Assay Detail
Binding
CHEMBL3707836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Assay: The inhibition constants for human plasmin (h plasmin), human plasma kallikrein (h PK), thrombin and factor Xa were determined in analogy to a previously disclosed method (Stürzebecher et al., J. Med. Chem., 40, 3091-3099 (1997)), using a microplate reader (Multiscan Ascent, Thermo Scientific) at 405 nm. The reactions to determine the inhibition of human plasmin and human plasma kallikrein were carried out at 25° C. in 200 μl 50 mM Tris×HCl buffer pH 8.0 (containing 0.154 M NaCl, 2% ethanol and inhibitor in appropriate concentrations) and 25 μl substrate solution. Reactions were started by addition of 50 μl of enzyme solution.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Serine protease inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.38 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2016873 | — | — | 1 | 8.62 |
| CHEMBL3666822 | — | — | 1 | 8.05 |
| CHEMBL3666823 | — | — | 1 | 8.03 |
| CHEMBL2016874 | — | — | 1 | 8.00 |
| CHEMBL3666826 | — | — | 1 | 7.92 |
| CHEMBL2016870 | — | — | 1 | 7.76 |
| CHEMBL3666824 | — | — | 1 | 7.75 |
| CHEMBL2016866 | — | — | 1 | 7.60 |
| CHEMBL2016869 | — | — | 1 | 7.50 |
| CHEMBL2016872 | — | — | 1 | 7.47 |
| CHEMBL2016868 | — | — | 1 | 6.87 |
| CHEMBL3666825 | — | — | 1 | 6.50 |
| CHEMBL2016867 | — | — | 1 | 6.31 |
| CHEMBL3666821 | — | — | 1 | 6.26 |
| CHEMBL2016864 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2016873 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL3666822 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL3666823 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2016874 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL3666826 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2016870 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL3666824 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2016866 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2016869 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL2016872 | — | Ki | = | 34.2 | nM | 7.47 |
| CHEMBL2016868 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL3666825 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2016867 | — | Ki | = | 493.0 | nM | 6.31 |
| CHEMBL3666821 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2016864 | — | Ki | = | 868.0 | nM | 6.06 |