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A Four-Point Screening Method for Assessing Molecular Mechanism of Action (MMOA) Identifies Tideglusib as a Time-Dependent Inhibitor of Trypanosoma brucei GSK3β

Table 1

Evaluation of time dependent inhibition withTbGSK3β inhibitors.

Tideglusib, AZ960, CT99021, LY278544, sorafenib, and TWS119 were evaluated for time-dependent activity. The procedures are described in Fig 4. Data are the mean of duplicate experiments with N = 2 for each experiment. Data shown are percent inhibition of DMSO control. Ratio is % inhibition at 30 min preincubation/ % inhibition at 0 min preincubation at 10 μM ATP. Concentrations were selected based on preliminary screening IC50 measurements with no preincubation. IC50 values ± standard deviation +n = 3) were determined with 10 μM ATP and 10 μM GSM.

Table 1