Table 3.
The structures and corresponding IC50 values of compounds B1‐B14 toward the ATR and PARP1 a)
|
| |||
| Compd | Linker | IC50 (nM) | |
| ATR | PARP1 | ||
| B1 | — | 39.5 ± 3.7 | 420 ± 31 |
| B2 |
|
168 ± 7.8 | 16 ± 2.4 |
| B3 |
|
347 ± 15.7 | 9.5 ± 1.8 |
| B4 |
|
111 ± 8.1 | 6.2 ± 0.9 |
| B5 |
|
36.7 ± 4.6 | 1.2 ± 0.3 |
| B6 |
|
112 ± 5.3 | 0.46 ± 0.10 |
| B7 |
|
78.8 ± 6.2 | 0.76 ± 0.09 |
| B8 |
|
17.3 ± 2.5 | 0.38 ± 0.08 |
| B9 |
|
205 ± 13.1 | 0.64 ± 0.21 |
| B10 |
|
19 ± 1.2 | 0.61 ± 0.15 |
| B11 |
|
31.1 ± 4.7 | 1.0 ± 0.13 |
| B12 |
|
37 ± 4.2 | 2.0 ± 0.3 |
| B13 |
|
22 ± 1.7 | 1.3 ± 0.6 |
| B14 |
|
23 ± 2.1 | 1.2 ± 0.4 |
| 1 (Olaparib) | — | – | 1.3 |
| 8 (AZD6738) | — | 7.3 | — |
a)
Assays were performed in replicate (n = 3), IC50 values are shown as mean ± SD.