Table 1.
Ki values and ligand efficiencies for 3-aminopyridin-2-one library against Aurora A, Aurora B and MPS1.
| Compd | MPS1 Ki µM (LE) | AurA Ki µM (LE) | AurB Ki µM (LE) |
|---|---|---|---|
| 1 | >1000 (-) | 361.0 (0.59) | 159.7 (0.64) |
| 2 | 94.7 (0.39) | 7.5 (0.53) | 3.2 (0.53) |
| 3 | 80.8 (0.40) | 393.9 (0.30) | 59.3 (0.41) |
| 4 | 236.4 (0.33) | 99.5 (0.36) | 102.7 (0.36) |
| 5 | 91.2 (0.37) | 184.7 (0.31) | 63.9 (0.38) |
| 6 | 30.2 (0.34) | 76.3 (0.31) | 41.7 (0.33) |
| 7 | 25.6 (0.39) | 21.3 (0.40) | 15.1 (0.41) |
| 8 | 11.0 (0.37) | 30.2 (0.34) | 12.0 (0.37) |
| 9 | 128.2 (0.38) | 66.9 (0.41) | 70.3 (0.40) |
| 10 | 269.3 (0.35) | 89.6 (0.39) | 18.7 (0.46) |
| 11 | 98.1 (0.39) | 125.2 (0.38) | 97.2 (0.39) |
| 12 | 367.3 (0.26) | >100 (-) | 12.9 (0.37) |
| 13 | >100 (-) | >100 (-) | >100 (-) |
| 14 | >100 (-) | >100 (-) | >100 (-) |
| 15 | >100 (-) | >100 (-) | 25.7 (0.42) |
Ki values were calculated from IC50 values using the Cheng-Prusoff equation.48