PT  - JOURNAL ARTICLE
AU  - Christopher R. M. Asquith
AU  - Benedict-Tilman Berger
AU  - Jing Wan
AU  - James M. Bennett
AU  - Michael P. East
AU  - Jonathan M. Elkins
AU  - Oleg Fedorov
AU  - Paulo H. Godoi
AU  - Debra M. Hunter
AU  - Stefan Knapp
AU  - Susanne Müller
AU  - Carrow I. Wells
AU  - H. Shelton Earp
AU  - Timothy M. Willson
AU  - William J. Zuercher
TI  - SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)
AID  - 10.1101/376772
DP  - 2018 Jan 01
TA  - bioRxiv
PG  - 376772
4099  - http://biorxiv.org/content/early/2018/07/25/376772.1.short
4100  - http://biorxiv.org/content/early/2018/07/25/376772.1.full
AB  - We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G associated kinase (GAK), together with a structurally-related negative control SGC-GAK-1N (14). SGC-GAK-1 is highly selective in a kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent inhibitor of RIPK2 lacking GAK activity. Together, the chemical probe set of 11, 14, and 18 can be used to interrogate the cellular biology of GAK inhibition.