Assay Detail
Binding
CHEMBL656673
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In vitro inhibitory activity against human cathepsin K, using 2 uM of Z -Leu-Arg-AMC as substrate
42
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.04 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331506 | — | — | 1 | 8.52 |
| CHEMBL184514 | — | — | 1 | 8.52 |
| CHEMBL122879 | — | — | 1 | 8.22 |
| CHEMBL2111806 | — | — | 1 | 8.22 |
| CHEMBL123227 | — | — | 1 | 8.10 |
| CHEMBL2448126 | — | — | 1 | 8.10 |
| CHEMBL122149 | — | — | 1 | 8.05 |
| CHEMBL123200 | — | — | 1 | 8.00 |
| CHEMBL123291 | — | — | 1 | 7.92 |
| CHEMBL333413 | — | — | 1 | 7.80 |
| CHEMBL123038 | — | — | 1 | 7.75 |
| CHEMBL123199 | — | — | 1 | 7.70 |
| CHEMBL334074 | — | — | 1 | 7.43 |
| CHEMBL121801 | — | — | 1 | 7.29 |
| CHEMBL122513 | — | — | 1 | 7.29 |
| CHEMBL122324 | — | — | 1 | 7.28 |
| CHEMBL122764 | — | — | 1 | 7.25 |
| CHEMBL123037 | — | — | 1 | 7.24 |
| CHEMBL122812 | — | — | 2 | 7.24 |
| CHEMBL122043 | — | — | 1 | 7.21 |
| CHEMBL126210 | — | — | 1 | 7.19 |
| CHEMBL2111805 | — | — | 1 | 7.10 |
| CHEMBL122431 | — | — | 1 | 7.06 |
| CHEMBL126152 | — | — | 1 | 7.01 |
| CHEMBL121807 | — | — | 1 | 6.85 |
| CHEMBL125656 | — | — | 1 | 6.82 |
| CHEMBL122318 | — | — | 1 | 6.54 |
| CHEMBL122424 | — | — | 1 | 6.31 |
| CHEMBL333716 | — | — | 1 | 6.21 |
| CHEMBL421457 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331506 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL184514 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL122879 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2111806 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL123227 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2448126 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL122149 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL123200 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL123291 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL333413 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL123038 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL123199 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL334074 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL122513 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL121801 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL122324 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL122764 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL123037 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL122812 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL122043 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL126210 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2111805 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL122431 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL126152 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL121807 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL125656 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL122812 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL122318 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL122424 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL333716 | — | IC50 | = | 614.0 | nM | 6.21 |
| CHEMBL421457 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL124159 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL122672 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL123592 | — | IC50 | = | 803.0 | nM | 6.09 |
| CHEMBL122561 | — | IC50 | = | 922.0 | nM | 6.04 |
| CHEMBL333987 | — | IC50 | = | 1015.0 | nM | 5.99 |
| CHEMBL122350 | — | IC50 | = | 1036.0 | nM | 5.99 |
| CHEMBL123178 | — | IC50 | = | 1227.0 | nM | 5.91 |
| CHEMBL332776 | — | IC50 | = | 1405.0 | nM | 5.85 |
| CHEMBL331422 | — | IC50 | = | 1463.0 | nM | 5.83 |
| CHEMBL123754 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL123987 | — | IC50 | > | 10000.0 | nM | - |