Assay Detail
Binding
CHEMBL3389936
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Inhibition of recombinant hepsin (unknown origin) using Boc-QAR-AMC as substrate by fluorescence assay
20
Total Activities
20
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
Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 9.10 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3356591 | — | — | 1 | 9.68 |
| CHEMBL3356597 | — | — | 1 | 9.68 |
| CHEMBL3356589 | — | — | 1 | 9.66 |
| CHEMBL3356594 | — | — | 1 | 9.55 |
| CHEMBL3356595 | — | — | 1 | 9.47 |
| CHEMBL3356590 | — | — | 1 | 9.39 |
| CHEMBL3356606 | — | — | 1 | 9.33 |
| CHEMBL273264 | NAFAMOSTAT | 3.0 | 1 | 9.28 |
| CHEMBL3356600 | — | — | 1 | 9.26 |
| CHEMBL3356596 | — | — | 1 | 9.24 |
| CHEMBL3356592 | — | — | 1 | 9.24 |
| CHEMBL3356599 | — | — | 1 | 9.22 |
| CHEMBL3356604 | — | — | 1 | 9.21 |
| CHEMBL3356603 | — | — | 1 | 9.17 |
| CHEMBL3356598 | — | — | 1 | 8.92 |
| CHEMBL3356605 | — | — | 1 | 8.92 |
| CHEMBL3356602 | — | — | 1 | 8.85 |
| CHEMBL3356593 | — | — | 1 | 8.68 |
| CHEMBL3356601 | — | — | 1 | 8.07 |
| CHEMBL191881 | LEUPEPTIN | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3356591 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3356597 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3356589 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3356594 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3356595 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3356590 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3356606 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL273264 | NAFAMOSTAT | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL3356600 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL3356596 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL3356592 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL3356599 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3356604 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL3356603 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL3356598 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3356605 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3356602 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3356593 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3356601 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL191881 | LEUPEPTIN | Ki | = | 61.0 | nM | 7.21 |