Table 3. Residence Time of Small Molecules Compound 1, Compound 2, and Compound 3 for GSK3α and GSK3βa.
Kobserved(normalized to DMSO) | ||
---|---|---|
compound | GSK3α | GSK3β |
compound 1 | 1 | 0.91 |
compound 2 | 0.54 | 0.91 |
compound 3 | 0.46 | 0.87 |
The novel compound 2 and compound 3 demonstrate longer residence times specially at the GSK3α paralog when compared to previously profiled compounds.