Table 2.
SGC-CLK-1 binding, enzymatic and cellular target engagement characterization data.
| Kinase | % Control (1 μM)a | IC50 (nM)b | Cellular IC50 (nM)c |
|---|---|---|---|
| CLK1 | 8 | 13 | 154 ± 50 |
| CLK4 | 13 | 46 | 137 ± 100 |
| CLK2 | 16 | 4 | 58 ± 23 |
| ERK8 | 21 | nt | ntd |
| HIPK1 | 31 | 50 | >10,000 (n = 1) |
| HIPK2 | 34 | 42 | >10,000 (n = 1) |
| NEK7 | 40 | nt | ntd |
| PIP5K2B | 50 | nte | ntd |
| STK16 | 53 | 49 | 167f (n = 1) |
| CLK3 | 92 | 363 | ntd |
nt = not tested.
a
% Control data was generated at Eurofins DiscoverX at a concentration of 1 μM.
b
Enzymatic IC50 values were generated at Eurofins.
c
Cellular IC50 values were generated in a NanoBRET assay (n = 3).
d
NanoBRET assay not available.
e
No commercial enzyme assay available.
f
NanoBRET showed only partial inhibition (Supplemental Fig. S3).