Table 5. Compound 15 Selectivity vs Protein Kinases, Lipid Kinases, and a Cerep Safety Panel.
panel screened | results |
---|---|
140 protein kinases | Compound screened at 10 μM. Two hits with <50% residual activity: AURKB (31%), CLK2 (37%) |
23 lipid kinases | 2 hits: PI5P4Kγ KD = 7.1 nM, PIP5K1C KD = 230 nM |
Cerep safety panel (24 cellular and nuclear receptors, 10 enzymes and uptake receptors, 6 ion channels) | Compound screened at 10 μM. One hit >50% inhibition compared with control: dopamine uptake (59%) |