High quality chemical probes are highly valuable reagents to explore biology of their target proteins. The most useful chemical probes meet five criteria:
- The chemical probe is a potent inhibitor of its primary target, ideally with an in vitro potency in biochemical assays < 100 nM.
- The chemical probe demonstrates selectivity over other proteins, with at least a 30-fold window over closely related targets in the same protein family.
- The chemical probe shows activity in cellular assays at or below a concentration of 1 µM.
- A close analog of the chemical probe that lacks activity on the primary target is available as a negative control compound.
- The chemical probe is publicly available without restrictions on its use.
SGC-UNC has generated high quality chemical probes for several dark kinases.
SGC-AAK1-1 for adaptor protein 2-associated kinase (AAK1) and BMP-2 inducible kinase (BMP2K/BIKE)
SGC-GAK-1 for Cyclin G-associated Kinase (GAK)
We have also collaborated with SGC scientists in Frankfurt, Campinas, and Oxford to release chemical probes for several additional kinases.