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. 2017 Sep 8;6:e24502. doi: 10.7554/eLife.24502

Table 2. Activity of novel indole compounds against DYRK1A and related kinases relative to ID-8.

Compound R1 R2 R3 IC50 (μM)
DYRK1A DYRK1B DYRK2 CLK1 CLK4 GSK3α GSK3β LRRK2 PIM1 PIM3
ID-8 6-OH NO2 p-OCH3 0.104 0.040 NC 1.37 1.05 0.428 0.153 0.100 0.376 0.176
34 6-OCOCH3 NHCOCH3 p-OCH3 NC NC NC NC NC NC NC NC NC NC
28 6-OCH3 NO2 p-OCH3 0.346 0.695 NC NC 2.23 2.36 3.44 0.854 0.176 0.259
29 6-OCH2C6H5 NO2 p-OCH3 6.52 3.57 NC NC NC 18.0 14.3 8.16 18.5 8.28
30 6-OCOCH3 NO2 p-OCH3 0.680 0.299 NC NC 11.95 22.15 1.71 0.891 4.15 1.21
45 6-OH NO2 p-OH 0.122 0.060 2.30 0.364 0.163 0.375 0.233 0.046 0.243 0.180
48 6-OH NO2 m-OCH3 0.594 0.257 NC 13.0 4.77 2.32 0.692 2.17 0.654 0.593
49 6-OH NO2 o-OCH3 0.829 0.341 41.9 10.7 8.59 6.12 3.82 1.98 1.44 0.892
51 5-NO2 NO2 p-OCH3 NC NC NC NC NC NC NC NC 7.62 4.57
38 H NO2 p-OCH3 NC NC NC NC NC NC NC NC NC 20.74