Table 3.
AlphaScreen IC50 values for displacement of H3K4me3-Bn from His-KDM7(PHD) by AMI derivatives. Final concentrations of protein and H3K4me3-Bn were: 6.25 nM KDM7A(PHD) and 25 nM peptide, 12.5 nM each for KDM7B(PHD), and 25 nM KDM7C(PHD) and 6.25 nM peptide. Average ± StdDev (n ≥ 3 independent replicates) shown.
| Compounds | IC50 (µM) |
||
|---|---|---|---|
| KDM7A(PHD) | KDM7B(PHD) | KDM7C(PHD) | |
| AMI | 156 ± 12 | 252 ± 53 | 84 ± 14 |
| WAG-003 | 2232 ± 790 | 307 ± 76 | 976 ± 146 |
| WAG-005 | 50 ± 5 | 390 ± 158 | 740 ± 149 |
| 1a | 333 ± 39 | 397 ± 77 | 158 ± 30 |
| 2a | 86 ± 9 | 355 ± 39 | 579 ± 87 |
| 2b | 108 ± 15 | 310 ± 78 | 598 ± 119 |
| 2c | 104 ± 8 | 377 ± 76 | 501 ± 75 |
| 2d | 98 ± 10 | 697 ± 154 | 682 ± 97 |
| 7a | 102 ± 15 | 496 ± 181 | 1294 ± 280 |
| 7b | 326 ± 14 | 286 ± 84 | 533 ± 99 |
| 8a | 76 ± 14 | 240 ± 58 | 228 ± 66 |
| 8b | 68 ± 13 | 242 ± 41 | 220 ± 40 |
| 10 | 534 ± 150 | 386 ± 41 | 359 ± 89 |
| 12 | 151 ± 17 | 221 ± 57 | 334 ± 45 |
| H3(1–21)K4me3 | 1.9 ± 0.1 μM | 1.7 ± 0.2 μM | 2.7 ± 0.2 μM |