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IC50 values of bisubstrate analogs (1-7).
| Compound | IC50 (μM) |
|---|---|
| Lys-CoA | 0.060 ± 0.008 |
| 1 | 2.6 ± 0.24 |
| 2 | 3.2 ± 0.4 |
| 3 | 2.4 ± 0.3 |
| 4 | 1.6 ± 0.2 |
| 5 | 1.2 ± 0.1 |
| 6 | 0.97 ± 0.1 |
| 7 | 0.4 ± 0.05 |
| Compound 7 | IC50 (μM) |
| wt p300 HAT | 0.4 ± 0.05 |
| D1625R; D1628R | 6.7 ± 0.8 |
| Lys-CoA | IC50 (μM) |
| wt p300 HAT | 0.060 ± 0.008 |
| D1625R; D1628R | 0.209 ± 0.015 |
