Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure–Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept

[Image: see text] 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 chemica...

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Bibliographic Details
Published in:J Med Chem
Main Authors: Hudson, Liam, Mui, James, Vázquez, Santiago, Carvalho, Diana M., Williams, Eleanor, Jones, Chris, Bullock, Alex N., Hoelder, Swen
Format: Artigo
Language:Inglês
Published: American Chemical Society 2018
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6109843/
https://ncbi.nlm.nih.gov/pubmed/30085668
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00782
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