Assay Detail
Binding
CHEMBL4343402
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Inhibition of BACE1 (unknown origin) using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET assay
22
Total Activities
22
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
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 | 22 | 8.91 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4577527 | — | — | 1 | 9.70 |
| CHEMBL4437161 | — | — | 1 | 9.70 |
| CHEMBL4472708 | — | — | 1 | 9.52 |
| CHEMBL4560579 | — | — | 1 | 9.40 |
| CHEMBL4475533 | — | — | 1 | 9.40 |
| CHEMBL4473740 | — | — | 1 | 9.40 |
| CHEMBL4468455 | — | — | 1 | 9.22 |
| CHEMBL4456778 | — | — | 1 | 9.15 |
| CHEMBL4579155 | — | — | 1 | 9.10 |
| CHEMBL4575413 | — | — | 1 | 8.96 |
| CHEMBL4457316 | — | — | 1 | 8.96 |
| CHEMBL4459222 | — | — | 1 | 8.92 |
| CHEMBL4539909 | — | — | 1 | 8.89 |
| CHEMBL4452318 | — | — | 1 | 8.74 |
| CHEMBL4471141 | — | — | 1 | 8.72 |
| CHEMBL4456863 | — | — | 1 | 8.68 |
| CHEMBL4575752 | — | — | 1 | 8.62 |
| CHEMBL4564735 | — | — | 1 | 8.52 |
| CHEMBL4593414 | — | — | 1 | 8.38 |
| CHEMBL4461994 | — | — | 1 | 8.21 |
| CHEMBL4460278 | — | — | 1 | 7.92 |
| CHEMBL4544525 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4577527 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4437161 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4472708 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4560579 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4475533 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4473740 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4468455 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4456778 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4579155 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4575413 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4457316 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4459222 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4539909 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4452318 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4471141 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4456863 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4575752 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4564735 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4593414 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4461994 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4460278 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4544525 | — | IC50 | = | 16.0 | nM | 7.80 |