Assay Detail
Binding
CHEMBL4374440
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal met-His6-tagged matriptase catalytic domain (Gly596 to Val855 residues) expressed in Escherichia coli 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 |
Target
Suppressor of tumorigenicity 14 protein (CHEMBL3018) ↗| 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 | 6.33 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454016 | — | — | 1 | 8.96 |
| CHEMBL4540950 | — | — | 1 | 8.21 |
| CHEMBL4469506 | — | — | 1 | 7.70 |
| CHEMBL4469962 | — | — | 1 | 7.52 |
| CHEMBL4530678 | — | — | 1 | 7.16 |
| CHEMBL4434900 | — | — | 1 | 7.05 |
| CHEMBL379186 | — | — | 1 | 6.62 |
| CHEMBL4436751 | — | — | 1 | 6.19 |
| CHEMBL4453382 | — | — | 1 | 6.14 |
| CHEMBL4462597 | — | — | 1 | 6.09 |
| CHEMBL4452723 | — | — | 1 | 5.96 |
| CHEMBL4527923 | — | — | 1 | 5.68 |
| CHEMBL4541290 | — | — | 1 | 5.62 |
| CHEMBL3781349 | — | — | 1 | 5.50 |
| CHEMBL4448976 | — | — | 1 | 5.40 |
| CHEMBL4537657 | — | — | 1 | 5.35 |
| CHEMBL4558850 | — | — | 1 | 5.12 |
| CHEMBL3403531 | — | — | 1 | 5.08 |
| CHEMBL4472744 | — | — | 1 | 5.00 |
| CHEMBL4559504 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454016 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4540950 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4469506 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4469962 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4530678 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4434900 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL379186 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4436751 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4453382 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4462597 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4452723 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4527923 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4541290 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3781349 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4448976 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4537657 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4558850 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3403531 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4472744 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4559504 | — | IC50 | > | 20000.0 | nM | - |