Towards the development of an in vivo chemical probe for cyclin G associated kinase (GAK)

SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and in mice, which limited its utility in in vivo...

Full description

Bibliographic Details
Main Authors: Asquith, C, Bennett, J, Su, L, Laitinen, T, Elkins, J, Pickett, J, Wells, C, Li, Z, Willson, T, Zuercher, W
Format: Journal article
Language:English
Published: MDPI 2019