Table 4.
Biochemical and cellular activity of MU1210 and negative control MU140. The cellular Ki values were determined by NanoBRET assays in HEK293T cells.
| Kinase |
 MU1210 Activity [nM] |
 MU140 Activity [nM] (Negative Control) |
||
|---|---|---|---|---|
| Biochemical IC50 | Cellular Ki | Biochemical IC50 | Cellular Ki | |
| CLK1 | 8 | 84 | >3000 | >10,000 |
| CLK2 | 20 | 91 | >10,000 | >10,000 |
| CLK3 | >3000 | - | >3000 | - |
| CLK4 | 12 | 23 | >10,000 | >10,000 |
| DYRK1A | 213 | 6580 | >3000 | >10,000 |
| DYRK1B | 956 | >10,000 | >3000 | >10,000 |
| DYRK2 | 1309 | 1700 | >10,000 | >10,000 |
| HIPK1 | 187 | - | >10,000 | - |
| HIPK2 | 29 | >10,000 | >10,000 | - |
| HIPK3 | 159 | - | >3000 | - |
| HIPK4 | - | 5410 | - | - |