TABLE 1.
Inhibition of PC1/3, PC2, and furin by individual pyrrolidine bispiperazines and bicyclic guanidines
Values represent the mean ± S.D. of Ki determinations carried out in triplicate.
|
Compound
|
Ki
|
||
|---|---|---|---|
| PC1/3 | PC2 | Furin | |
| μM | |||
| 1435-6 | >40 | 0.66 ± 0.10 | >25 |
| 1435-10 | >40 | 0.59 ± 0.08 | >25 |
| 1435-16 | >40 | 0.56 ± 0.07 | >25 |
| 1435-18 | >40 | 0.54 ± 0.10 | >25 |
| 1669-2 | >20 | 3.60 ± 0.30 | >15 |
| 1669-7 | >20 | 10.0 ± 0.90 | >15 |
| 1267-7 | >20 | 3.30 ± 0.50 | >15 |