Assay Detail
Binding
CHEMBL656686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against recombinant human cathepsin K determined in a fluorescence assay using 10 uM Cbz-Phe-Arg-AMC as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.27 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114462 | — | — | 1 | 9.89 |
| CHEMBL117658 | — | — | 1 | 9.46 |
| CHEMBL113948 | — | — | 1 | 9.30 |
| CHEMBL118016 | — | — | 1 | 9.25 |
| CHEMBL326164 | — | — | 1 | 9.06 |
| CHEMBL115756 | — | — | 1 | 8.96 |
| CHEMBL114844 | — | — | 1 | 8.82 |
| CHEMBL114161 | — | — | 1 | 8.74 |
| CHEMBL117144 | — | — | 1 | 8.70 |
| CHEMBL116779 | — | — | 1 | 8.68 |
| CHEMBL116724 | — | — | 1 | 8.62 |
| CHEMBL116402 | — | — | 1 | 8.57 |
| CHEMBL264458 | — | — | 1 | 8.54 |
| CHEMBL324986 | — | — | 1 | 8.51 |
| CHEMBL325976 | — | — | 1 | 8.40 |
| CHEMBL117149 | — | — | 1 | 8.34 |
| CHEMBL117304 | — | — | 1 | 8.33 |
| CHEMBL117303 | — | — | 1 | 8.27 |
| CHEMBL114904 | — | — | 1 | 8.19 |
| CHEMBL326494 | — | — | 1 | 8.12 |
| CHEMBL117082 | — | — | 1 | 7.92 |
| CHEMBL96875 | — | — | 1 | 7.29 |
| CHEMBL113842 | — | — | 1 | 7.15 |
| CHEMBL323674 | — | — | 1 | 7.00 |
| CHEMBL114951 | — | — | 1 | 6.57 |
| CHEMBL116932 | — | — | 1 | 6.27 |
| CHEMBL442755 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114462 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL117658 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL113948 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL118016 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL326164 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL115756 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL114844 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL114161 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL117144 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL116779 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL116724 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL116402 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL264458 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL324986 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL325976 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL117149 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL117304 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL117303 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL114904 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL326494 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL117082 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL96875 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL113842 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL323674 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL114951 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL116932 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL442755 | — | IC50 | = | 600.0 | nM | 6.22 |