Novel Quinazolinone inhibitors of ALK2 flip between alternate binding modes: Structure-activity relationship, structural characterization, Kinase profiling, and cellular proof of concept

Structure-activity relationship and crystallographic data revealed that quinazolinone-containing fragments flip between two distinct modes of binding to activin receptor-like kinase-2 (ALK2). We explored both binding modes to discover potent inhibitors and characterized the chemical modifications th...

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Bibliographic Details
Main Authors: Hudson, L, Mui, J, Vázquez, S, Carvalho, D, Williams, E, Jones, C, Bullock, A, Hoelder, S
Format: Journal article
Language:English
Published: American Chemical Society 2018