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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