Assay Detail
Binding
CHEMBL5521822
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal Met/6His tagged human recombinant matriptase catalytic domain (Gly596 to Val855 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis
14
Total Activities
14
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
Mechanism-Based Macrocyclic Inhibitors of Serine Proteases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.57 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5559738 | — | — | 1 | 8.54 |
| CHEMBL5558547 | — | — | 1 | 8.47 |
| CHEMBL5560415 | — | — | 1 | 8.24 |
| CHEMBL5555448 | — | — | 1 | 8.01 |
| CHEMBL5562350 | — | — | 1 | 7.85 |
| CHEMBL5564865 | — | — | 1 | 7.77 |
| CHEMBL5560759 | — | — | 1 | 7.50 |
| CHEMBL5559988 | — | — | 1 | 7.41 |
| CHEMBL5561725 | — | — | 1 | 7.27 |
| CHEMBL5557087 | — | — | 1 | 7.24 |
| CHEMBL5568169 | — | — | 1 | 7.05 |
| CHEMBL5556134 | — | — | 1 | 7.04 |
| CHEMBL5558228 | — | — | 1 | 6.85 |
| CHEMBL5557551 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5559738 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5558547 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5560415 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5555448 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5562350 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5564865 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5560759 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5559988 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5561725 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5557087 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5568169 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5556134 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5558228 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5557551 | — | IC50 | = | 180.0 | nM | 6.75 |