Assay Detail
Binding
CHEMBL3101481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of matriptase-SP1 (615 to 855) (unknown origin) expressed in Escherichia coli BL21(DE3) using Boc-Gln-Ala-Arg-7-amido-4-methyl coumarin hydrobromide as substrate by fluorescence assay
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
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.52 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099587 | — | — | 1 | 7.40 |
| CHEMBL3099586 | — | — | 1 | 7.40 |
| CHEMBL3099812 | — | — | 1 | 7.40 |
| CHEMBL3099585 | — | — | 1 | 7.00 |
| CHEMBL3099584 | — | — | 1 | 6.70 |
| CHEMBL3099813 | — | — | 1 | 6.70 |
| CHEMBL3099589 | — | — | 1 | 6.70 |
| CHEMBL3099583 | — | — | 1 | 6.40 |
| CHEMBL3099814 | — | — | 1 | 6.30 |
| CHEMBL3100168 | — | — | 1 | 6.22 |
| CHEMBL3099811 | — | — | 1 | 5.92 |
| CHEMBL3099588 | — | — | 1 | 5.54 |
| CHEMBL298415 | — | — | 1 | 5.02 |
| CHEMBL20936 | BENZAMIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099587 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3099586 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3099812 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3099585 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3099584 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3099813 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3099589 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3099583 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3099814 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL3100168 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3099811 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3099588 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL298415 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL20936 | BENZAMIDINE | Ki | = | 400000.0 | nM | - |