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| compound | inhibition of tubulin assembly IC50 (μM) ± SD | inhibition of colchicine binding (%) ± SD |
|---|---|---|
| 6a | 1.40 ± 0.01 | 80 ± 2.0 |
| 7g | 1.50 ± 0.20 | 88 ± 0.5 |
| 8c | 1.70 ± 0.20 | 82 ± 1.0 |
|
| ||
| CA-4c | 1.20 ± 0.20 | 98 ± 0.6 |
The tubulin assembly assay measured the extent of assembly of 10 μM tubulin after 20 min at 30 °C.
Tubulin: 1 μM. [3H]colchicine: 5 μM. Inhibitor: 5 μM. Incubation was performed for 10 min at 37 °C.
reference compound is a drug candidate in phase II clinical trial.
