化学
激酶
EPH受体A2
立体化学
结构-活动关系
生物化学
组合化学
体外
受体酪氨酸激酶
作者
Joshua Gerninghaus,Rezart Zhubi,Andreas Krämer,Marwah Karim,Tran Do Hoang Nhu,Andreas C. Joerger,Christian Schreiber,Lena M. Berger,Benedict‐Tilman Berger,Theresa A. L. Ehret,Lewis Elson,Christopher Lenz,Krishna Saxena,Susanne Müller,Shirit Einav,Stefan Knapp,Thomas Hanke
标识
DOI：10.1021/acs.jmedchem.4c00411
摘要
Macrocyclization of acyclic compounds is a powerful strategy for improving inhibitor potency and selectivity. Here we have optimized 2-aminopyrimidine-based macrocycles to use these compounds as chemical tools for the ephrin kinase family. Starting with a promiscuous macrocyclic inhibitor,
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