Table 6.
Species selectivity: in vitro potency of BAY-678 (20) and BAY 85-8501 (29).
| Compd | Ki [nm][a] | Ser protease | ||||
|---|---|---|---|---|---|---|
| HNE | RNE | MNE[b] | panel IC50 [nm][c] | |||
| 20 | 15 | 600 | 700 | >30 000 | ||
| 29 | 0.08 | 8.0 | 6.0 | >30 000 |
[286]
Ki values were extrapolated from Dixon plots (Supporting Information). As expected, Ki values showed good correlation to the IC50 values.[24]
[b]
Murine neutrophil elastase.
[c]
IC50 values for 21 related serine proteases, including porcine pancreatic elastase (PPE), were determined by applying functional biochemical assays with the respective isolated enzyme and the appropriate fluorogenic peptide substrate (Supporting Information).