Assay Detail
Binding
CHEMBL817809
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory constant against trypsin
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.72 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277695 | — | — | 1 | 8.36 |
| CHEMBL416912 | — | — | 1 | 7.92 |
| CHEMBL431292 | CVS-2359 | — | 1 | 7.91 |
| CHEMBL19666 | — | — | 1 | 7.87 |
| CHEMBL19831 | — | — | 1 | 7.78 |
| CHEMBL19453 | — | — | 1 | 7.73 |
| CHEMBL19359 | — | — | 1 | 7.71 |
| CHEMBL19599 | CVS-2139 | — | 1 | 7.68 |
| CHEMBL279199 | — | — | 1 | 7.50 |
| CHEMBL19731 | — | — | 1 | 7.31 |
| CHEMBL283555 | — | — | 1 | 7.12 |
| CHEMBL19798 | — | — | 1 | - |
| CHEMBL19037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277695 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL416912 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL431292 | CVS-2359 | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL19666 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL19831 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL19453 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL19359 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL19599 | CVS-2139 | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL279199 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL19731 | — | Ki | = | 49.3 | nM | 7.31 |
| CHEMBL283555 | — | Ki | = | 76.5 | nM | 7.12 |
| CHEMBL19798 | — | Ki | > | 168.0 | nM | - |
| CHEMBL19037 | — | Ki | > | 168.0 | nM | - |