Table 4.
Effect of 7a and 7b on the Chk1 activity in an in vitro assay system.
| NSC30049 (7a) and ASR352 (7b) Concentration (M) |
Percent activity |
Saturosporine Concentration (M) |
||
|---|---|---|---|---|
| NSC30049 (7a) | ASR352 (7b) | Staurosporine | ||
| 1.00E-04 | 91.54 | 90.47 | 0.31 | 2.00E-05 |
| 3.33E-05 | 105.37 | 95.76 | −1.28 | 5.00E-06 |
| 1.11E-05 | 94.37 | 94.16 | 1.47 | 1.25E-06 |
| 3.70E-06 | 106.53 | 96.66 | 2.55 | 3.13E-07 |
| 1.23E-06 | 113.75 | 95.86 | −0.27 | 7.81E-08 |
| 4.12E-07 | 99.00 | 105.75 | 6.54 | 1.95E-08 |
| 1.37E-07 | 100.06 | 106.27 | 9.81 | 4.88E-09 |
| 4.57E-08 | 92.52 | 106.18 | 13.67 | 1.22E-09 |
| 1.52E-08 | 92.23 | 90.13 | 41.24 | 3.05E-10 |
| 5.08E-09 | 112.15 | 104.82 | 55.99 | 7.63E-11 |
| DMSO | 103.06 | 100.00 | 96.94 | DMSO |
Compounds were tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Control compound, Staurosporine, was tested in 10-dose IC50 mode with 4-fold serial dilution starting at 20 μM. Reactions were carried out at 10 μM ATP. Data is presented as % enzyme activity (relative to DMSO controls).