Assay Detail
Binding
CHEMBL4137005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BACE1 (1 to 454 residues) (unknown origin) using APP derived polypeptide harboring Lys-Met/Asn-Leu mutation as substrate by FRET assay
19
Total Activities
19
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
Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.20 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3634342 | — | — | 1 | 8.14 |
| CHEMBL4161795 | — | — | 1 | 7.97 |
| CHEMBL4162197 | — | — | 1 | 7.94 |
| CHEMBL3634125 | — | — | 1 | 7.92 |
| CHEMBL4175845 | — | — | 1 | 7.74 |
| CHEMBL3261072 | — | — | 1 | 7.69 |
| CHEMBL4165225 | — | — | 1 | 7.65 |
| CHEMBL4167487 | — | — | 1 | 7.61 |
| CHEMBL4169060 | — | — | 1 | 7.54 |
| CHEMBL4165629 | — | — | 1 | 7.53 |
| CHEMBL4174699 | — | — | 1 | 7.52 |
| CHEMBL4159574 | — | — | 1 | 7.39 |
| CHEMBL4173236 | — | — | 1 | 6.89 |
| CHEMBL4170106 | — | — | 1 | 6.82 |
| CHEMBL4160644 | — | — | 1 | 6.34 |
| CHEMBL4167898 | — | — | 1 | 5.73 |
| CHEMBL4175758 | — | — | 1 | 5.63 |
| CHEMBL4171250 | — | — | 1 | 5.52 |
| CHEMBL4164046 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3634342 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4161795 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL4162197 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL3634125 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4175845 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL3261072 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL4165225 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL4167487 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL4169060 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL4165629 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4174699 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4159574 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL4173236 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4170106 | — | IC50 | = | 151.4 | nM | 6.82 |
| CHEMBL4160644 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL4167898 | — | IC50 | = | 1862.0 | nM | 5.73 |
| CHEMBL4175758 | — | IC50 | = | 2344.0 | nM | 5.63 |
| CHEMBL4171250 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4164046 | — | IC50 | > | 10000.0 | nM | - |