Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T64795 | ||||
Target Name | Voltage-gated calcium channel alpha Cav3.1 (CACNA1G) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | IC50 = 369000 nM | [9] | ||
Ethosuximide | Drug Info | IC50 = 7000 nM | [8] | ||
Methsuximide | Drug Info | IC50 = 1100000 nM | [8] | ||
Verapamil | Drug Info | IC50 = 250 nM | [10] | ||
Drug Info | IC50 = 2460 nM | [3] | |||
Drug Info | IC50 = 41 nM | [7] | |||
Drug Info | IC50 = 2080 nM | [3] | |||
Drug Info | IC50 = 9230 nM | [3] | |||
Drug Info | IC50 = 3380 nM | [3] | |||
Cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamide | Drug Info | IC50 = 1010 nM | [2] | ||
KKHT-10608 | Drug Info | IC50 = 16870 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] | ||
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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