Assay Detail
Binding
CHEMBL4844448
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Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as substrate measured after 3 mins by microplate reader analysis
32
Total Activities
28
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 | 32 | 6.93 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189739 | BEROTRALSTAT | 4.0 | 3 | 9.06 |
| CHEMBL4847070 | — | — | 3 | 8.92 |
| CHEMBL4847782 | — | — | 1 | 8.28 |
| CHEMBL4868429 | — | — | 1 | 8.19 |
| CHEMBL4872758 | — | — | 1 | 8.14 |
| CHEMBL4867028 | — | — | 1 | 8.00 |
| CHEMBL4846073 | — | — | 1 | 7.98 |
| CHEMBL4854896 | — | — | 1 | 7.43 |
| CHEMBL4852994 | — | — | 1 | 7.42 |
| CHEMBL4868583 | — | — | 1 | 7.00 |
| CHEMBL4874867 | — | — | 1 | 6.87 |
| CHEMBL4861549 | — | — | 1 | 6.83 |
| CHEMBL4851909 | — | — | 1 | 6.64 |
| CHEMBL4868267 | — | — | 1 | 6.40 |
| CHEMBL4848851 | — | — | 1 | 6.40 |
| CHEMBL4875350 | — | — | 1 | 6.24 |
| CHEMBL4862937 | — | — | 1 | 6.19 |
| CHEMBL4850202 | — | — | 1 | 6.15 |
| CHEMBL4854785 | — | — | 1 | 6.15 |
| CHEMBL4854127 | — | — | 1 | 6.00 |
| CHEMBL4845951 | — | — | 1 | 5.99 |
| CHEMBL4867482 | — | — | 1 | 5.91 |
| CHEMBL4848716 | — | — | 1 | 5.54 |
| CHEMBL4876796 | — | — | 1 | 4.81 |
| CHEMBL4849589 | — | — | 1 | 4.65 |
| CHEMBL4850991 | — | — | 1 | 4.56 |
| CHEMBL1622853 | — | — | 1 | - |
| CHEMBL4873539 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL4847070 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4847782 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4868429 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4872758 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4847070 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4867028 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4846073 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5189739 | BEROTRALSTAT | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4847070 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4854896 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4852994 | — | IC50 | = | 37.6 | nM | 7.42 |
| CHEMBL4868583 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4874867 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4861549 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4851909 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4848851 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4868267 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL4875350 | — | IC50 | = | 577.0 | nM | 6.24 |
| CHEMBL4862937 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL4850202 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4854785 | — | IC50 | = | 708.0 | nM | 6.15 |
| CHEMBL4854127 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4845951 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4867482 | — | IC50 | = | 1229.0 | nM | 5.91 |
| CHEMBL4848716 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4876796 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL4849589 | — | IC50 | = | 22600.0 | nM | 4.65 |
| CHEMBL4850991 | — | IC50 | = | 27300.0 | nM | 4.56 |
| CHEMBL4873539 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL1622853 | — | IC50 | = | 3400000.0 | nM | - |