Assay Detail
Binding
CHEMBL5032466
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
18
Total Activities
18
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
Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.39 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081575 | — | — | 1 | 9.89 |
| CHEMBL5086585 | — | — | 1 | 9.00 |
| CHEMBL5091091 | — | — | 1 | 8.96 |
| CHEMBL5081508 | — | — | 1 | 8.66 |
| CHEMBL5077855 | — | — | 1 | 8.60 |
| CHEMBL5081335 | — | — | 1 | 8.51 |
| CHEMBL5084226 | — | — | 1 | 8.49 |
| CHEMBL5075134 | — | — | 1 | 8.47 |
| CHEMBL5088958 | — | — | 1 | 8.43 |
| CHEMBL5078472 | — | — | 1 | 8.42 |
| CHEMBL5083517 | — | — | 1 | 8.36 |
| CHEMBL5081851 | — | — | 1 | 8.21 |
| CHEMBL5081090 | — | — | 1 | 8.20 |
| CHEMBL5091578 | — | — | 1 | 8.11 |
| CHEMBL5092327 | — | — | 1 | 7.96 |
| CHEMBL5075263 | — | — | 1 | 7.70 |
| CHEMBL5074750 | — | — | 1 | 7.68 |
| CHEMBL5091873 | — | — | 1 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081575 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5086585 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5091091 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5081508 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5077855 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5081335 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5084226 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5075134 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5088958 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5078472 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5083517 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5081851 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5081090 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL5091578 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL5092327 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5075263 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5074750 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5091873 | — | IC50 | = | 41.0 | nM | 7.39 |