血小板生成素（Tpo）受体的苯并[a]咔唑基小分子激动剂的发现与生物学评价。
Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.
作者信息
Alper Phil B, Marsilje Thomas H, Mutnick Daniel, Lu Wenshuo, Chatterjee Arnab, Roberts Michael J, He Yun, Karanewsky Donald S, Chow Donald, Lao Jianmin, Gerken Andrea, Tuntland Tove, Liu Bo, Chang Jonathan, Gordon Perry, Seidel H Martin, Tian Shin-Shay
机构信息
Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5255-8. doi: 10.1016/j.bmcl.2008.08.068. Epub 2008 Aug 22.
A novel series of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. Starting from a 3.4 microM high throughput screen hit, members of this series have been identified which are full agonists with functional potency <50 nM and oral bioavailability in mice.
报道了一系列基于苯并[a]咔唑的新型血小板生成素（Tpo）受体小分子激动剂。从一个3.4微摩尔的高通量筛选命中物开始，已鉴定出该系列的成员，它们是功能效力<50纳摩尔且在小鼠中有口服生物利用度的完全激动剂。
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