Assay Detail
Binding
CHEMBL3635178
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Inhibition of BACE1 in human SKNBE2 cells expressing wild type human APP695 assessed as reduction in amyloid beta-42 production after 18 hrs by sandwich alphalisa assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SKNBE2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.53 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3634341 | — | — | 1 | 8.48 |
| CHEMBL2403769 | — | — | 1 | 8.39 |
| CHEMBL3634340 | — | — | 1 | 8.28 |
| CHEMBL3634123 | — | — | 1 | 8.27 |
| CHEMBL3634342 | — | — | 1 | 8.09 |
| CHEMBL3634122 | — | — | 1 | 8.04 |
| CHEMBL3634125 | — | — | 1 | 8.04 |
| CHEMBL3634128 | — | — | 1 | 7.89 |
| CHEMBL3634129 | — | — | 1 | 7.85 |
| CHEMBL3634126 | — | — | 1 | 7.47 |
| CHEMBL3634124 | — | — | 1 | 7.03 |
| CHEMBL3634338 | — | — | 1 | 6.59 |
| CHEMBL3634127 | — | — | 1 | 6.49 |
| CHEMBL3634130 | — | — | 1 | 6.22 |
| CHEMBL3634339 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3634341 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2403769 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3634340 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3634123 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3634342 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3634122 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3634125 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3634128 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3634129 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3634126 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3634124 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3634338 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3634127 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL3634130 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL3634339 | — | IC50 | = | 1445.0 | nM | 5.84 |