Assay Detail
Binding
CHEMBL4374439
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal 10-His tagged hepsin (Arg45 to Leu417) expressed in mouse myeloma cells using Boc-QAR-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 |
Publication
Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.68 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454016 | — | — | 1 | 9.77 |
| CHEMBL4540950 | — | — | 1 | 9.49 |
| CHEMBL4530678 | — | — | 1 | 9.30 |
| CHEMBL4469962 | — | — | 1 | 9.22 |
| CHEMBL4469506 | — | — | 1 | 8.70 |
| CHEMBL4434900 | — | — | 1 | 8.30 |
| CHEMBL4452723 | — | — | 1 | 8.10 |
| CHEMBL4453382 | — | — | 1 | 8.00 |
| CHEMBL4462597 | — | — | 1 | 7.70 |
| CHEMBL4436751 | — | — | 1 | 7.70 |
| CHEMBL4541290 | — | — | 1 | 7.22 |
| CHEMBL4448976 | — | — | 1 | 7.22 |
| CHEMBL4537657 | — | — | 1 | 7.16 |
| CHEMBL4558850 | — | — | 1 | 7.16 |
| CHEMBL4527923 | — | — | 1 | 7.05 |
| CHEMBL3403531 | — | — | 1 | 7.05 |
| CHEMBL4472744 | — | — | 1 | 6.96 |
| CHEMBL4559504 | — | — | 1 | 6.96 |
| CHEMBL3781349 | — | — | 1 | 5.72 |
| CHEMBL379186 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454016 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4540950 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4530678 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4469962 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4469506 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4434900 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4452723 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4453382 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4462597 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4436751 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4541290 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4448976 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4537657 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4558850 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4527923 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3403531 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4472744 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4559504 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3781349 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL379186 | — | IC50 | = | 14000.0 | nM | 4.85 |