Assay Detail
Binding
CHEMBL4122270
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of doxycycline induced Hepsin in human MCF10A cells using Boc-QRR-AMC as substrate preincubated for 24 hrs followed by doxycycline induction for 24 hrs and subsequent addition of substrate by fluorescence assay
5
Total Activities
5
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
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 | 5 | 5.92 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129836 | — | — | 1 | 7.00 |
| CHEMBL4130135 | — | — | 1 | 6.00 |
| CHEMBL4128554 | — | — | 1 | 5.89 |
| CHEMBL4127452 | — | — | 1 | 5.50 |
| CHEMBL4129630 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129836 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4130135 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4128554 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4127452 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4129630 | — | IC50 | = | 6490.0 | nM | 5.19 |