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In Vitro Potencies of Newly Synthesized Inhibitors with Indazole N-1 Modifications
| |||
|---|---|---|---|
| Cmpd | Structure | IC50(nM) | |
| EZH2 | EZH1 | ||
| 5 |
|
<10 | 69 ± 14 |
| 51 |
|
<10 | 127 ± 29 |
| 52 |
|
<10 | 126 ± 22 |
| 53 |
|
<10 | 108 ±23 |
| 54 |
|
<10 | 315 ± 19 |
| 55 |
|
190 ± 33 | >2500 |
| 56 |
|
117 ± 17 | >2500 |
| 57 |
|
57 ±3 | >2500 |
| 58 |
|
149 ± 34 | >2500 |
| 59 |
|
697 ± 42 | >2500 |
| 60 |
|
280 ± 64 | >5000 |
| 61 |
|
1111 ± 35 | >5000 |
| 62 |
|
>1250 | >2500 |
| 63 |
|
25 ± 5 | 394 ± 55 |
