Assay Detail
Binding
CHEMBL3708030
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 | 6.25 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2016869 | — | — | 1 | 8.04 |
| CHEMBL2016870 | — | — | 1 | 7.57 |
| CHEMBL2016868 | — | — | 1 | 7.34 |
| CHEMBL3666823 | — | — | 1 | 7.00 |
| CHEMBL3666824 | — | — | 1 | 6.73 |
| CHEMBL3666826 | — | — | 1 | 6.66 |
| CHEMBL2016872 | — | — | 1 | 6.29 |
| CHEMBL3666822 | — | — | 1 | 6.24 |
| CHEMBL2016866 | — | — | 1 | 5.70 |
| CHEMBL2016867 | — | — | 1 | 5.67 |
| CHEMBL3666821 | — | — | 1 | 5.52 |
| CHEMBL2016873 | — | — | 1 | 5.37 |
| CHEMBL2016874 | — | — | 1 | 5.34 |
| CHEMBL2016864 | — | — | 1 | 5.19 |
| CHEMBL3666825 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2016869 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2016870 | — | Ki | = | 26.8 | nM | 7.57 |
| CHEMBL2016868 | — | Ki | = | 45.4 | nM | 7.34 |
| CHEMBL3666823 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3666824 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL3666826 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL2016872 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL3666822 | — | Ki | = | 575.0 | nM | 6.24 |
| CHEMBL2016866 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL2016867 | — | Ki | = | 2119.0 | nM | 5.67 |
| CHEMBL3666821 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2016873 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL2016874 | — | Ki | = | 4560.0 | nM | 5.34 |
| CHEMBL2016864 | — | Ki | = | 6520.0 | nM | 5.19 |
| CHEMBL3666825 | — | Ki | = | 8400.0 | nM | 5.08 |