Table 2.
Entry |
Inhibitor |
AspH variant |
IC50 [μM][a] |
---|---|---|---|
1 |
MnCl2 |
wt [17] |
5.1±1.1 |
H679A |
23.1±8.6 |
||
H725A |
>40 |
||
2 |
CoCl2 |
wt [17] |
0.4±0.2 |
H679A |
1.5±0.2 |
||
H725A |
3.0±0.5 |
||
3 |
NiSO4 |
wt [17] |
0.17±0.08 |
H679A |
2.7±0.4 |
||
H725A |
1.8±0.4 |
||
4 |
Zn(OAc)2 |
wt [17] |
0.05±0.01 |
H679A |
0.16±0.01 |
||
H725A |
0.16±0.01 |
||
5 |
N‐oxalyl‐glycine (NOG) |
wt [17] |
1.1±0.3 |
H679A |
inactive |
||
H725A |
inactive |
||
6 |
Pyridine‐2,4‐dicarboxylic acid (2,4‐PDCA) |
wt [17] |
0.03±0.01 |
H679A |
0.13±0.01 |
||
H725A |
11.2±1.4 |
[a] Mean of two independent runs (n=2; mean ± SD). H679A/H725A AspH inhibition assays were performed as described in the Supporting Information Section 2 using 0.1 μM AspH variant and 4.0 μM hFX‐EGFD186‐124‐4Ser (Supporting Figure S2a); the assays were of good quality as high S/N ratios and Z′‐factors [19] (>0.5 for each plate) manifest (Supporting Figure S9).