IC50 values of PIM-1 kinase inhibition of the most cytotoxic compounds.
| Compound | % of PIM-1 inhibition | IC50 ± SDa (nM) |
|---|---|---|
| 4 | 97.8 ± 1.8 | 11.4 ± 0.13 |
| 6 | 89.6 ± 2.1 | 34.6 ± 0.18 |
| 10 | 94.6 ± 2.1 | 17.2 ± 0.20 |
| 11 | 92.1 ± 1.9 | 21.4 ± 0.24 |
| Staurosporine | 95.6 ± 2.4 | 16.7 ± 0.32 |
| Pyrido[4,3-d]pyrimidine-derivative inhibitor (SKI-O-068)32 | — | 123 ± 14 |
a
Values are expressed as an average of three independent replicates. “IC50 values were calculated using sigmoidal non-linear regression curve fit of percentage inhibition against five concentrations of each compound”.