TABLE 5.
Enzyme mutation | Inhibitor | k2/K (M−1 s−1) | koff (s−1) | Residence time (min) | Kd (nM) |
---|---|---|---|---|---|
WT | Avibactam | 2.3 × 104 ± 0.2 × 104 | 3.3 × 10−4 ± 0.1 × 10−4 | 51 ± 2 | 14 ± 1 |
S130G | Avibactam | 8.6 ± 1.3 | ND | ND | ND |
WT | Vaborbactam | 5.8 × 103 ± 0.3 × 103 | 4.3 × 10−5 ± 0.6 × 10−5 | 394 ± 50 | 7.4 ± 0.9 |
S130G | Vaborbactam | 6.7 × 104 ± 0.3 × 104 | 4.5 × 10−3 ± 1.0 × 10−3 | 3.8 ± 1.0 | 67 ± 13 |
ND, not determined.