Table 1.
Inhibition constants and selectivity ratio (S.R.) of inhibitors for O-GlcNAcase, β-hexosaminidase B, NAGLU, VcNagZ and StNagZ.
| Compound | O-GlcNAcase Ki | β-Hexosaminidase B | NAGLU Ki | VcNagZ Ki | StNagZ Ki | S.R. | S.R. |
|---|---|---|---|---|---|---|---|
| [μM] | Ki [μM] | [μM] | [μM] | [μM] | (Ki OGA/Ki VcNagZ) | (Ki OGA/Ki StNagZ) | |
| 1 | 23 | 0.5435 | 0.4546 | 8.5 | 25.2 | 2.8 | 0.94 |
| 20 | 130 | 61 | 96 | 4.2 | 45.4 | 31 | 2.9 |
| 21 | >500 | 1460 | >1000 | 9.4 | 23.2 | >53 | >22 |
| 22 | >1000 | >5000 | >1000 | 110 | 47.3 | >9 | >21 |
| 23 | >1000 | >5000 | >1000 | 1135 | 102 | >0.9 | >10 |
| 24 | >1000 | 670 | 800 | 15.8 | 24.6 | 63 | >40 |
| 25 | >1000 | >5000 | >1000 | 555 | 294 | >1.8 | >3.4 |