Table 3.
Structure-activity of the N-(1H-indol-6-yl)acetamide series of 3-cyanopyrazolo[1,5-a]pyrimidines 16–33.
| ||||
|---|---|---|---|---|
| Compound | R2 | CSNK2A1 nanoBRET (pIC50)a | CSNK2A2 nanoBRET (pIC50)a | MHV replication (pIC50)b |
| 16 |
|
8.0 | 8.4 | 7.4 |
| 17 |
|
7.9 | 8.0 | 6.3 |
| 18 |
|
7.4 | 7.0 | 6.0 |
| 19 |
|
6.8 | 7.1 | 5.2 |
| 20 |
|
6.3 | 5.8 | i.a. |
| 21 |
|
i.a. | i.a. | i.a. |
| 22 |
|
5.1 | i.a. | i.a. |
| 23 |
|
7.4 | 7.6 | 5.8 |
| 24 |
|
7.0 | 6.7 | 5.4 |
| 25 |
|
7.5 | 6.6 | 6.2 |
| 26 |
|
7.0 | 5.7 | 6.0 |
| 27 |
|
6.4 | 6.7 | 5.5 |
| 28 |
|
7.2 | 6.4 | 5.4 |
| 29 |
|
6.8 | 6.7 | 5.5 |
| 30 |
|
6.9 | 7.1 | 5.5 |
| 31 |
|
5.4 | 5.9 | i.a. |
| 32 |
|
i.a. | i.a. | i.a. |
| 33 |
|
5.2 | 5.2 | 5.5 |
a
In cell target engagement of CSNK2A2-nLuc in HEK293 cells.
b
Inhibition of MHV-nLuc replication in DBT cells. All values are the mean of three assays with range ± 15%. i.a. inactive.