- HETEROARYL COMPOUNDS AS KINASE INHIBITOR
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Provided herein are heteroaryl compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R 1, R 2, R 3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof.
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Page/Page column 89-90
(2019/10/04)
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- Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode
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The work described herein demonstrates the utility of structure-based drug design (SBDD) in shifting the binding mode of an HTS hit from a DFG-in to a DFG-out binding mode resulting in a class of novel potent CSF-1R kinase inhibitors suitable for lead development.
- Meyers, Marvin J.,Pelc, Matthew,Kamtekar, Satwik,Day, Jacqueline,Poda, Gennadiy I.,Hall, Molly K.,Michener, Marshall L.,Reitz, Beverly A.,Mathis, Karl J.,Pierce, Betsy S.,Parikh, Mihir D.,Mischke, Deborah A.,Long, Scott A.,Parlow, John J.,Anderson, David R.,Thorarensen, Atli
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scheme or table
p. 1543 - 1547
(2010/06/21)
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