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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 that triggered the flip in binding mode. We report kinase selectivity and demonstrate that compounds of this series modulate ALK2 in cancer cells. These inhibitors are attractive starting points for the discovery of more advanced ALK2 inhibitors.

Original publication

DOI

10.1021/acs.jmedchem.8b00782

Type

Journal article

Journal

J Med Chem

Publication Date

23/08/2018

Volume

61

Pages

7261 - 7272