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. 2015 Dec 23;55(3):608–617. doi: 10.1021/acs.biochem.5b01128

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
a

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.