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

被引:22
作者
Burgess, LE
Koch, K
Cooper, K
Biggers, MS
Ramchandani, M
Smitrovich, JH
Gilbert, EJ
Bruns, MJ
Mather, RJ
Donovan, CB
Hanson, DC
机构
[1] PFIZER INC,DIV CENT RES,DEPT MED CHEM,GROTON,CT 06340
[2] PFIZER INC,DIV CENT RES,DEPT IMMUNOL,GROTON,CT 06340
关键词
D O I
10.1016/S0960-894X(97)00163-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
UK-78,282 was identified in a human T cell Rb-86 efflux high-throughput screen of our compound libraries. This compound was found to be a potent and selective blacker 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. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1047 / 1052
页数:6
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