We demonstrate an innovative approach for optimization of kinase inhibitor potency and selectivity utilising kinase mini-panels and kinome-wide panels. We present a focused case study on development of a selective inhibitor of cyclin G associated kinase (GAK) using the quin(az)oline inhibitor chemotype. These results exemplify a versatile, efficient approach to drive kinome selectivity during inhibitor development programs.
Keywords: 4-Anilinoquinazoline; 4-anilinoquinoline; Cyclin G associated kinase (GAK); Kinome selectivity; Mini-kinome panel.
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