Assay Detail
Binding
CHEMBL4122265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by manual fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.71 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129836 | — | — | 1 | 7.66 |
| CHEMBL4130135 | — | — | 1 | 7.42 |
| CHEMBL4128554 | — | — | 1 | 6.72 |
| CHEMBL4127165 | — | — | 1 | 6.66 |
| CHEMBL4128355 | — | — | 1 | 6.60 |
| CHEMBL4128356 | — | — | 1 | 6.48 |
| CHEMBL4127452 | — | — | 1 | 6.07 |
| CHEMBL4128512 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129836 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4130135 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4128554 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4127165 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4128355 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4128356 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4127452 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4128512 | — | IC50 | = | 870.0 | nM | 6.06 |