- Discovery of INCB3284, a Potent, Selective, and Orally Bioavailablle hCCR2 Antagonist
[作者:XUE CHUBIAO; FENG HAO; CAO GANFENG; HUANG TAISHENG; GLENN JOSEPH; ANAND RAJAN; MELONI DAVID; ZHANG KE; KONG LINGQUAN; WANG ANLAI; ZHANG YINGXIN; ZHENG CHANGSHENG; XIA MICHAEL; CHEN LIHUA; TANAKA HIROYUKI; HAN QI; ROBINSON D J; MODI DILIP; STORACE LOU; SHAO LIXIN; SHARIEF VAQAR; LI MEI; GALYA LAURINE G; COVINGTON MARYANNE; SCHERLE PEGGY; DIAMOND SHARON; EMM TOM; YELESWARAM SWAMY; CONTEL NANCY; VADDI KRIS; NEWTON ROBERT; HOLLIS GREG; FRIEDMAN STEVEN; METCALF BRIAN,期刊:ACS Medicinal Chemistry Letters, 页码:450-454 , 文章类型: Article,,卷期:2011年2-6]
- We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in ant...
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