Assay Detail
Binding
CHEMBL5737779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Plasma Kallikrein Activity Assay: Plasma kallikrein activity assay. The effect of compounds of the invention on human plasma kallikrein activity was determined using the chromogenic substrates (DiaPharma Group, Inc., West Chester, Ohio, USA). In these experiments, 2 nM kallikrein (Enzyme Research Laboratories, South Bend, Ind., USA) was incubated with 80 μM S2302 (H-D-Pro-Phe-Arg-p-nitroaniline) in the absence or presence of increasing concentrations of compounds of the invention in a final volume of 200 μL Tris-HCl buffer (200 mM NaCl; 2.5 mM CaCl2; 50 mM Tris-HCl, pH 7.8).After incubation at 30° C., the activity of kallikrein was measured as a change in absorbance at OD 405 nm using BioTek Power Wave X340 Microplate Reader (Winooski, Vt., USA). Data were analyzed using SigmaPlot software.
906
Total Activities
244
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Human plasma kallikrein inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 302 | 7.60 | 7.60 |
| kon | 302 | - | - |
| k_off | 302 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5880741 | — | — | 3 | 7.60 |
| CHEMBL4867028 | — | — | 3 | 7.60 |
| CHEMBL5805068 | — | — | 3 | 7.60 |
| CHEMBL6030905 | — | — | 3 | 7.60 |
| CHEMBL5853740 | — | — | 3 | 7.60 |
| CHEMBL4854896 | — | — | 3 | 7.60 |
| CHEMBL5840895 | — | — | 3 | 7.60 |
| CHEMBL4852994 | — | — | 9 | 7.60 |
| CHEMBL5218665 | — | — | 3 | 7.60 |
| CHEMBL4847070 | — | — | 9 | 7.60 |
| CHEMBL5218770 | — | — | 9 | 7.60 |
| CHEMBL5218471 | — | — | 3 | 7.60 |
| CHEMBL6007256 | — | — | 3 | 7.60 |
| CHEMBL5847996 | — | — | 3 | 7.60 |
| CHEMBL5220941 | — | — | 3 | 7.60 |
| CHEMBL5877277 | — | — | 3 | 7.60 |
| CHEMBL5908529 | — | — | 3 | 7.60 |
| CHEMBL5220737 | — | — | 9 | 7.60 |
| CHEMBL5219216 | — | — | 9 | 7.60 |
| CHEMBL5949523 | — | — | 3 | 7.60 |
| CHEMBL4868429 | — | — | 9 | 7.60 |
| CHEMBL5770259 | — | — | 3 | 7.60 |
| CHEMBL5862639 | — | — | 3 | 7.60 |
| CHEMBL5751462 | — | — | 3 | 7.60 |
| CHEMBL4868583 | — | — | 3 | 7.60 |
| CHEMBL5872982 | — | — | 3 | 7.60 |
| CHEMBL5221062 | — | — | 3 | 7.60 |
| CHEMBL5900782 | — | — | 9 | 7.60 |
| CHEMBL5829884 | — | — | 9 | 7.60 |
| CHEMBL5889251 | — | — | 3 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5219926 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL6007256 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5762130 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5880741 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5966133 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5800986 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5929109 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5825652 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5908529 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5992835 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5770667 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5759971 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5939579 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5885714 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5218627 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5899953 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5830319 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5220941 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5848868 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5906069 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5829884 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5847996 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5796510 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5218476 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5751829 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5829884 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5827332 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4852994 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5885714 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5784656 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5218665 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5899953 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5899953 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4847070 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5850171 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5796510 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5288637 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5219643 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL6001154 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5218770 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4846073 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5997463 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5820462 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5219216 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5999054 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5918949 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5780759 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5219926 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5218471 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL6023303 | — | Ki | = | 25.1 | nM | 7.60 |