Assay Detail
Binding
CHEMBL868299
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Inhibition of recombinant human cathepsin K in a fluorescence assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.07 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL203663 | — | — | 1 | 9.48 |
| CHEMBL117658 | — | — | 1 | 9.46 |
| CHEMBL113948 | — | — | 1 | 9.30 |
| CHEMBL204605 | — | — | 1 | 9.03 |
| CHEMBL426308 | — | — | 1 | 8.96 |
| CHEMBL114161 | — | — | 1 | 8.74 |
| CHEMBL438798 | — | — | 1 | 7.62 |
| CHEMBL204666 | — | — | 1 | 7.51 |
| CHEMBL205173 | — | — | 1 | 7.46 |
| CHEMBL204103 | — | — | 1 | 7.44 |
| CHEMBL204102 | — | — | 1 | 7.40 |
| CHEMBL205062 | — | — | 1 | 7.35 |
| CHEMBL381715 | — | — | 1 | 7.32 |
| CHEMBL96875 | — | — | 1 | 7.29 |
| CHEMBL383002 | — | — | 1 | 7.24 |
| CHEMBL204133 | — | — | 1 | 7.23 |
| CHEMBL425042 | — | — | 1 | 7.14 |
| CHEMBL203501 | — | — | 1 | 7.14 |
| CHEMBL203766 | — | — | 1 | 7.03 |
| CHEMBL382947 | — | — | 1 | 6.96 |
| CHEMBL380636 | — | — | 1 | 6.89 |
| CHEMBL369961 | — | — | 1 | 6.80 |
| CHEMBL204451 | — | — | 1 | 6.77 |
| CHEMBL380659 | — | — | 1 | 6.77 |
| CHEMBL204197 | — | — | 1 | 6.75 |
| CHEMBL204448 | — | — | 1 | 6.70 |
| CHEMBL204913 | — | — | 1 | 6.66 |
| CHEMBL383206 | — | — | 1 | 6.58 |
| CHEMBL381047 | — | — | 1 | 6.55 |
| CHEMBL204123 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL203663 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL117658 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL113948 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL204605 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL426308 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL114161 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL438798 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL204666 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL205173 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL204103 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL204102 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL205062 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL381715 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL96875 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL383002 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL204133 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL425042 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL203501 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL203766 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL382947 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL380636 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL369961 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL204451 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL380659 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL204197 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL204448 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL204913 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL383206 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL381047 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL204123 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL204079 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL204592 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL204907 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL204305 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL381837 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL205071 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL383406 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL204744 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL204537 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL203719 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL381474 | — | IC50 | = | 33000.0 | nM | 4.48 |