Assay Detail
Binding
CHEMBL4844499
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of purified human plasma kallikrein assessed as inhibition constant using H-D-Pro-Phe-Arg-pNA.2HCl as substrate measured after 3 mins by microplate reader analysis
2
Total Activities
2
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 |
|---|---|---|---|
| Ki | 2 | 9.48 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297502 | AVORALSTAT | 3.0 | 1 | 9.59 |
| CHEMBL5189739 | BEROTRALSTAT | 4.0 | 1 | 9.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297502 | AVORALSTAT | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL5189739 | BEROTRALSTAT | Ki | = | 0.44 | nM | 9.36 |