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PCAF Brd‐binding affinity of compounds 39–45 measured by ITC.
| Compound | R | Configuration | K D (nm) (ITC) |
|---|---|---|---|
| 39 | F | (1S*, 2S*) | 195±23 |
| 40 | CO2Me | (1S*, 2S*) | 133±15 |
| 41 | Me | (1S*, 2S*) | 160±54 |
| 42 | Cl | (1S*, 2S*) | 223±78 |
| 43 | CF3 | (1S*, 2S*) | 163±117 |
| 44 | OMe | (1S*, 2S*) | 179±48 |
| 45 | H | (1S*, 2S*) | 168±27 |
| L ‐45/L‐Moses | H | (1S, 2S) | 126±15 |
| D ‐45 | H | (1R, 2R) | Inactive |
