Assay Detail
Binding
CHEMBL4038128
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Sprague-Dawley rat plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.48 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075544 | — | — | 1 | 9.40 |
| CHEMBL4079711 | — | — | 1 | 9.05 |
| CHEMBL4093698 | — | — | 1 | 8.70 |
| CHEMBL4059991 | — | — | 1 | 8.47 |
| CHEMBL4070056 | — | — | 1 | 8.26 |
| CHEMBL4079260 | — | — | 1 | 7.96 |
| CHEMBL4094403 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075544 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4079711 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4093698 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4059991 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4070056 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4079260 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4094403 | — | Ki | = | 30.0 | nM | 7.52 |