Delving into the Latest Updates on SGC-GAK-1 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

GAK

Action

inhibitors

Mechanism

GAK inhibitors(cyclin G associated kinase inhibitors)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

The University of North Carolina at Chapel Hill

Active Organization-

Inactive Organization

The University of North Carolina at Chapel Hill

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Zuercher, William J. ; Knapp, Stefan ; Muller, Susanne ; Asquith, Christopher R. M. ; Earp, H. Shelton ; Wan, Jing ; East, Michael P. ; Berger, Benedict-Tilman ; Fedorov, Oleg ; Wells, Carrow I. ; Drewry, David H. ; Willson, Timothy M. ; Bennett, James M. ; Crona, Daniel J. ; Godoi, Paulo H. ; Hunter, Debra M. ; Elkins, Jonathan M. ; Capuzzi, Stephen J. ; Torrice, Chad D.

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). 11 was highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent RIPK2 inhibitor lacking GAK activity. Together, this chemical probe set can be used to interrogate GAK cellular biology.

100 Deals associated with SGC-GAK-1

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