Table 1. Inhibition of tested proteases by compounds Camostat, “Novartis166” and “Novartis848”.
Protease | IC50 value/µM | ||
Camostat | Novartis166 | Novartis848 | |
h cationic trypsin | 0.0028 | 0.008 | 0.003 |
h anionic trypsin | – | 0.005 | – |
rat anionic trypsin S1-94 | <0.0003 | 0.001 | 0.0001 |
h thrombin | 0.458 | 39.3 | 20.5 |
h factor VIIa | 0.531 | >100 | >100 |
h factor Xa | 6.6 | 37.6 | 35.1 |
h factor XIa | 0.008 | 17.1 | 0.61 |
h factor XIIa | 8.0 | 43.0 | >100 |
h plasma kallikrein | 0.002 | 0.133 | 2.0 |
h kallikrein 1 | 72.4 | 18.8 | 4.48 |
h kallikrein 5 | 0.10 | 22.0 | 14.0 |
h kallikrein 7 | 41.5 | >100 | >100 |
h neutrophil elastase | 91.4 | 48.6 | >100 |
h pancreatic elastase | >50 | >100 | >100 |
rat pancreatic elastase | >100 | - | |
h cathepsin G | 44.6 | 61.0 | 54.6 |
h proteinase 3 | >50 | >100 | >100 |
h chymotrypsin | 12.17 | 2.26 | 59.3 |
h matriptase | 0.0065 | >30 | >100 |
h chymase | >50 | >100 | >100 |
h cathepsin K | >50 | >30 | >100 |
h cathepsin L | >50 | >30 | >100 |
h cathepsin S | >50 | >30 | >100 |
h cathepsin C | >50 | >30 | >100 |
h cathepsin B | >50 | - | >100 |