Table 2.
Reference IC50 parameters of the substrate compounds. Relative conversions (Rel. conv., control incubation with no inhibition is 100%) measured in the presence of 10 μM concentration of the compound tested. Mean ± SD, n = 3.
Comp. | Structure | Arom | STS | 17β-HSD1 |
---|---|---|---|---|
IC50 ± SD (µM) | IC50 ± SD (µM) | IC50 ± SD (µM) | ||
Testosterone (2) | ![]() |
0.52 ± 0.14 | ||
E1S (3) | ![]() |
5.2 ± 1.2 | ||
E1 (4) | ![]() |
>10 Rel. conv. 78 ± 7% | 24 ± 10 | 0.63 ± 0.11 |
IC50: the inhibitor concentration decreasing the enzyme activity to 50%. Ki: inhibitor constant determined from Dixon plot; SD: standard deviation.