Assay Detail
Binding
CHEMBL2073365
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Inhibition of human recombinant cathepsin K using Z-Phe-Arg-AMC as substrate preincubated for 30 mins measured after 1 hr by quenched fluorescent resonance energy transfer assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.56 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070937 | — | — | 1 | 8.00 |
| CHEMBL2070942 | — | — | 1 | 8.00 |
| CHEMBL2071098 | — | — | 1 | 7.90 |
| CHEMBL2071096 | — | — | 1 | 7.90 |
| CHEMBL2069324 | — | — | 1 | 7.80 |
| CHEMBL2070951 | — | — | 1 | 7.80 |
| CHEMBL2070936 | — | — | 1 | 7.80 |
| CHEMBL2070941 | — | — | 1 | 7.70 |
| CHEMBL2070940 | — | — | 1 | 7.70 |
| CHEMBL2070939 | — | — | 1 | 7.70 |
| CHEMBL2070944 | — | — | 1 | 7.60 |
| CHEMBL2071097 | — | — | 1 | 7.60 |
| CHEMBL2070938 | — | — | 1 | 7.60 |
| CHEMBL2070947 | — | — | 1 | 7.60 |
| CHEMBL2070945 | — | — | 1 | 7.50 |
| CHEMBL2070950 | — | — | 1 | 7.50 |
| CHEMBL2070948 | — | — | 1 | 7.40 |
| CHEMBL2071095 | — | — | 1 | 7.30 |
| CHEMBL2070943 | — | — | 1 | 7.20 |
| CHEMBL2070946 | — | — | 1 | 6.70 |
| CHEMBL2070949 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070937 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2070942 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2071098 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL2071096 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL2069324 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2070951 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2070936 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2070941 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2070940 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2070939 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2070944 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2071097 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2070938 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2070947 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2070945 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2070950 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2070948 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL2071095 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL2070943 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL2070946 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL2070949 | — | IC50 | = | 316.23 | nM | 6.50 |