Target Validation Information
TTD ID T39078
Target Name Calcium-activated potassium channel (KCN)
Type of Target
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]
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]
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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