Table 2.
The HMTs inhibitors derived based on virtual screening or high throughput screening.
| Targets | Virtual screen | High throughput screen | ||||
|---|---|---|---|---|---|---|
| Ia | IIb | IIIc | I | II | III | |
| PRMT1 | ★ | ★ | ||||
| PRMT3 | ★ | ★ | ||||
| PRMT4 | ★ | ★ | ||||
| PRMT5 | ★ | ★ | ||||
| PRMT6 | ★ | ★ | ||||
| DOT1L | ★ | ★ | ||||
| SUV420H1 | – | – | – | ★ | ||
| SUV420H2 | – | – | – | ★ | ||
| SMYD2 | – | – | – | ★ | ||
| SMYD3 | ★ | ★ | ||||
| GLP | – | – | – | ★ | ||
| G9a | ★ | ★ | ||||
| NSD2 | ★ | – | – | – | ||
| SETD2 | – | – | – | ★ | ||
| SETD7 | ★ | ★ | ||||
| SETD8 | ★ | ★ | ||||
| EZH1 | – | – | – | ★ | ||
| EZH2 | ★ | ★ | ||||
a
The IC50 values smaller than 1 μM.
b
The IC50 values at the range of 1–10 μM.
c
The IC50 values at the range of 10–100 μM.
The stars here denote that the IC50 value of the most potent compound against this target is in the corresponding range.