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. 2021 Aug 3;64(15):11709–11728. doi: 10.1021/acs.jmedchem.1c01115

Table 9. Selectivity Profiles of Lead Compoundsa.

compound DYRK1A DYRK1B DYRK2 CLK1 CLK2 CLK3 CDK2 GSK3β S score (35)
11 0.4 2.7 19 7.1 9.4 54 100 94 0.027
12 34 43 100 79 95 96 100 91 0.013
22 0.7 8.3 11 33 13 54 100 75 0.042
24 33 81 66 71 61 100 100 92 0.004
28 2.4 7.2 15 17 16 88 100 77 0.050
29 1.5 9.1 25 16 15 73 95 100 0.035
31 20 34 39 48 62 96 95 98 0.011
33 1.7 18 29 36 72 95 100 100 0.027
34 1.3 10 28 47 51 89 86 100 0.032
63 1.1 1.6 25 15 13 76 89 100 0.027
66 0.2 0.7 24 7.8 12 83 100 100 0.022
70 0.7 6.2 35 20 31 56 86 77 0.022
95 18 71 55 53 54 84 100 93 0.002
a

% Remaining activity as determined by DiscoverX KINOMEscan experiment. Inhibitor concentration = 1 μM.