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Inhibition of human mature cathepsin K.
| Compound | mCatK inhibitiona |
||
|---|---|---|---|
|
Ki (nM) |
kon (103 M−1 s−1) |
koff (10−3 s−1) |
|
| Gü2602 | 0.013 ± 0.008 | n.d.b | n.d.b |
| Gü1303 | 0.91 ± 0.04 | 527 ± 8 | 0.48 ± 0.03 |
aThe inhibition parameters were measured using a kinetic activity assay with the fluorogenic peptide substrate Cbz-Gly-Pro-Arg-AMC at pH 5.5. bn.d.: not determined for linear progress curves.
