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Analysis of covalent complex formation of menin inhibitors with recombinant human menin protein by mass spectrometry.
| Compound | Incubation time with menin protein | |||
|---|---|---|---|---|
|
| ||||
| 10 minutes | 30 minutes | 1 hr | overnight | |
|
| ||||
| % of menin covalent complex | ||||
|
| ||||
| 19 | 36.9% | 83.4% | 85.4% | 90.9% |
| 20 | 24.1% | 40.9% | 59.4% | 81.5% |
| 21 | 0% | 0% | 0% | 27.0% |
| 22 | 8.8% | 27.9% | 37.4% | 93.1% |
| 23 | 9.8% | 22.6% | 40.5% | 90.0% |
| 24 (M-1121) | 27% | 59% | 66% | 100% |
| 25 | 0% | 0% | 0% | 45.1% |
| 26 | 0% | 0% | 0% | 0% |
