Assay Detail
Binding
CHEMBL4137008
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Inhibition of BACE1 in human SKNBE2 cells transfected with APP695 protein assessed as reduction in amyloid beta (1 to 42) levels after 18 hrs by sandwich alphalisa 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 | 7.43 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162197 | — | — | 1 | 8.31 |
| CHEMBL4165225 | — | — | 1 | 8.22 |
| CHEMBL4169060 | — | — | 1 | 8.19 |
| CHEMBL3261072 | — | — | 1 | 8.14 |
| CHEMBL3634342 | — | — | 1 | 8.08 |
| CHEMBL4175845 | — | — | 1 | 7.91 |
| CHEMBL4159574 | — | — | 1 | 7.90 |
| CHEMBL3634125 | — | — | 1 | 7.88 |
| CHEMBL4161795 | — | — | 1 | 7.81 |
| CHEMBL4167487 | — | — | 1 | 7.68 |
| CHEMBL4165629 | — | — | 1 | 7.56 |
| CHEMBL4170106 | — | — | 1 | 7.46 |
| CHEMBL4173236 | — | — | 1 | 7.39 |
| CHEMBL4174699 | — | — | 1 | 7.31 |
| CHEMBL4160644 | — | — | 1 | 6.94 |
| CHEMBL4175758 | — | — | 1 | 6.60 |
| CHEMBL4171250 | — | — | 1 | 6.22 |
| CHEMBL4167898 | — | — | 1 | 6.20 |
| CHEMBL4164046 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162197 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4165225 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4169060 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3261072 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3634342 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4175845 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL4159574 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL3634125 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4161795 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL4167487 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL4165629 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL4170106 | — | IC50 | = | 35.1 | nM | 7.46 |
| CHEMBL4173236 | — | IC50 | = | 40.3 | nM | 7.39 |
| CHEMBL4174699 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4160644 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4175758 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4171250 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL4167898 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL4164046 | — | IC50 | = | 4500.0 | nM | 5.35 |