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. 2020 May 26;15(13):1139–1149. doi: 10.1002/cmdc.202000147

Table 2.

The inhibition of human AspH by C‐3 aminoalkyl‐substituted 2,4‐PDCA derivatives.

Compound

IC50 [μM][a]

1

18

0.58 ±0.06

2

25

3.95 ±0.33

3

26

7.66 ±1.45

4

27

10.91 ±1.83

5

28

10.76 ±0.28

6

29

0.28 ±0.11

7

30

1.22 ±0.26

8

31

1.86 ±1.06

9

32

3.67 ±0.74

10

33

13.13 ±4.84

[a] Mean average of two independent runs (n=2; mean ± SD). AspH inhibition assays were performed as described in the Experimental Section by using 50 nM His6‐AspH315‐758 and 1.0 μM hFX‐CP101‐119 (Figure 2D) as a substrate.