Table 3 Binding affinity and inhibitory activities of compounds 1–8.

From: Novel small molecule 11β-HSD1 inhibitor from the endophytic fungus Penicillium commune

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.

  1. a The Kd value is automatic calculated by the curve fitting and presents as means ± SD for three experiments.
  2. b n.b. is no clear binding detected in the MST measurement.
  3. c n.i. is no inhibition detected in the experiments (IC50 > 200 μM).
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