Table 10. Sebetralstat Protease Selectivity.
| enzyme | IC50a (nM) | fold to PKa IC50 |
|---|---|---|
| plasma kallikrein | 6.0 | – |
| tissue kallikrein (KLK1) | >40000 | >6667 |
| factor XIIa | >40000 | >6667 |
| factor XIa | >40000 | >6667 |
| factor Xa | >10000 | >1667 |
| factor VIIa | >10000 | >1667 |
| plasmin | >40000 | >6667 |
| thrombin | >40000 | >6667 |
| trypsin | >40000 | >6667 |
| β-secretase 1 | >10000 | >1667 |
| cathepsin D | >10000 | >1667 |
| cathepsin G | >10000 | >1667 |
| renin | >10000 | >1667 |
| tissue plasminogen activator | >10000 | >1667 |
| tryptase | >10000 | >1667 |
a
IC50 values for sebetralstat inhibition of PKa and related proteases in isolated enzyme kinetic fluorogenic substrate assays.