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 534526 | J 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 534526 | J 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 526979 | J Med Chem. 2004 Mar 11;47(6):1303-14.Selective optimization of side activities: another way for drug discovery. | ||||
Ref 526184 | J 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 552213 | 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. | ||||
Ref 526184 | J 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 526184 | J 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 526184 | J 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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