Table 2. Preliminary Biological Screening of Compounds Showing EC50 on ELISA Assay Ranging from 0.95 to 20 μM.
| compd | EC50 ELISA (μM) | preliminary biological screening |
|---|---|---|
| 4d | 16 ± 4 | HR inhibition = 10%, 40 μM |
| 12d | 16 ± 2 | HR inhibition = not present |
| olaparib association = not present | ||
| 18d | 13 ± 1 | olaparib association = not present |
| 20d | 20 ± 2 | olaparib association = not present |
| 21d | 20 ± 4 | NEa |
| 22d | 2 ± 0.5 | HR inhibition = not present |
| olaparib association = not present at 5 μM | ||
| 23d | 10 ± 2 | olaparib association = not present |
| 30d | 15 ± 3 | NEa |
| 31d | 17 ± 4 | HR inhibition = NDDb |
| olaparib association = present at 20 μM | ||
| 33d | 8 ± 2 | HR inhibition = not present |
| olaparib association = not present | ||
| 34d | 19 ± 1 | HR inhibition = not present |
| olaparib association = NEa | ||
| 35d | 19 ± 1 | HR inhibition = 54%, 20 μM |
| olaparib association = present at 15 μM | ||
| 36d | 10 ± 0.7 | HR inhibition = 24%, 10 μM |
| olaparib association = not present | ||
| 39d | 15 ± 4 | HR inhibition = NDDb |
| 45d | 18 ± 1 | HR inhibition = not present |
| 49d | 0.95 ± 0.05 | HR inhibition = not present |
| olaparib association = not present |
a
NE, not evaluable.
b
NDD, not dose-dependent.