Target Validation Information
TTD ID	T39716
Target Name	Voltage-gated sodium channel alpha Nav1.5 (SCN5A)
Type of Target	Successful
Drug Potency against Target	Disopyramide	Drug Info	Ki = 2700 nM	[7]
	Mexiletine	Drug Info	IC50 = 130000 nM	[5]
	Quinine	Drug Info	Ki = 43 nM	[6]
		Drug Info	IC50 = 5500 nM	[1]
	1-[5-(4-Chlorophenyl)-2-furoyl]piperazine	Drug Info	IC50 = 4600 nM	[3]
	LOMERIZINE	Drug Info	IC50 = 26 nM	[1]
	LUBELUZOLE	Drug Info	IC50 = 280 nM	[1]
	N-(4-Methyl-benzoyl)-N'-phenethyl-guanidine	Drug Info	IC50 = 5650 nM	[2]
	N-Butyl-N'-(4-methyl-benzoyl)-guanidine	Drug Info	IC50 = 9000 nM	[2]
	NS-7	Drug Info	IC50 = 1000 nM	[1]
	PD-85639	Drug Info	IC50 = 46 nM	[1]
	SIPATRIGINE	Drug Info	IC50 = 5300 nM	[1]
Action against Disease Model	Procainamide	Drug Info	The uptake of [14C]pramipexole by rOCT1, rOCT2, and kidney slices was inhibited by procainamide and corticosterone, which are selective inhibitors of rOCT1 and rOCT2, respectively. The IC50 values of procainamide and corticosterone for the uptake of [14C]pramipexole by rOCT1, rOCT2, and kidney slices were 7.7, 167.0, and 47.0 microM and 163.7, 10.7, and 47.7 microM, respectively. These results demonstrate that both rOCT1 and rOCT2 are involved in the renal uptake of pramipexole across the basolateral membrane of the proximal tubular epithelial cells.	[4]
References
REF 1	Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37.
REF 2	Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3151-5.
REF 3	Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86.
REF 4	Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. Drug Metab Dispos. 2005 Apr;33(4):495-9.
REF 5	Analysis of human Nav1.8 expressed in SH-SY5Y neuroblastoma cells. Eur J Pharmacol. 2005 Dec 28;528(1-3):52-8.
REF 6	Development and validation of an in silico P450 profiler based on pharmacophore models. Curr Drug Discov Technol. 2006 Mar;3(1):1-48.
REF 7	Drug target identification using side-effect similarity. Science. 2008 Jul 11;321(5886):263-6.

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