Table 2. IC50 Values for Inhibitors for CLK Family Membersa.
| TG003 | NR9 | 3A5 | 5E4 | 5F4 | |
|---|---|---|---|---|---|
| CLK1 (nM) | 49 | 390 | 51 | 277 | 273 |
| CLK2 (nM) | 353 | 553 | 68 | 174 | 127 |
| CLK3 (nM) | >3000 | >3000 | 346 | >3000 | >3000 |
| DYRK1A (nM) | 204 | 596 | 260 | 334 | 213 |
IC50 values were determined for the five inhibitors for CLK1, CLK2, CLK3, and DYRK1A. Literature values for TG003 according to Muraki et al.:21 CLK1, 20 nM; CLK2, 200 nM; CLK3, >10 μM; CLK4, 15 nM. Literature values for TG003 according to Fedorov et al.:14 CLK1, 48.6 nM; CLK3, >4 μM; Dyrk1A, 156.1 nM. Literature values for TG003 according to Mott et al.:26 CLK1, 19 nM; CLK2, 95 nM; CLK3, 3 μM; CLK4, 30 nM; Dyrk1A, 12 nM.