2. Academic Validation
  3. Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5255-8. doi: 10.1016/j.bmcl.2008.08.068.
Phil B Alper 1,  Thomas H Marsilje,  Daniel Mutnick,  Wenshuo Lu,  Arnab Chatterjee,  Michael J Roberts,  Yun He,  Donald S Karanewsky,  Donald Chow,  Jianmin Lao,  Andrea Gerken,  Tove Tuntland,  Bo Liu,  Jonathan Chang,  Perry Gordon,  H Martin Seidel,  Shin-Shay Tian
Affiliations

Affiliation

  • 1 Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
PMID: 18778936 DOI: 10.1016/j.bmcl.2008.08.068
Abstract

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.

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