Table 1. Virtual screening hits and their in vitro assay results for mTOR inhibitions.
Compound | % of mTOR inhibition at 10 μMa | IC50(μM)b |
---|---|---|
6 | 22% | ND |
9 | 23% | ND |
12 | 30% | ND |
13 | 76% | 5.83 ± 1.85 |
17 | 61% | 7.59 ± 2.44 |
18 | 38% | >50 |
20 | 55% | 9.20 ± 2.15 |
21 | 50% | 14.38 ± 2.02 |
25 | 36% | >50 |
26 | 33% | >50 |
27 | 38% | 28.65 ± 2.65 |
33 | 21% | ND |
36 | 31% | 14.88 ± 1.01 |
37 | 22% | ND |
40 | 91% | 1.47 ± 0.33 |
Wortmaninc | – | 0.14 ± 0.02 |
a% Inhibition values are the mean ± SD of triplicate measurements at 10 μM.
bIC50 values for mTOR shown are the mean ± SD of triplicate measurements.
cUsed as a positive control compound. ND: not determined. Wortmanin is suggested and supplied by CBA104-1KIT from Calbiochem.