Assay Detail
Binding
CHEMBL4343403
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Inhibition of BACE in HEK293 cells harboring APP Swedish mutant assessed as reduction in amyloid beta 40 level measured after overnight incubation by sandwich ELISA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 21 | 8.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4472708 | — | — | 1 | 9.52 |
| CHEMBL4577527 | — | — | 1 | 9.22 |
| CHEMBL4437161 | — | — | 1 | 9.22 |
| CHEMBL4473740 | — | — | 1 | 9.15 |
| CHEMBL4468455 | — | — | 1 | 9.05 |
| CHEMBL4459222 | — | — | 1 | 8.92 |
| CHEMBL4560579 | — | — | 1 | 8.92 |
| CHEMBL4475533 | — | — | 1 | 8.89 |
| CHEMBL4575752 | — | — | 1 | 8.70 |
| CHEMBL4456863 | — | — | 1 | 8.68 |
| CHEMBL4456778 | — | — | 1 | 8.66 |
| CHEMBL4539909 | — | — | 1 | 8.62 |
| CHEMBL4579155 | — | — | 1 | 8.47 |
| CHEMBL4593414 | — | — | 1 | 8.38 |
| CHEMBL4457316 | — | — | 1 | 8.10 |
| CHEMBL4575413 | — | — | 1 | 8.08 |
| CHEMBL4460278 | — | — | 1 | 7.92 |
| CHEMBL4452318 | — | — | 1 | 7.77 |
| CHEMBL4471141 | — | — | 1 | 7.35 |
| CHEMBL4461994 | — | — | 1 | 7.28 |
| CHEMBL4544525 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4472708 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4577527 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4437161 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4473740 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4468455 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4459222 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4560579 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4475533 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4575752 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4456863 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4456778 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4539909 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4579155 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4593414 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4457316 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4575413 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4460278 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4452318 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4471141 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4461994 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4544525 | — | IC50 | = | 66.0 | nM | 7.18 |