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...
| Main Authors: | , , , , , , , |
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| Format: | Journal article |
| Sprog: | English |
| Udgivet: |
American Chemical Society
2018
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