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. Author manuscript; available in PMC: 2014 Feb 15.
Published in final edited form as: Bioorg Med Chem. 2012 Dec 20;21(4):891–902. doi: 10.1016/j.bmc.2012.12.010

Table 4.

Inhibition of Tubulin Assembly and Inhibition of Colchicine Binding.

Compd Inhibition of tubulin assembly
IC50 ± SD (µM)
Inhibition of colchicine binding
(% inhibition ± SD) at 5 µM
6 1.4 ± 0.007 84 ± 0.5
14 1.7 ± 0.2 76 ± 3
15 1.7 ± 0.07 82 ± 1
1 2.6 ± 0.05 70 ± 2
CA-4 1.0 ± 0.09 99 ± 0.2

Inhibition of tubulin assembly was performed as described previously,26 with tubulin at 10 µM (1.0 mg/mL) and varying concentrations of potential inhibitors. Extent of assembly at 20 min was the parameter measured. The CA-4 control is performed twice a year, and IC50 values obtained range from 1 to 1.2 µM. The most recent value is shown in the table. Inhibition of colchicine binding was performed as described previously,27 with tubulin at 1.0 µM and both [3H]colchicine and potential inhibitor at 5.0 µM. Incubation was for 10 min at 37 °C.