Table 2. Inhibition constants determined by the standard kinetic assay and DIANA.
| Compound | Chemical formula | Ki (kinetic assay) (pH 6.15) (nM) | Ki (DIANA) (pH 7.4) (nM) | Fold Ki |
|---|---|---|---|---|
| 1 |  |
24 ± 5 | 33 ± 8 | 1.4 |
| 2 |  |
26 ± 4 | 52 ± 9 | 2.0 |
| 3 |  |
39 ± 1 | 100 ± 20 | 2.6 |
| 4 |  |
24 ± 4 | 31 ± 6 | 1.3 |
| 5 |  |
2100 ± 200 | 2000 ± 500 | 1.0 |
| 6 |  |
140 ± 30 | 570 ± 180 | 4.1 |
| 7 |  |
46 ± 12 | 570 ± 200 | 12 |
| 8 |  |
15 ± 2 | 170 ± 60 | 11 |
| 9 |  |
250 ± 40 | 960 ± 260 | 3.8 |
| 10 |  |
13 000 ± 1000 | 16 000 ± 5000 | 1.3 |
| 11 |  |
43 000 ± 11 000 | 210 000 ± 110 000 | 5 |
The chemical formulae of the inhibitors are also shown. The ‘fold Ki’ parameter represents the ratio Ki (DIANA, pH 7.4)/Ki (kinetic assay, pH 6.15). Substitutions of the moieties in oseltamivir carboxylate (4) are highlighted in blue. The Ki values for both assays were calculated from two independent experiments.