Table 3. Binding affinity and inhibitory activities of compounds 1–8.
Compound | Inhibitory activities against 11β-HSD1 | Dissociation constant with 11β-HSD1 |
---|---|---|
Kd a (μM) | IC50 (μM) | |
1 | n.b.b | n.i. c |
2 | n.b. | n.i. |
3 | 82.1 ± 5.01 | 9.07 ± 0.61 |
4 | n.b. | n.i. |
5 | 420.51 ± 12.11 | 45.51 ± 7.82 |
6 | 513.14 ± 10.61 | 68.05 ± 7. 84 |
7 | n.b. | n.i. |
8 | n.b. | n.i. |
a The Kd value is automatic calculated by the curve fitting, and presents as means ± SD for three experiments.
b n.b. is no clear binding detected in the MST measurement.
c n.i. is no inhibition detected in the experiments (IC50 > 200 μM).