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

Abstract UK-78,282 was identified in a human T cell 86 Rb 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.