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. | ||||
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