Table 1. IC50 Values for Inhibition of Enzyme Activity by Test 2-Arylquinazolin-4-ones.
compd | TNKS-1 IC50 (nM) | TNKS-2 IC50 (nM) | PARP-1 IC50 (nM) | IMPDH2 IC50 (μM) |
---|---|---|---|---|
1 | 17 | 9.6 | 1200 | >10 |
7a | 42 | 41 | 795 | >10 |
7b | 35 | 6.7 | 685 | >10 |
7c | 48 | 10 | >5000a | >10 |
7d | 32 | 30 | 104 | >10 |
7e | 37 | 12 | 891 | >10 |
7f | 36 | 33 | >5000a | >10 |
7g | 32 | 5.5 | >5000a | >10 |
7h | 44 | 40 | >5000a | >10 |
7j | 35 | 3.3 | 504 | >10 |
7k | 52 | 5.5 | 1200 | >10 |
10 | 73 | 44 | >5000a | >10 |
11 | NDb | ∼100 | NDb | NDb |
Limited by solubility.
Not determined.