Table 1.
IC50 values for inhibition of CypD PPIase activity by C31 derivatives
| Compound | CypD PPIase activity IC50 (μM) |
|---|---|
| CsA | 0.02 ± 0003 |
| ALV | 0.03 ± 0.005 |
| C31 | 0.20 ± 0.10 |
| C32 | 1.18 ± 0.43 |
| C71 | 0.79 ± 0.21 |
| C90 | 0.32 ± 0.16 |
| C99 | 0.63 ± 0.49 |
| C101 | 0.40 ± 0.19 |
| C104 | 0.22 ± 0.06 |
| C105 | 0.35 ± 0.16 |
| C106 | 1.26 ± 0.11 |
| C107 | 0.17 ± 0.05 |
| C108 | 0.48 ± 0.23 |
| C110 | 0.10 ± 0.02 |
| C112 | 0.48 ± 0.04 |
| C115 | 0.50 ± 0.32 |
| C119 | 0.15 ± 0.03 |
| C120 | 0.15 ± 0.05 |
| C123 | 1.26 ± 0.37 |
| C129 | 0.26 ± 0.07 |
| C131 | 0.48 ± 0.12 |
| C142 | 0.42 ± 0.10 |
| C143 | 0.72 ± 0.21 |
| C144 | 0.31 ± 0.16 |
| C170 | 1.05 ± 0.72 |
| C171 | 0.34 ± 0.13 |
| C172 | 0.21 ± 0.07 |
| C173 | 0.65 ± 0.14 |
| C177 | 0.49 ± 0.32 |
| C178 | 0.40 ± 0.19 |
| C179 | 0.28 ± 0.06 |
| C182 | 0.16 ± 0.03 |
| C183 | 0.26 ± 0.13 |
| C185 | 0.59 ± 0.19 |
ALV, alisporivir; CsA, cyclosporin A; CypD, cyclophilin D; PPIase, peptidyl-prolyl cis-trans isomerase.