Table 3. IC 50 values for the inhibitory effects of the test drugs (compounds and reference inhibitors) on the enzymatic activity of human COX-1 (rational assays selected by our modeling) and human MAO-B (control assays not selected by the modeling).
DRUG | IC50hCOX-1 (μM) | IC50 hMAO-B (μM) |
---|---|---|
Lapatinib | a19.5 % inhibition at 25 μM | ** |
SB-202190 | 23.59 ± 3.53 | ** |
RO-316233 | 25.35 ± 3.80 | ** |
GW786460X | ** | ** |
Indirubin-3′-monoxime | a28 % inhibition at 25 μM | ** |
Iproniazide (Reference inhibitor) | 7.54 ± 0.36 | |
Selegiline (Reference inhibitor) | 0.019 ± 0.001 | |
FR122047 (Reference inhibitor) | 0.094 ± 0.006 | |
Indomethacin (Reference inhibitor) | 12.16 ± 1.16 | |
Diclofenac (Reference inhibitor) | 18.23 ± 1.73 |
Each IC50 value is the mean ± S.E.M. from three experiments (n = 3). ** Inactive at 100 μM (highest concentration tested). a % enzymatic inhibition at 25 μM (compounds precipitated at higher concentrations).