The Discovery of Tricyclic Pyridone Jak2 Inhibitors. Part 1: Hit to Lead

Tony Siu,Ekaterina S. Kozina,Joon Jung,Craig Rosenstein,Anjili Mathur,Michael D. Altman,Grace Chan,Lin Xu,Eric Bachman,Jan-Rung Mo,Melaney Bouthillette,Thomas Rush,Christopher J. Dinsmore,C. Gary Marshall,Jonathan R. Young

Bioorganic & medicinal chemistry letters（2010）

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摘要

This paper describes the discovery and design of a novel class of JAK2 inhibitors. Furthermore, we detail the optimization of a screening hit using ligand binding efficiency and logD. These efforts led to the identification of compound 41, which demonstrates in vivo activity in our study.

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关键词

JAK2,Kinase,Ligand binding efficiency,Structure based design

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