Assay Detail
Binding
CHEMBL4374438
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Inhibition of recombinant HGFA serine protease domain (unknown origin) using Boc-QLR-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorescence based 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 |
Target
Hepatocyte growth factor activator (CHEMBL3351190) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.42 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454016 | — | — | 1 | 7.22 |
| CHEMBL4540950 | — | — | 1 | 7.18 |
| CHEMBL4434900 | — | — | 1 | 6.11 |
| CHEMBL4469962 | — | — | 1 | 5.92 |
| CHEMBL4469506 | — | — | 1 | 5.22 |
| CHEMBL4448976 | — | — | 1 | 5.20 |
| CHEMBL4462597 | — | — | 1 | 5.07 |
| CHEMBL4559504 | — | — | 1 | 5.06 |
| CHEMBL4541290 | — | — | 1 | 5.05 |
| CHEMBL379186 | — | — | 1 | 4.96 |
| CHEMBL4452723 | — | — | 1 | 4.85 |
| CHEMBL4537657 | — | — | 1 | 4.75 |
| CHEMBL3781349 | — | — | 1 | 4.70 |
| CHEMBL3403531 | — | — | 1 | 4.52 |
| CHEMBL4527923 | — | — | 1 | - |
| CHEMBL4530678 | — | — | 1 | - |
| CHEMBL4436751 | — | — | 1 | - |
| CHEMBL4453382 | — | — | 1 | - |
| CHEMBL4558850 | — | — | 1 | - |
| CHEMBL4472744 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454016 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4540950 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4434900 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4469962 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4469506 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4448976 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4462597 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4559504 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4541290 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL379186 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4452723 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4537657 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3781349 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3403531 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4527923 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4530678 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4436751 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4453382 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4558850 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4472744 | — | IC50 | > | 20000.0 | nM | - |