Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma
C. Asquith, K. Naegeli, M. P. East, T. Laitinen, T. M. Havener, C. I. Wells, G. L. Johnson, D. H. Drewry, W. J. Zuercher, D. C. Morris
Abstract
We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles.
02 /Specification & Classification
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