Target Validation Information
TTD ID	T17569
Target Name	Voltage-gated potassium channel Kv1.5 (KCNA5)
Type of Target	Successful
Drug Potency against Target	Azimilide	Drug Info	IC50 = 30 nM	[7]
	Dalfampridine	Drug Info	IC50 = 160 nM	[5]
	Dronedarone	Drug Info	IC50 = 10 nM	[8]
	2-amino-2-phenyl-1,1-di(pyridin-3-yl)ethanol	Drug Info	IC50 = 16390 nM	[3]
	2-morpholino-1,1,2-triphenylethanol	Drug Info	IC50 = 204 nM	[3]
	2-morpholino-1,1-di(pyridin-3-yl)hexan-1-ol	Drug Info	IC50 = 2869 nM	[3]
	2-morpholino-1,1-di(pyridin-3-yl)octan-1-ol	Drug Info	IC50 = 3357 nM	[3]
	2-morpholino-2-phenyl-1,1-di(pyridin-3-yl)ethanol	Drug Info	IC50 = 256 nM	[3]
	2-phenyl-1,1-di(pyridin-3-yl)ethanol	Drug Info	IC50 = 7107 nM	[3]
	3-(4-methoxybenzyloxy)-2-phenylthiazolidin-4-one	Drug Info	IC50 = 924 nM	[2]
	3-(benzyloxy)-2-(4-chlorophenyl)thiazolidin-4-one	Drug Info	IC50 = 997 nM	[2]
	3-methyl-2-morpholino-1,1-diphenylbutan-1-ol	Drug Info	IC50 = 3242 nM	[3]
	4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one	Drug Info	IC50 = 3450 nM	[4]
	N-Benzyl-2-(toluene-4-sulfonylamino)-benzamide	Drug Info	IC50 = 4100 nM	[1]
	N-Phenethyl-2-(toluene-4-sulfonylamino)-benzamide	Drug Info	IC50 = 6700 nM	[1]
Action against Disease Model	Dronedarone	Drug Info	WT I(HERG) tails, measured at -40 mV following activating pulses to +30 mV, were blocked with IC(50) values of approximately 59 nM of dronedarone (DRONED). I(HERG) inhibition byDRONED was contingent upon channel gating, with block developing rapidly on membrane depolarization, but with no preference for activated over inactivated channels. High external [K(+)] (94 mM) reduced the potency of I(HERG) inhibition by both DRONED	[6]
References
REF 1	Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2823-7.
REF 2	Evolution of thiazolidine-based blockers of human Kv1.5 for the treatment of atrial arrhythmias. Bioorg Med Chem Lett. 2007 Jan 1;17(1):282-4.
REF 3	Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6.
REF 4	Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92.
REF 5	Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity. Curr Top Med Chem. 2003;3(14):1663-82.
REF 6	High affinity HERG K(+) channel blockade by the antiarrhythmic agent dronedarone: resistance to mutations of the S6 residues Y652 and F656. Biochem Biophys Res Commun. 2004 Dec 17;325(3):883-91.
REF 7	N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. Curr Top Med Chem. 2006;6(8):749-70.
REF 8	Dronedarone: a novel antiarrhythmic agent for the treatment of atrial fibrillation. Curr Opin Cardiol. 2010 Jan;25(1):53-8.

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