| 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 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 552415 | Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. J Bioenerg Biomembr. 2003 Dec;35(6):577-98. | ||||
| Ref 529566 | Bioorg 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 529044 | Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.Discovery of potent T-type calcium channel blocker. | ||||
| Ref 529566 | Bioorg 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 529566 | Bioorg 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 529566 | Bioorg 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 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 528504 | Bioorg 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 529566 | Bioorg 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 529566 | Bioorg 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 528495 | Bioorg 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 528495 | Bioorg 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 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 553134 | 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 528344 | Bioorg 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 527099 | Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers. | ||||
| Ref 553172 | Specific calcium antagonist binding sites in brain. Life Sci. 1982 Oct 11;31(15):1575-85. | ||||
| Ref 528476 | Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. | ||||
| Ref 552415 | Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. J Bioenerg Biomembr. 2003 Dec;35(6):577-98. | ||||
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