Assay Detail
Binding
CHEMBL1827652
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Inhibition of BACE1 using 19F-labeled EVNLDAEF(CF3) as substrate after 20 mins by NMR spectrometry
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 3.31 | 3.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189197 | — | — | 1 | 3.47 |
| CHEMBL1821800 | — | — | 1 | 3.40 |
| CHEMBL1821799 | — | — | 1 | 3.34 |
| CHEMBL1821798 | — | — | 1 | 3.25 |
| CHEMBL61236 | — | — | 1 | 3.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189197 | — | IC50 | = | 338000.0 | nM | 3.47 |
| CHEMBL1821800 | — | IC50 | = | 400000.0 | nM | 3.40 |
| CHEMBL1821799 | — | IC50 | = | 460000.0 | nM | 3.34 |
| CHEMBL1821798 | — | IC50 | = | 562000.0 | nM | 3.25 |
| CHEMBL61236 | — | IC50 | = | 800000.0 | nM | 3.10 |