Discovery of a benzo [e] pyrimido-[5, 4-b][1, 4] diazepin-6 (11H)-one as a potent and selective inhibitor of big MAP kinase 1

X Deng, Q Yang, N Kwiatkowski, T Sim…

文献索引：Deng, Xianming; Yang, Qingkai; Kwiatkowski, Nicholas; Sim, Taebo; McDermott, Ultan; Settleman, Jeffrey E.; Lee, Jiing-Dwan; Gray, Nathanael S. ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 3 p. 195 - 200

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被引用次数: 20

摘要

Kinome-wide selectivity profiling of a collection of 2-amino-pyrido [2, 3-d] pyrimidines followed by cellular structure− activity relationship-guided optimization resulted in the identification of moderately potent and selective inhibitors of BMK1/ERK5 exemplified by 11, 18, and 21. For example, 11 possesses a dissociation constant (K d) for BMK1 of 19 nM, a cellular IC50 for inhibiting epidermal growth factor induced BMK1 autophosphorylation of ...