Table 1 Selectivity of inhibitors against cpA production in clonal striatal X57 cells (EC50) compared to selectivity against purified aspartic proteases (IC50) in μM.
From: Huntingtin cleavage product A forms in neurons and is reduced by gamma-secretase inhibitors
Compound | Human Htt cpA EC50 | Human BACE1 IC50 | Human BACE2 IC50 | Human Cathepsin D IC50 | Human Cathepsin E IC50 | Porcine Pepsin IC50 |
|---|---|---|---|---|---|---|
P1-N031 | 0.2 | 5.5 | 3.1 | 0.018 | 0.0002 | 0.29 |
P1-N034 | 4.9 | < 0.0005 | 0.0006 | ~0.5 | 0.002 | 0.79 |
P1-N038 | > 10 | 0.007 | 0.014 | 0.52 | 0.81 | 0.14 |
P1-N039 | 1.3 | 0.003 | 0.003 | 0.0006 | 0.0002 | 0.0002 |