鉴定一种新型、选择性、非甾体、功能性糖皮质激素受体拮抗剂。
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
机构信息
Medicines Research Centre, Verona, Italy.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3. doi: 10.1016/j.bmcl.2010.01.133. Epub 2010 Feb 4.
PMID:20202837
Abstract
The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.
摘要
本文描述了一种新型、有效、非甾体/小分子功能 GR 拮抗剂 GSK1564023A 的鉴定，该拮抗剂对 PR 具有选择性。还描述了相关的构效关系和对初始高通量筛选命中化合物的优化过程。
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