3区 · 医学
Article
作者: Roberts, Bryan ; Mete, Antonio ; Hemsley, Paul ; Johnson, Timothy ; Vaughan, Deborah ; Unitt, John ; Walters, Iain ; Kindon, Nicholas ; Teobald, Barry ; Baxter, Andrew ; Cheshire, David ; Steele, John ; Reuberson, James ; McGinnity, Dermot ; Andrews, Glen ; Stocks, Michael J. ; Liu, Yu-Zhen ; McHale, Mark
N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs.