Table 5. Biochemical and cellular characterization of the most potent TbrPDEB1 inhibitors.
| Compound | Reg Number | cLogP | TbrPDEB1 (IC50 μM)a |
TbrPDEB2 (IC50 μM)a |
hPDE4 (IC50 μM)a |
T brucei cell (EC50, μM)a |
|---|---|---|---|---|---|---|
| 3 | NEU-355 | 4.33 | 24 ± 1.7 | 29.8 ± 7.5 | 7.9×10−6 | 7.8 ± 2.5 |
| 10a | NEU-356 | 5.04 | 3.5 ± 0.3 | 15.1 ± 3.9 | - | 7.3 ± 0.97 |
| 17a | NEU-433 | 5.73 | 6.4 ± 1.7 | 6.2 ± 0.6 | 4.2×10−5 | 7.0± 3.9 |
| 17t | NEU-489 | 5.82 | 5.9 ± 1.0 | 13.5 ± 3.5 | - | 5.6 ± 1.9 |
| 19a | NEU-462 | 5.17 | 3.1 ± 0.5 | 8.0 ± 3.9 | 8.3×10−5 | 6.8 ± 0.82 |
| 19c | NEU-528 | 5.62 | 3.7 ± 0.5 | 5.6 ± 3.4 | - | 7.9 ± 2.7 |
| 24d | NEU-542 | 6.29 | 3.5 ± 0.5 | 12.1 ± 3.2 | - | 8.7± 1.8 |
a
All values are the mean of three or more replicates ± SEM.