TABLE 2.
Selection of hit compounds and their normalized inhibitory activity in MT-stimulated ATPase assays
Shown are the averages and S.D. values of 6–12 independent measurements. STLC, which binds to the loop-5 pocket, is not expected to inhibit PvEg5, which has a different loop-5 sequence.
| Compound (12.5 μm) | PvEg5 |
HsEg5 |
||
|---|---|---|---|---|
| MT-stimulated rate | Normalized rate | MT-stimulated rate | Normalized rate | |
| s−1 | % | s−1 | % | |
| DMSO | 1.21 ± 0.10 | 6.49 ± 0.31 | ||
| STLC | 1.04 ± 0.04 | 86 ± 5 | 1.43 ± 0.13 | 22 ± 3 |
| NSC19063 | 0.06 ± 0.03 | 5 ± 1 | 3.53 ± 0.01 | 54 ± 1 |
| NSC99796 | 0.03 ± 0.03 | 2 ± 2 | 4.92 ± 0.18 | 76 ± 3 |
| MMV666693 | 0.69 ± 0.16 | 57 ± 13 | 7.06 ± 0.74 | 109 ± 11 |
| NSC80141 | 0.46 ± 0.09 | 38 ± 8 | 0.29 ± 0.20 | 4 ± 4 |
| NSC70931 | 0.06 ± 0.01 | 5 ± 1 | 0.98 ± 0.47 | 15 ± 7 |
| NSC44750 | 0.06 ± 0.07 | 5 ± 5 | 1.01 ± 1.01 | 15 ± 8 |
| NSC92937 | 0.02 ± 0.03 | 2 ± 2 | 0.69 ± 0.61 | 11 ± 9 |
| NSC228150 | 0.08 ± 0.04 | 6 ± 3 | 1.93 ± 0.03 | 30 ± 1 |
| NSC129260 | 0.50 ± 0.13 | 42 ± 11 | 2.42 ± 0.58 | 37 ± 9 |
| NSC65248 | 0.66 ± 0.15 | 55 ± 13 | 4.36 ± 0.17 | 67 ± 3 |