Target Validation Information
TTD ID T76914
Target Name Voltage-gated potassium channel Kv1.3 (KCNA3)
Type of Target
Clinical trial
Drug Potency against Target 1-Benzyl-7-chloro-4-hexyloxy-quinolinium Drug Info IC50 = 828 nM [6]
2-Methoxy-N-(3-methyl-2-phenyl-butyl)-benzamide Drug Info IC50 = 150 nM [2]
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one Drug Info IC50 = 740 nM [5]
5-(4-Phenylbutoxy)psoralen Drug Info IC50 = 724 nM [4]
Correloid Drug Info IC50 = 184 nM [3]
CP-339818 Drug Info IC50 = 230 nM [1]
UK-78282 Drug Info IC50 = 280 nM [1]
[1-Benzyl-1H-quinolin-(4E)-ylidene]-hexyl-amine Drug Info IC50 = 1053 nM [6]
References
REF 1 Angular methoxy-substituted furo- and pyranoquinolinones as blockers of the voltage-gated potassium channel Kv1.3. J Med Chem. 2001 Apr 12;44(8):1249-56.
REF 2 Benzamide derivatives as blockers of Kv1.3 ion channel. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4.
REF 3 Potent Kv1.3 inhibitors from correolide-modification of the C18 position. Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51.
REF 4 N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6983-8.
REF 5 Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92.
REF 6 Novel inhibitors of potassium ion channels on human T lymphocytes. J Med Chem. 1995 May 26;38(11):1877-83.

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