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. 2021 Aug 1;65(2):1313–1328. doi: 10.1021/acs.jmedchem.1c00440

Table 3. Combined Enzymatic Data.

compound potently activea moderately activeb weakly activec
15   MYLK2 = 479 nM DRAK2: 91%
8     MKNK2 = 2866 nM, DRAK2: 60%, YANK2 > 10000 nM
12   CSF1R = 233 nM  
16 TYK2 = 33 nM CSF1R = 305 nM JAK2: 62%
21   TBK1 = 128 nM, TRKA = 477 nM BMPR2 = 2918 nM, AURKB: 61%, JAK2: 107%
3 LRRK2 = 89 nM   DRAK2: 59%, NIM1 = 4398 nM, MYLK2 = 1119 nM
5   TBK1 = 149 nM IKKε = 1199 nM
11   TBK1 = 187 nM, TRKA = 153 nM JAK2: 87%, IKKε = 1314 nM, AURKB: 51%
17   DRAK1 = 325 nM, DRAK2 = 161 nM, AAK1 = 390 nM, SIK2 = 481 nM MKNK2 = 769 nM, TYK2 = 720 nM, JAK2 > 10000 nM, BMP2K: 56%
19 CSF1R = 91 nM TYK2 = 276 nM JAK2: 54%, ERBB2 > 10000 nM, TBK1 = 2737 nM
GSK8612 TBK1 = 37 nM LRRK2 = 159 nM, MAP2K5: 11%, CSF1R = 264 nM IKKε = 552 nM, DAPK3 > 10000 nM, NUAK2 = 1151 nM, ULK3 = 946 nM, MKNK2 = 1369 nM
20 AURKB: 5% NUAK1 = 176 nM, SIK2 = 185 nM BMP2K: 58%, DRAK1: 78%, DRAK2: 65%, JAK2: 81%, ACVR1 = 537 nM, BMPR1B = 9028 nM
4 LRRK2 = 19 nM, DRAK2 = 62 nM IKKε = 216 nM, DRAK1 = 202 nM, ULK3 = 343 nM, MKNK2 = 380 nM, TBK1 = 192 nM, MAP2K5: 12% ULK2 = 1742 nM, ULK1: 58%
13 AURKB: 6%, BMP2K = 40 nM, AAK1 = 74 nM, TYK2 = 48 nM, STK16 = 82 nM TBK1 = 192 nM, JAK2: 12%, BMPR2 = 488 nM, TRKA = 283 nM, NUAK1 = 317 nM NUAK2 = 900 nM, CSNK2A2 = 2269 nM, PIP5K1A > 10000 nM, MKNK2 = 1009 nM
6 TBK1 = 66 nM, JAK2: 3%, BMP2K = 38 nM, STK16 = 88 nM, TYK2 = 67 nM, AURKB: 7%, AAK1 = 80 nM CSF1R = 192 nM, TRKA = 158 nM, NUAK1 = 171 nM PRP4 > 10000 nM, PIP5K1A > 10000 nM, CSNK2A2 = 2304 nM, CSNK2A1 > 10000 nM, ULK3 = 1371 nM
a

Potently active: IC50 value < 100 nM or < 10% control at 1 μM (Table S1). All IC50 values determined in duplicate.

b

Moderately active: IC50 value 200–500 nM or 10–49% control at 1 μM (Table S1). All IC50 values determined in duplicate.

c

Weakly active: IC50 value > 500 nM or > 49% control at 1 μM (Table S1). All IC50 values determined in duplicate.