Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).

ID: ALA4665659

Journal: Bioorg Med Chem Lett

Title: Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).

Authors: Asquith CRM,Treiber DK,Zuercher WJ

Abstract: 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.

CiteXplore: 31129055

DOI: 10.1016/j.bmcl.2019.05.025

Patent ID: ┄