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The SAR of UK-78,282: a novel blocker of human T cell Kv1. 3 potassium channels

…, MS Biggers, M Ramchandani, JH Smitrovich…

文献索引:Burgess, Laurence E.; Koch, Kevin; Cooper, Kelvin; Biggers, Michael S.; Ramchandani, Mukesh; Smitrovich, Jacqueline H.; Gilbert, Eric J.; Bruns, Matthew J.; Mather, Robert J.; Donovan, Carol B.; Hanson, Douglas C. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 8 p. 1047 - 1052

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被引用次数: 18

摘要

UK-78,282 was identified in a human T cell 86Rb efflux high-throughput screen of our compound libraries. This compound was found to be a potent and selective blocker of human T cell voltage-gated K+ channels and to inhibit T cell activation. The SAR around UK- 78,282 and a general pharmacophore hypothesis are presented in this communication.