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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