Table 2.
In vitro selectivity ratios of the Aurora inhibitor panel (fold difference in potency calculated by dividing Ki values measured for each kinase).
| Aur A versus Aur A-TPX21–43 | Aur A versus Aur B-INCENP783–918 | Aur A-TPX21–43 versus Aur B-INCENP783–918 | Aur B-INCENP783–918 versus Aur A | Aur B-INCENP783–918 versus Aur A-TPX21–43 | |
|---|---|---|---|---|---|
| VX-680 | 4.4 | 1.1 | 0.2 | 0.9 | 4.1 |
| MK-5108 | >4 | >149 | 39.1 | ||
| MK-8745 | 6.3 | 1030 | 162 | ||
| MLN8054 | 5.5 | 11.3 | 2.1 | ||
| MLN8237 | 5.5 | 26.8 | 4.9 | ||
| Genentech Aurora Inhibitor 1 | 0.4 | 274 | 654 | ||
| ZM447439 | 6.1 | 30 | 184 | ||
| AZD1152-HQPA | 4.2 | 3759 | 15779 | ||
| Hesperadin | 1.1 | 40.2 | 45.3 | ||
| GSK1070916 | 8.1 | 42.2 | 343 |