Table 5. Nek2 SAR for a series of published PERK inhibitors.
| ||||||||||||
| Compound | R 1 | # kinases ≥90% Inh | NEK1 | NEK2 | NEK3 | NEK4 | NEK5 | NEK6 | NEK7 | NEK9 | NEK10 | NEK11 |
| % Inh (1 μM) | ||||||||||||
| UNC5254 |
|
15 | 89 | 97 | 0 | 29 | 34 | 0 | 0 | 0 | 0 | 58 |
| UNC5490 |
|
16 | 31 | 96.9 | 7 | 11 | 45 | 19 | 0 | 20 | 0 | 59 |
| UNC5071 |
|
11 | 7 | 84 | 0 | 32 | 8 | 18 | 0 | 8 | 10 | 38 |
| UNC5172 |
|
86 | 0 | 79 | 0 | 5 | 7 | 3 | 17 | 33 | 0 | 0 |
| UNC4987 |
|
15 | 21 | 74 | 4 | 44 | 24 | 18 | 11 | 25 | 7 | 49 |
| UNC5297 |
|
14 | 31 | 73 | 11 | 22 | 28 | 0 | 0 | 0 | 22 | 8 |
| UNC5039 |
|
17 | 26 | 66 | 1 | 22 | 32 | 11 | 0 | 18 | 18 | 0 |
| UNC5478 |
|
13 | 9 | 18 | 0 | 13 | 0 | 6 | 0 | 25 | 6 | 8 |
| UNC5165 |
|
5 | 0 | 15 | 0 | 7 | 0 | 0 | 11 | 8 | 18 | 14 |