Table 3.
In-vivo and in vitro Aurora A activities of bisanilinopyrimidines with water-solubilizing moieties
| Entry | Compound ID | Aurora A in vitro IC50 (nM)a | Aurora A in vivo IC50 (μM) [Inhibition of Aurora A T288] | Aurora B in vitro IC50 (nM)b | Aurora B in vivo IC50 (μM) [Inhibition of H3-Ser10] |
|---|---|---|---|---|---|
| 44 |
|
216 ± 10.3 | 1-3 | 232 | 1-10 |
| 45 |
|
28.1 ± 5.5 | <1 | 93.9 | 1-10 |
| 46 |
|
18 ± 2.8 | 1-3 | 123 | 1-10 |
| 47 |
|
44.9 ± 4.7 | <1 | 180 | > 10 |
| 48 |
|
71.2 ± 9.0 | 1-3 | 174 | >10 |
| 49 |
|
316 ± 44.2 | 3-10 | 361 | 1-10 |
| 50 |
|
116.5 ± 10.6 | 3-10 | 1510 | >10 |
| 51 |
|
27 ± 7.6 | <1 | 194 | <1 |
| 52 |
|
30.2 ± 1.4 | <1 | 50.2 | <1 |
| 53 |
|
253 ± 41.6 | <1 | 43.3 | <1 |
| 54 |
|
21.4 ± 2.5 | <1 | 25.6 | <1 |
| 55 |
|
23.2 ± 1.6 | <1 | 30.0 | <1 |
| 56 |
|
12.3 ± 1.1 | <1 | 40.4 | <1 |
| 57 |
|
14.4 ± 1.7 | <1 | 10.7 | <1 |
| 58 |
|
21.2 ± 2.2 | <1 | 56.6 | >10 |
| 59 |
|
3.1 ± 0.16 | > 10 | 226 | > 10 |
| 60 |
|
2.9 ± 0.30 | 3-10 | 83.7 | >10 |
| 61 |
|
17.3 ± 2.3 | >10 | n.d. | >10 |
| 62 |
|
3.0 ± 0.53 | 3-10 | 106 | 1-10 |
a
Determined in-house using the DiscoveRx format
b
measured by Reaction Biology using a 33P assay.