TABLE 3.
Kinetic parameters of inhibition
| Tazobactam | LN-1-255 | |
|---|---|---|
| KDa(μm) | ||
| SHV-1 | 0.333 ± 0.033 | 0.027 ± 0.002 |
| SHV-2 | 0.182 ± 0.018 | 0.015 ± 0.002 |
| KDb(μm) | ||
| SHV-1 | 0.206 ± 0.019 | 0.019 ± 0.003 |
| SHV-2 | 0.041 ± 0.009 | 0.009 ± 0.002 |
| KI (μm) | ||
| SHV-1 | 0.200 ± 0.035 | 0.11 ± 0.01 |
| SHV-2 | 0.030 ± 0.003 | 0.10 ± 0.01 |
| kinact (s–1) | ||
| SHV-1 | 0.14 ± 0.01 | 0.55 ± 0.03 |
| SHV-2 | 0.030 ± 0.003 | 0.71 ± 0.07 |
| kinact/KI (s–1 μm–1) | ||
| SHV-1 | 0.70 ± 0.12 | 5.0 ± 0.7 |
| SHV-2 | 1.00 ± 0.14 | 7.1 ± 1.1 |
| tn | ||
| SHV-1 | 9 | 4 |
| SHV-2 | 9 | 0 |
a
KD measured using a direct competition reaction
b
KD measured using progress curves