Target Validation Information
Target ID T49526
Target Name Potassium voltage-gated channel subfamily KQT member 1
Target Type
Successful
Drug Potency against Target L-768673 Drug Info IC50 = 6 nM [534526]
L-365260 Drug Info IC50 = 214 nM [534526]
HMR-1556 Drug Info IC50 = 120 nM [526979]
N-(3,3-Dimethyl-butyl)-4-hexyloxy-benzamide Drug Info IC50 = 250 nM [526184]
Indapamide Drug Info IC50 = 100 nM/mL [552213]
N-(3,3-Dimethyl-butyl)-4-indol-1-yl-benzamide Drug Info IC50 = 260 nM [526184]
N-(2-Diethylamino-ethyl)-4-hexyloxy-benzamide Drug Info IC50 = 3500 nM [526184]
N-(3,3-Dimethyl-cyclopentyl)-4-hexyloxy-benzamide Drug Info IC50 = 360 nM [526184]
References
Ref 534526J Med Chem. 1997 Nov 21;40(24):3865-8.Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Ref 534526J Med Chem. 1997 Nov 21;40(24):3865-8.Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Ref 526979J Med Chem. 2004 Mar 11;47(6):1303-14.Selective optimization of side activities: another way for drug discovery.
Ref 526184J Med Chem. 2001 Nov 8;44(23):3764-7.Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.
Ref 552213Concomitant Block of the Rapid (I(Kr)) and Slow (I(Ks)) Components of the Delayed Rectifier Potassium Current is Associated With Additional Drug Effects on Lengthening of Cardiac Repolarization. J Cardiovasc Pharmacol Ther. 1999 Jul;4(3):143-150.
Ref 526184J Med Chem. 2001 Nov 8;44(23):3764-7.Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.
Ref 526184J Med Chem. 2001 Nov 8;44(23):3764-7.Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.
Ref 526184J Med Chem. 2001 Nov 8;44(23):3764-7.Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.

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