Assay Detail
Binding
CHEMBL2073368
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Inhibition of human recombinant cathepsin B using Z-Arg-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 | 5.43 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070936 | — | — | 1 | 6.00 |
| CHEMBL2070937 | — | — | 1 | 5.80 |
| CHEMBL2071096 | — | — | 1 | 5.70 |
| CHEMBL2071098 | — | — | 1 | 5.60 |
| CHEMBL2070938 | — | — | 1 | 5.60 |
| CHEMBL2070939 | — | — | 1 | 5.60 |
| CHEMBL2070940 | — | — | 1 | 5.50 |
| CHEMBL2070942 | — | — | 1 | 5.50 |
| CHEMBL2071097 | — | — | 1 | 5.50 |
| CHEMBL2070951 | — | — | 1 | 5.50 |
| CHEMBL2069324 | — | — | 1 | 5.40 |
| CHEMBL2070950 | — | — | 1 | 5.40 |
| CHEMBL2071095 | — | — | 1 | 5.40 |
| CHEMBL2070946 | — | — | 1 | 5.40 |
| CHEMBL2070941 | — | — | 1 | 5.30 |
| CHEMBL2070948 | — | — | 1 | 5.30 |
| CHEMBL2070945 | — | — | 1 | 5.30 |
| CHEMBL2070944 | — | — | 1 | 5.30 |
| CHEMBL2070943 | — | — | 1 | 5.20 |
| CHEMBL2070947 | — | — | 1 | 5.10 |
| CHEMBL2070949 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070936 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2070937 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2071096 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL2071098 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2070938 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2070939 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL2070940 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2070942 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2071097 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2070951 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL2069324 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2070950 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2071095 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2070946 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL2070941 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL2070948 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL2070945 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL2070944 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL2070943 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL2070947 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2070949 | — | IC50 | = | 25118.86 | nM | 4.60 |