Table 2. Biological Profile of Compounds 12 and 21.
assay details | Cpd 12 IC50 (μM)a | Cpd 21 IC50 (μM)a | |
---|---|---|---|
enzyme inhibition | ATM | 0.00029 | 0.0007 |
mTOR | 5.3 | 21 | |
DNAPK | 1.8 | 2.8 | |
PI3Kα | 2.2 | 3.8 | |
PI3Kβ | 8.1 | 10.3 | |
PI3Kγ | 2.9 | 3.0 | |
PI3Kδ | 0.80 | 0.73 | |
cellular inhibition | ATM | 0.0019 | 0.0028 |
ATR | >30 | >30 | |
PI3Kα | >30 | >30 | |
PI3Kβ/mTOR | >15 | >19 |
Geometric means of multiple IC50 determinations.