Target Validation Information
TTD ID	T39078
Target Name	Calcium-activated potassium channel (KCN)
Type of Target	Successful
Drug Potency against Target	Charybdotoxin	Drug Info	IC50 = 30 nM	[7]
	Chlorzoxazone	Drug Info	EC50 = 30000 nM	[3]
	Halofantrine	Drug Info	IC50 = 2.98 nM	[4]
	Quinine	Drug Info	IC50 = 100000 nM	[7]
	AVE0118	Drug Info	IC50 = 1100 nM	[6]
	(2-fluorophenyl)-(4-fluorophenyl)phenylacetamide	Drug Info	IC50 = 9 nM	[1]
	1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole	Drug Info	IC50 = 20 nM	[2]
	2,2,2-tris-(3-fluorophenyl)-acetamide	Drug Info	IC50 = 13 nM	[1]
	2,2,2-tris-(4-fluorophenyl)-acetamide	Drug Info	IC50 = 14 nM	[1]
	2,2-bis-(2-fluorophenyl)-2-phenylacetamide	Drug Info	IC50 = 30 nM	[1]
	2,2-bis-(3-fluorophenyl)-2-phenylacetamide	Drug Info	IC50 = 30 nM	[1]
	2-(2,4-difluorophenyl)-2,2-diphenylacetamide	Drug Info	IC50 = 34 nM	[1]
	2-(2-chlorophenyl)-2,2-diphenylethanamide	Drug Info	IC50 = 20 nM	[1]
	2-(3,4-Difluorophenyl)-2,2-diphenylacetamide	Drug Info	IC50 = 14 nM	[1]
	2-fluorophenyl-2,2-diphenylacetamide	Drug Info	IC50 = 15 nM	[1]
	2-trityl-4,5-dihydrooxazole	Drug Info	IC50 = 4300 nM	[1]
	4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one	Drug Info	IC50 = 10000 nM	[2]
	4-fluorophenyl-2,2-diphenylacetamide	Drug Info	IC50 = 40 nM	[1]
	5-tosyl-5H-dibenzo[b,d]azepin-7(6H)-one	Drug Info	IC50 = 2100 nM	[2]
	Bis(4-fluorophenyl)-2-fluorophenylacetamide	Drug Info	IC50 = 10 nM	[1]
	ICA-17043	Drug Info	IC50 = 12 nM	[1]
	N,N-dimethyl-2,2,2-triphenylacetamide	Drug Info	IC50 = 3150 nM	[1]
	N-ethyl-2,2,2-triphenylacetamide	Drug Info	IC50 = 1750 nM	[1]
	N-methyl-2,2,2-triphenylacetamide	Drug Info	IC50 = 550 nM	[1]
	Triphenylacetic acid methyl ester	Drug Info	IC50 = 330 nM	[1]
	TRIPHENYLMETHANAMINE	Drug Info	IC50 = 70 nM	[1]
Action against Disease Model	Halofantrine	Drug Info	The drug resistance profiles of Plasmodi uM falcipar uM isolated from four regions in Kenya were analyzed for drug resistance profiles. We observed variability in resistance to a broad range of antimalarial drugs across Kenya as determined from in vitro drug susceptibility screening and genotyping analysis.IC50 for Plasmodi uM falcipar uM isolates from Kericho, Kenya: 0.2 ng/mL	[5]
References
REF 1	Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. J Med Chem. 2008 Feb 28;51(4):976-82.
REF 2	Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304.
REF 3	Stimulatory effects of chlorzoxazone, a centrally acting muscle relaxant, on large conductance calcium-activated potassium channels in pituitary GH3 cells. Brain Res. 2003 Jan 3;959(1):86-97.
REF 4	In vitro activity of halofantrine and its relationship to other standard antimalarial drugs against African isolates and clones of Plasmodium falciparum. Am J Trop Med Hyg. 1992 Oct;47(4):521-7.
REF 5	Drug susceptibility and genetic evaluation of Plasmodium falciparum isolates obtained in four distinct geographical regions of Kenya. Antimicrob Agents Chemother. 2004 Sep;48(9):3598-601.
REF 6	Kv1.5 blockers for the treatment of atrial fibrillation: approaches to optimization of potency and selectivity and translation to in vivo pharmacology. Curr Top Med Chem. 2009;9(5):436-51.
REF 7	A charybdotoxin-sensitive, Ca(2+)-activated K+ channel with inward rectifying properties in brain microvascular endothelial cells: properties and activation by endothelins. J Neurochem. 1995 Sep;65(3):1274-81.

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