期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 9, 页码 981-986出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00315
关键词
Chemokine receptor 4; MDC; TARC; CCR4; antagonist
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.
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