Assay Detail
Binding
CHEMBL4308356
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Inhibition of Cathepsin L (unknown origin) using Z-Phe-Arg-7-amido-4-methylcoumarin as substrate preincubated for 2 mins followed by susbtrate addition by fluorescence based analysis
19
Total Activities
19
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
Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.57 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4451757 | — | — | 1 | 8.30 |
| CHEMBL4442543 | — | — | 1 | 7.70 |
| CHEMBL4473385 | — | — | 1 | 7.60 |
| CHEMBL4463665 | — | — | 1 | 7.40 |
| CHEMBL4578891 | — | — | 1 | 7.20 |
| CHEMBL4544254 | — | — | 1 | 6.80 |
| CHEMBL4455305 | — | — | 1 | 6.60 |
| CHEMBL4446278 | — | — | 1 | 6.60 |
| CHEMBL4440148 | — | — | 1 | 6.20 |
| CHEMBL4546133 | — | — | 1 | 6.20 |
| CHEMBL4586752 | — | — | 1 | 6.20 |
| CHEMBL4579894 | — | — | 1 | 6.10 |
| CHEMBL4515535 | — | — | 1 | 6.00 |
| CHEMBL4543467 | — | — | 1 | 6.00 |
| CHEMBL481611 | ODANACATIB | 3.0 | 1 | 5.90 |
| CHEMBL4535973 | — | — | 1 | 5.90 |
| CHEMBL4565840 | — | — | 1 | 5.80 |
| CHEMBL4456233 | — | — | 1 | 5.80 |
| CHEMBL4441186 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4451757 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4442543 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL4473385 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL4463665 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4578891 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4544254 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL4455305 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4446278 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4440148 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4546133 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4586752 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4579894 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4515535 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4543467 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL481611 | ODANACATIB | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4535973 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4565840 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4456233 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4441186 | — | Ki | > | 10000.0 | nM | - |