Table 2. Target Inhibition by NBTIsa.
| compd | DNA gyrase IC50 (μM)b | TopoIV IC50 (μM)c | TopoIV/gyrase ratio |
|---|---|---|---|
| 2a | 0.047 (3) | 0.54 (3) | 11 |
| 3a | 0.23 (2) | 0.60 (2) | 2.6 |
| 4a | 0.23 (2) | 1.7 (2) | 7.6 |
| 2b | 2.1 (2) | 1.6 (2) | 0.76 |
| 3b | 0.58 (3) | 2.9 (3) | 5.0 |
| 2c | 1.8 (3) | 10 (2) | 5.6 |
| 3c | 1.7 (2) | 7.4 (2) | 4.4 |
| 3d | 3.5 (2) | 9.7 (2) | 2.8 |
| 2e | 4.2 (2) | 1.4 (2) | 0.33 |
| 3e | 1.6 (2) | 1.3 (5) | 0.81 |
| 4e | 0.19 (1) | 1.1 (2) | 5.8 |
| 2f | 1.4 (2) | 2.1 (2) | 1.5 |
| 4f | 0.15 (1) | 0.42 (1) | 2.8 |
| gepotidacin (racemic) | 0.17 (2) | 2.8 (3) | 16 |
| ciprofloxacin | 28 (2) | 8.6 (2) | 0.31 |
Average IC50 values from full concentration–response curves performed on separate days, with the number of replicate experiments in parentheses.
Inhibition of supercoiling activity.
Inhibition of decatenation activity.