Assay Detail
Binding
CHEMBL655074
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In vitro inhibition of bovine trypsin.
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.51 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL339122 | — | — | 1 | 8.51 |
| CHEMBL340183 | — | — | 1 | 8.40 |
| CHEMBL556199 | — | — | 1 | 8.22 |
| CHEMBL421643 | — | — | 1 | 8.15 |
| CHEMBL124571 | — | — | 2 | 8.09 |
| CHEMBL421466 | — | — | 1 | 8.04 |
| CHEMBL127773 | — | — | 1 | 8.00 |
| CHEMBL339764 | — | — | 1 | 7.80 |
| CHEMBL340547 | — | — | 1 | 7.52 |
| CHEMBL124809 | — | — | 1 | 7.42 |
| CHEMBL339703 | — | — | 1 | 7.28 |
| CHEMBL341083 | — | — | 1 | 7.09 |
| CHEMBL542712 | — | — | 1 | 7.00 |
| CHEMBL341148 | — | — | 1 | 6.80 |
| CHEMBL340098 | — | — | 1 | 6.58 |
| CHEMBL127185 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL339122 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL340183 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL556199 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL421643 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL124571 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL421466 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL127773 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL339764 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL340547 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL124809 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL339703 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL341083 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL542712 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL341148 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL124571 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL340098 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL127185 | — | Ki | = | 960.0 | nM | 6.02 |