Table 1. Lipid Kinase Competition Assay for 22 Inositol Kinases Including Clinically Relevant Mutantsa.
| target | % control |
|---|---|
| PIK3C2B | 76 |
| PIK3C2G | 39 |
| PIK3CA | 99 |
| PIK3CA(C420R) | 100 |
| PIK3CA(E542K) | 98 |
| PIK3CA(E545A) | 82 |
| PIK3CA(E545K) | 81 |
| PIK3CA(H1047L) | 72 |
| PIK3CA(H1047Y) | 92 |
| PIK3CA(I800L) | 72 |
| PIK3CA(M1043I) | 98 |
| PIK3CA(Q546K) | 82 |
| PIK3CB | 46 |
| PIK3CD | 66 |
| PIK3CG | 54 |
| PIK4CB | 87 |
| PIKFYVE | 0 |
| PIP5K1A | 61 |
| PIP5K1C | 0 |
| PIP5K2B | 96 |
| PIP5K2C | 66 |
| VPS34 | 50 |
a
MOMIPP (10 μM ) was used for the competition. Data are shown as % control, where lower numbers indicate more competition between the control compound and MOMIPP. % control was calculated as follows. (MOMIPP signal – positive control signal)/(negative control signal – positive control signal) × 100. Negative control = DMSO (100% control); positive control = control compound that binds specifically to each kinase (0% control).