Assay Detail
Binding
CHEMBL4844450
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Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as substrate measured after 5 mins by microplate reader analysis
16
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.40 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189739 | BEROTRALSTAT | 4.0 | 3 | 8.24 |
| CHEMBL4847070 | — | — | 3 | 8.07 |
| CHEMBL4867028 | — | — | 1 | 8.00 |
| CHEMBL4847782 | — | — | 1 | 7.78 |
| CHEMBL4872758 | — | — | 1 | 7.72 |
| CHEMBL4846073 | — | — | 1 | 7.57 |
| CHEMBL4868429 | — | — | 1 | 6.54 |
| CHEMBL4852994 | — | — | 1 | 6.52 |
| CHEMBL4874867 | — | — | 1 | 5.89 |
| CHEMBL4854896 | — | — | 1 | - |
| CHEMBL4868583 | — | — | 1 | - |
| CHEMBL4854785 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4847070 | — | IC50 | = | 8.51 | nM | 8.07 |
| CHEMBL4867028 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4847782 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL4847070 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4872758 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4846073 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 48.1 | nM | 7.32 |
| CHEMBL4847070 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4868429 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL4852994 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4874867 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL4854896 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4868583 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4854785 | — | IC50 | > | 1000.0 | nM | - |