Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00161
Target NameVoltage-dependent T-type calcium channel alpha-1G subunit    
Type of TargetSuccessful target    
Drug Potency against TargetMethsuximideIC50 = 1100000 nM[1]
PregabalinIC50 = 16800 nM[2]
VerapamilIC50 = 250 nM[3]
TrimethadioneIC50 = 369000 nM[4]
EthosuximideIC50 = 7000 nM[1]
cis-N,5-dibenzyl-6-oxomorpholine-3-carboxamideIC50 = 1010 nM[5]
KYS-05065IC50 = 1040 nM[6]
KYS-05042IC50 = 110 nM[6]
KYS-05042IC50 = 110 nM[7]
KYS-05001IC50 = 1160 nM[8]
KYS-05050IC50 = 130 nM[9]
KYS-05040IC50 = 14400 nM[10]
KKHT-20818IC50 = 1520 nM[11]
KKHT-10608IC50 = 16870 nM[11]
KYS-05041IC50 = 170 nM[7]
KKHT-20918IC50 = 1950 nM[11]
KKHT-10618IC50 = 2080 nM[11]
KKHT-10318IC50 = 2460 nM[11]
KYS-05041IC50 = 250 nM[12]
KYS-05080IC50 = 260 nM[6]
KKHT-11018IC50 = 3380 nM[11]
KYS-05055IC50 = 350 nM[6]
KKHT-20718IC50 = 3720 nM[11]
KYS-05056IC50 = 380 nM[6]
KYS-05090IC50 = 41 nM[6]
KYS-05077IC50 = 4200 nM[9]
KYS-05057IC50 = 630 nM[6]
KKHT-10609IC50 = 9230 nM[11]
KYS-05064IC50 = 960 nM[12]
Ref 1J Bioenerg Biomembr. 2003 Dec;35(6):577-98.Modulation and pharmacology of low voltage-activated ("T-Type") calcium channels. To Reference
Ref 2Neuropharmacology. 2002 Feb;42(2):229-36.Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex. To Reference
Ref 3Life Sci. 1982 Oct 11;31(15):1575-85.Specific calcium antagonist binding sites in brain. To Reference
Ref 4Life Sci. 1988;43(6):477-84.Evidence for involvement of the astrocytic benzodiazepine receptor in the mechanism of action of convulsant and anticonvulsant drugs. To Reference
Ref 5Bioorg 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. To Reference
Ref 6Bioorg 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. To Reference
Ref 7Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6.Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. To Reference
Ref 8Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. Epub 2007 Sep 1.Discovery of potent T-type calcium channel blocker. To Reference
Ref 9Bioorg 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. To Reference
Ref 10Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers. To Reference
Ref 11Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives. To Reference
Ref 12Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.3D pharmacophore based virtual screening of T-type calcium channel blockers. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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