Table 3.
enzyme | inhibitor | IC50 (μM) | Ki (μM) |
---|---|---|---|
Eis_wt | 1 | 0.088 ± 0.012 | 0.048 ± 0.003 |
2 | 0.197 ± 0.025 | 0.095 ± 0.005 | |
3 | 0.093 ± 0.02 | 0.096 ± 0.010 | |
Eis_D26A | 1 | >200 | –a |
2 | >200 | – | |
3 | >200 | – | |
Eis_W36A | 1 | >200 | – |
2 | >200 | – | |
3 | >200 | – | |
Eis_W36R | 1 | 0.046 ± 0.016 | 0.037 ± 0.004 |
2 | >200 | – | |
3 | >200 | – | |
Eis_R37A | 1 | 0.388 ± 0.071 | 0.175 ± 0.037 |
2 | 0.301 ± 0.047 | 0.197 ± 0.017 | |
3 | 0.252 ± 0.024 | 0.185 ± 0.015 | |
Eis_R37G | 1 | >200 | – |
2 | 0.975 ± 0.080 | 0.351 ± 0.047 | |
3 | 1.72 ± 0.21 | 0.349 ± 0.039 | |
Eis_L63A | 1 | >200 | – |
2 | 0.227 ± 0.018 | 0.147 ± 0.014 | |
3 | 0.148 ± 0.016 | 0.063 ± 0.006 | |
Eis_M65A | 1 | 0.643 ± 0.099 | 0.122 ± 0.015 |
2 | >200 | – | |
3 | >200 | – | |
Eis_S83G | 1 | 0.880 ± 0.080 | 1.03 ± 0.09 |
2 | >200 | – | |
3 | 0.118 ± 0.017 | 0.060 ± 0.006 | |
Eis_F84A | 1 | >200 | – |
2 | >200 | – | |
3 | >200 | – |
Ki measurements were not carried out for IC50 > 200 μM due to very weak inhibitor binding.