Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameVoltage-gated sodium channel subunit alpha Nav1.3    
Type of TargetResearch target    
Drug Potency against Target4-Biphenyl-4-yl-2-(1-propyl-butyl)-1H-imidazoleIC50 = 100 nM[1]
5-Hexyl-5-phenyl-imidazolidine-2,4-dioneIC50 = 13000 nM[2]
4-Biphenyl-4-yl-2-methyl-1H-imidazoleIC50 = 1460 nM[1]
4-Biphenyl-4-yl-2-hexyl-1H-imidazoleIC50 = 16 nM[1]
SIPATRIGINEIC50 = 17850 nM[3]
2-Hexyl-4-(4-isobutyl-phenyl)-1H-imidazoleIC50 = 28 nM[1]
LUBELUZOLEIC50 = 2939 nM[3]
U-92032IC50 = 360 nM[4]
LIFARIZINEIC50 = 494 nM[3]
5-Nonyl-5-phenyl-imidazolidine-2,4-dioneIC50 = 5000 nM[2]
5-Heptyl-5-phenyl-imidazolidine-2,4-dioneIC50 = 5000 nM[2]
4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazoleIC50 = 70 nM[1]
4-Biphenyl-4-yl-2-(1-pentyl-hexyl)-1H-imidazoleIC50 = 8 nM[1]
2-(1-Pentyl-hexyl)-4-phenyl-1H-imidazoleIC50 = 86 nM[1]
2-Hydroxy-2-phenyl-nonanoic acid amideIC50 = 9000 nM[2]
L-741742Ki = 1900 nM[6]
PD-85639Ki = 260 nM[7]
Ref 1Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. To Reference
Ref 2J Med Chem. 1999 May 6;42(9):1537-45.Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. To Reference
Ref 3J Med Chem. 2002 Aug 15;45(17):3755-64.Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. To Reference
Ref 4J Med Chem. 2000 Sep 7;43(18):3372-6.Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity. To Reference
Ref 5J Biol Chem. 2007 Oct 19;282(42):30699-706. Epub 2007 Aug 27.Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels. To Reference
Ref 6J Med Chem. 1999 Jul 15;42(14):2706-15.1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. To Reference
Ref 7J Med Chem. 1994 Jan 21;37(2):268-74.Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. To Reference


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