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Binding Affinities and HMT Inhibition Activities of Selected Compounds
| compound | binding affinity to WDR5 | HMT inhibition |
|---|---|---|
| IC50 ± SD (nM) | IC50 ± SD (μM) | |
| 2d | >300 (μM) | >400 |
| 1a | 77.4 ± 13.2 (μM) | >400 |
| 1h | 3.1 ± 0.3 (μM) | >400 |
| ARA | 540 ± 30 | 141 ± 52 |
| 1c | 240 ± 30 | 12.1 ± 0.6 |
| 6g | 80 ± 14 | 2.8 ± 1.6 |
| 3b | 30 ± 8 | 1.8 ± 0.2 |
| 6b | 36 ± 5 | 5.2 ± 1.8 |
| 6a | 5 ± 1 | 0.5 ± 0.1 |
| 6c | 6 ± 0.4 | 0.9 ± 0.1 |
| 6f | 9 ± 1 | 0.7 ± 0.3 |
| MM-102 | 2.4 ± 1.7 | 0.4 ± 0.1 |
