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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21.

Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.

Author information

1
Pfizer Global Research & Development, St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, United States. marvin.j.meyers@pfizer.com

Abstract

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.

PMID:
20137931
DOI:
10.1016/j.bmcl.2010.01.078
[Indexed for MEDLINE]

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