077 Drug Info IC50 = 4200 nM [528495]
KKHT-20818 Drug Info IC50 = 1520 nM [528476]
Trimethadione Drug Info IC50 = 369000 nM [553134]
Cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamide Drug Info IC50 = 1010 nM [528344]
KYS-05040 Drug Info IC50 = 14400 nM [527099]
Verapamil Drug Info IC50 = 250 nM [553172]
KKHT-20718 Drug Info IC50 = 3720 nM [528476]
Methsuximide Drug Info IC50 = 1100000 nM [552415]
References
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 552415Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. J Bioenerg Biomembr. 2003 Dec;35(6):577-98.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 529044Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.Discovery of potent T-type calcium channel blocker.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 528504Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.3D pharmacophore based virtual screening of T-type calcium channel blockers.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 529566Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. Epub 2008 Jun 14.T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Ref 528495Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.Synthesis and biological evaluation of novel T-type calcium channel blockers.
Ref 528495Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.Synthesis and biological evaluation of novel T-type calcium channel blockers.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 553134Evidence 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 528344Bioorg Med Chem Lett. 2006 Oct 1;16(19):5244-8. Epub 2006 Jul 28.Morpholin-2-one derivatives as novel selective T-type Ca2+ channel blockers.
Ref 527099Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
Ref 553172Specific calcium antagonist binding sites in brain. Life Sci. 1982 Oct 11;31(15):1575-85.
Ref 528476Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.
Ref 552415Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. J Bioenerg Biomembr. 2003 Dec;35(6):577-98.

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