Target Validation Information
TTD ID T49526
Target Name Voltage-gated potassium channel Kv7.1 (KCNQ1)
Type of Target
Successful
Drug Potency against Target Indapamide Drug Info IC50 = 100 nM/mL [4]
HMR-1556 Drug Info IC50 = 120 nM [2]
L-365260 Drug Info IC50 = 214 nM [3]
L-768673 Drug Info IC50 = 6 nM [3]
N-(2-Diethylamino-ethyl)-4-hexyloxy-benzamide Drug Info IC50 = 3500 nM [1]
N-(3,3-Dimethyl-butyl)-4-hexyloxy-benzamide Drug Info IC50 = 250 nM [1]
N-(3,3-Dimethyl-butyl)-4-indol-1-yl-benzamide Drug Info IC50 = 260 nM [1]
N-(3,3-Dimethyl-cyclopentyl)-4-hexyloxy-benzamide Drug Info IC50 = 360 nM [1]
References
REF 1 Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers. J Med Chem. 2001 Nov 8;44(23):3764-7.
REF 2 Selective optimization of side activities: another way for drug discovery. J Med Chem. 2004 Mar 11;47(6):1303-14.
REF 3 Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(... J Med Chem. 1997 Nov 21;40(24):3865-8.
REF 4 Concomitant 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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.