Assay Detail
Binding
CHEMBL901116
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Inhibition of human matriptase
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 | Intermediate |
Target
Suppressor of tumorigenicity 14 protein (CHEMBL3018) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.74 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL239127 | — | — | 1 | 7.00 |
| CHEMBL268861 | — | — | 1 | 6.80 |
| CHEMBL437180 | — | — | 1 | 6.42 |
| CHEMBL240132 | — | — | 1 | 6.35 |
| CHEMBL409191 | — | — | 1 | 6.07 |
| CHEMBL410952 | — | — | 1 | 6.05 |
| CHEMBL430087 | — | — | 1 | 6.00 |
| CHEMBL397832 | — | — | 1 | 5.63 |
| CHEMBL394723 | — | — | 1 | 5.32 |
| CHEMBL394724 | — | — | 1 | 4.65 |
| CHEMBL267455 | — | — | 1 | 4.55 |
| CHEMBL412487 | — | — | 1 | 4.05 |
| CHEMBL397831 | — | — | 1 | - |
| CHEMBL412486 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL239127 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL268861 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL437180 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL240132 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL409191 | — | Ki | = | 857.0 | nM | 6.07 |
| CHEMBL410952 | — | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL430087 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL397832 | — | Ki | = | 2330.0 | nM | 5.63 |
| CHEMBL394723 | — | Ki | = | 4750.0 | nM | 5.32 |
| CHEMBL394724 | — | Ki | = | 22500.0 | nM | 4.65 |
| CHEMBL267455 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL412487 | — | Ki | = | 90000.0 | nM | 4.05 |
| CHEMBL397831 | — | Ki | = | 107000.0 | nM | - |
| CHEMBL412486 | — | Ki | > | 250000.0 | nM | - |