Table 2. Kinase Inhibition for the Selected Hit Finder Compounds.
| kinase
inhibition (IC50, nM ± SD)a |
||
|---|---|---|
| Compound | BCR-ABLWT | BCR-ABLT315I |
| 3c | 5.0 ± 0.3 | >10000 |
| 3d | 0.5 ± 0.3 | >10000 |
| 11b | 4.0 ± 0.3 | 547 ± 3.9 |
| 11c | 1000 | >10000 |
| 15 | 150 ± 16 | 360 ± 31 |
| 20 | 58.5 ± 1.0 | 120 ± 6.6 |
| 21b | 9.1 ± 2.8 | 670 ± 72 |
| 24 | 9.4 ± 2.0 | 16.1 ± 2.2 |
| 32 | 1.6 ± 0.3 | 390 ± 1.7 |
| imatinib | 190b | >10000b |
| dasatinib | 0.3b | 1140b |
| ponatinib | 2.2 ± 0.1 | 5.1 ± 0.1 |
a
IC50 was determined by following the biochemical kinase assay protocol. The data represent the mean and standard deviation of at least two independent experiments performed in duplicate.
b
Data taken from ref (52).