Target Validation Information
TTD ID	T76937
Target Name	Voltage-gated sodium channel alpha Nav1.3 (SCN3A)
Type of Target	Successful
Drug Potency against Target	2-(1-Pentyl-hexyl)-4-phenyl-1H-imidazole	Drug Info	IC50 = 86 nM	[5]
	2-Hexyl-4-(4-isobutyl-phenyl)-1H-imidazole	Drug Info	IC50 = 28 nM	[5]
	2-Hydroxy-2-phenyl-nonanoic acid amide	Drug Info	IC50 = 9000 nM	[1]
	4-Biphenyl-4-yl-2-(1-pentyl-hexyl)-1H-imidazole	Drug Info	IC50 = 8 nM	[5]
	4-Biphenyl-4-yl-2-(1-propyl-butyl)-1H-imidazole	Drug Info	IC50 = 100 nM	[5]
	4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazole	Drug Info	IC50 = 70 nM	[5]
	4-Biphenyl-4-yl-2-hexyl-1H-imidazole	Drug Info	IC50 = 16 nM	[5]
	4-Biphenyl-4-yl-2-methyl-1H-imidazole	Drug Info	IC50 = 1460 nM	[5]
	5-Heptyl-5-phenyl-imidazolidine-2,4-dione	Drug Info	IC50 = 5000 nM	[1]
	5-Hexyl-5-phenyl-imidazolidine-2,4-dione	Drug Info	IC50 = 13000 nM	[1]
	5-Nonyl-5-phenyl-imidazolidine-2,4-dione	Drug Info	IC50 = 5000 nM	[1]
	CCNCSSKWCRDHSRCC	Drug Info	IC50 = 8000 nM	[6]
	L-741742	Drug Info	Ki = 1900 nM	[2]
	LIDOFLAZINE	Drug Info	Ki = 77 nM	[7]
	PD-85639	Drug Info	Ki = 260 nM	[7]
	SIPATRIGINE	Drug Info	IC50 = 17850 nM	[4]
	U-92032	Drug Info	IC50 = 360 nM	[3]
References
REF 1	Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. J Med Chem. 1999 May 6;42(9):1537-45.
REF 2	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) rece... J Med Chem. 1999 Jul 15;42(14):2706-15.
REF 3	Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a ... J Med Chem. 2000 Sep 7;43(18):3372-6.
REF 4	Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. J Med Chem. 2002 Aug 15;45(17):3755-64.
REF 5	2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.
REF 6	Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels. J Biol Chem. 2007 Oct 19;282(42):30699-706.
REF 7	Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. J Med Chem. 1994 Jan 21;37(2):268-74.

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