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 |
Potently active: IC50 value < 100 nM or < 10% control at 1 μM (Table S1). All IC50 values determined in duplicate.
Moderately active: IC50 value 200–500 nM or 10–49% control at 1 μM (Table S1). All IC50 values determined in duplicate.
Weakly active: IC50 value > 500 nM or > 49% control at 1 μM (Table S1). All IC50 values determined in duplicate.