The GSK3� inhibitor AX9839  is both highly potent and selective (KiNativ�).  Due to a variety of molecular interactions detailed herein, AX9839  is a slow, tight-binding inhibitor of GSK3. The co-crystal structure also explains aspects of structure-activity relationships seen during the development of these inhibitors.

Co-crystal structures of GSK3� and the 4-quinolone inhibitor AX9839: Specific and potent binding facilitated by a fluorine H-bond acceptor, an arginine stacking interaction, and a water bridge

247th National Meeting (2014)

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