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Selectivity studies of BACE 1 inhibitors against BACE 2 & cathepsin D
| Entry | Inhibitor | BACE 1 Ki(nM) |
BACE 2 Ki(nM |
CD Ki(nM) |
BACE 2/BACE 1 (Selectivity) |
CD/BACE1 (Selectivity) |
|---|---|---|---|---|---|---|
| 1 | 4 | 27.12 | 1450 | 8264 | >55 | >300 |
| 2 | 5 | 0.017 | 120 | 4300 | >7000 | >250,000 |
| 3 | 18 | 7.3 | --- | 7100 | --- | >970 |
| 4 | 19 | 0.4 | --- | 690 | --- | >1700 |
| 5 | 20 | 0.036 | 11 | 530 | >300 | >14,700 |
| 6 | 22 | 0.47 | --- | 2000 | --- | >4,200 |
