Assay Detail
Functional
CHEMBL4323074
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vivo inhibition of BACE1 in po dosed Beagle dog assessed as unbound plasma level causing 50% reduction in amyloidbeta42 level in CSF administered as single dose measured after 4 to 49 hrs
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Canis lupus familiaris |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 8.26 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4557670 | — | — | 1 | 8.74 |
| CHEMBL4204869 | ELENBECESTAT | 3.0 | 1 | 8.09 |
| CHEMBL3301601 | VERUBECESTAT | 3.0 | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4557670 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4204869 | ELENBECESTAT | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3301601 | VERUBECESTAT | EC50 | = | 11.0 | nM | 7.96 |