Table 1.
Kinetic Parameters
| KPC-2 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 0.32 ± 0.03 | 2.4 ± 0.9 × 105 | 4.5 ± 0.5 × 10−4 | 26 ± 3 | 1.9 ± 0.2 | 1 |
| 2 | 4.5 ± 0.5 | 9.4 ± 0.6 × 103 | 4.0 ± 0.4 × 10−4 | 29 ± 3 | 43 ± 5 | 1 |
| 1 | 7.8 ± 0.8 | 8.8 ± 0.9 × 103 | 3.5 ± 0.5 × 10−4 | 33 ± 5 | 40 ± 7 | 1 |
| avibactam | 0.9 ± 0.1 | 1.3 × 104a | 1.4 × 10−4a | 82a | 11a | 1 |
| relebactam | 2.2 ± 0.3 | 2.8 ± 0.3 × 104 | 2.5 ± 0.5 × 10−4 | 46 ± 9 | 9 ± 2 | 1 |
| ADC-7 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 8.0 ± 0.8 | 1.9 ± 0.2 × 104 | 1.0 ± 0.1 × 10−3 | 12 ± 2 | 53 ± 7 | 6 |
| 2 | 2.3 ± 0.3 | 3.5 ± 0.4 × 104 | 1.1 ± 0.1 × 10−3 | 11 ± 1 | 32 ± 3 | 4 |
| 1 | 3.7 ± 0.4 | 3.2 ± 0.3 × 104 | 9.0 ± 0.1 × 10−4 | 13 ± 1 | 29 ± 3 | 4 |
| avibactam | 19 ± 2 | 3.9 ± 0.4 × 103 | 3.5 ± 0.5 × 10−4 | 33 ± 5 | 90 ± 9 | 4 |
| relebactam | 12.6 ± 2 | 7.8 ± 0.8 × 103 | 3.0 ± 0.3 × 10−4 | 39 ± 4 | 39 ± 4 | 2 |
| PDC-3 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 3.8 ± 0.4 | 2.3 ± 0.2 × 104 | 2.8 ± 0.3 × 10−3 | 4.1 ± 0.4 | 124 ± 18 | 5 |
| 2 | 0.14 ± 0.01 | 4.8 ± 0.7 × 105 | 3.5 ± 0.4 × 10−3 | 3.3 ± 0.4 | 7.3 ± 1.4 | 1 |
| 1 | 0.13 ± 0.02 | 6.3 ± 0.6 × 105 | 4.0 ± 0.4 × 10−3 | 2.9 ± 0.3 | 6.3 ± 0.9 | 1 |
| avibactam | 2.5 ± 0.3a | 2.9 × 104a | 8 × 10−4a | 14.4a | 27.6a | 1 |
| relebactam | 3.2 ± 0.3 | 4.6 ± 0.5 × 104 | 9.0 ± 0.1 × 10−4 | 12.8 ± 1.4 | 20 ± 3 | 1 |
| OXA-23 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 8±1 | 1.7 ± 0.2 × 104 | 5.0 ± 0.5 × 10−4 | 23 ± 2 | 29 ± 4 | 1 |
| 2 | >100 | ND | ND | ND | ND | ND |
| 1 | >100 | ND | ND | ND | ND | ND |
| avibactam | >100 | 3 × 102a | 8.0 × 10−6a | 1,436a | 27a | ND |
| relebactam | >100 | ND | ND | ND | ND | ND |
| OXA-24/40 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 5.0 ± 0.5 | 9.6 ± 1.0 × 103 | 4.0 ± 0.4 × 10−4 | 29 ± 3 | 42 ± 6 | 2 |
| 2 | >100 | ND | ND | ND | ND | ND |
| 1 | >100 | ND | ND | ND | ND | ND |
| avibactam | >100 | 5.2 × 101a | 6.3 × 10−6a | 1,823a | 121a | ND |
| relebactam | >100 | ND | ND | ND | ND | ND |
| OXA-48 | Ki app (μM) | k2/K (M−1 s−1) | koff (s−1) | half-life (min) | Kd (nM) | kcat/kinact |
| 3 | 0.29 ± 0.03 | 6.4 ± 0.6 × 105 | 9.0 ± 0.1 × 10−4 | 13 ± 1 | 1.4 ± 0.2 | 2 |
| 2 | >100 | ND | ND | ND | ND | ND |
| 1 | >100 | ND | ND | ND | ND | ND |
| avibactam | 30 ± 3 | 1.4 × 103a | 1.2 ± × 10−5a | 1,000a | 9a | 1 |
| relebactam | >100 | ND | ND | ND | ND | ND |