Assay Detail
ADMET
CHEMBL4343422
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Inhibition of recombinant human BACE2 expressed in HEK293 cells co-transfected with N-terminal HA-tagged/C-terminal Myc tagged Mbeta chain of human PMEL17 measured after overnight incubation by Gaussia luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.46 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4564735 | — | — | 1 | 7.25 |
| CHEMBL4560579 | — | — | 1 | 6.25 |
| CHEMBL4577527 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4564735 | — | IC50 | = | 55.7 | nM | 7.25 |
| CHEMBL4560579 | — | IC50 | = | 569.0 | nM | 6.25 |
| CHEMBL4577527 | — | IC50 | = | 1290.0 | nM | 5.89 |