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Results of the evaluation of inhibitory activity of compounds 2,3'-bis(1'H-indole) Heterocycles towards MDM2/MDMX as determined by FP.
| Ki (µM) | |||
|---|---|---|---|
| Compound | MDM2 | MDMX | |
| 2a | 17 | NA |  |
| 2c | 10 | NA | |
| 2d | >22 | NA | |
| 2e | 6.7 | 5.0 | |
| 2f | NA | NA | |
| 9a | 1.8 | 0.2 | |
| 9d | 0.7 | 1.5 | |
| 10d | NA | 6,09 | |
| WK23 (1) | 0.92 | 36 | |
NA: not active, Ki > 60 µM.
