Assay Detail
Binding
CHEMBL3371671
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Inhibition of human recombinant matriptase-2 using Boc-Gln-Ala-Arg-AMC as substrate by microplate reader analysis
15
Total Activities
15
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 |
Publication
Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptase and matriptase-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.15 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354675 | — | — | 1 | 9.13 |
| CHEMBL3354683 | — | — | 1 | 8.99 |
| CHEMBL3354676 | — | — | 1 | 8.85 |
| CHEMBL3354685 | — | — | 1 | 8.70 |
| CHEMBL3354686 | — | — | 1 | 8.61 |
| CHEMBL3354684 | — | — | 1 | 8.59 |
| CHEMBL3354677 | — | — | 1 | 8.20 |
| CHEMBL3354674 | — | — | 1 | 8.11 |
| CHEMBL3354679 | — | — | 1 | 7.87 |
| CHEMBL3354678 | — | — | 1 | 7.81 |
| CHEMBL3354687 | — | — | 1 | 7.68 |
| CHEMBL3354682 | — | — | 1 | 7.61 |
| CHEMBL3352840 | — | — | 1 | 7.46 |
| CHEMBL3354680 | — | — | 1 | 7.33 |
| CHEMBL3354681 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354675 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL3354683 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL3354676 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3354685 | — | Ki | = | 1.98 | nM | 8.70 |
| CHEMBL3354686 | — | Ki | = | 2.48 | nM | 8.61 |
| CHEMBL3354684 | — | Ki | = | 2.56 | nM | 8.59 |
| CHEMBL3354677 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3354674 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL3354679 | — | Ki | = | 13.47 | nM | 7.87 |
| CHEMBL3354678 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL3354687 | — | Ki | = | 20.79 | nM | 7.68 |
| CHEMBL3354682 | — | Ki | = | 24.84 | nM | 7.61 |
| CHEMBL3352840 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL3354680 | — | Ki | = | 46.78 | nM | 7.33 |
| CHEMBL3354681 | — | Ki | = | 47.77 | nM | 7.32 |