Assay Detail
Binding
CHEMBL1827653
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Inhibition of human recombinant BACE1 after 60 mins by FRET assay
23
Total Activities
23
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
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 | 23 | 7.58 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1821820 | — | — | 1 | 9.19 |
| CHEMBL1821728 | — | — | 1 | 9.15 |
| CHEMBL1821815 | — | — | 1 | 8.60 |
| CHEMBL1821814 | — | — | 1 | 8.43 |
| CHEMBL1821825 | — | — | 1 | 8.00 |
| CHEMBL1821827 | — | — | 1 | 7.96 |
| CHEMBL1821819 | — | — | 1 | 7.96 |
| CHEMBL1821830 | — | — | 1 | 7.82 |
| CHEMBL1821817 | — | — | 1 | 7.80 |
| CHEMBL1821826 | — | — | 1 | 7.80 |
| CHEMBL1821821 | — | — | 1 | 7.70 |
| CHEMBL1821818 | — | — | 1 | 7.57 |
| CHEMBL1821823 | — | — | 1 | 7.51 |
| CHEMBL1821812 | — | — | 1 | 7.47 |
| CHEMBL1821824 | — | — | 1 | 7.30 |
| CHEMBL1821811 | — | — | 1 | 7.13 |
| CHEMBL1821822 | — | — | 1 | 7.06 |
| CHEMBL1821828 | — | — | 1 | 7.01 |
| CHEMBL1821829 | — | — | 1 | 6.41 |
| CHEMBL1821816 | — | — | 1 | 6.01 |
| CHEMBL1821810 | — | — | 1 | 5.28 |
| CHEMBL1821813 | — | — | 1 | - |
| CHEMBL1821809 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1821820 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL1821728 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1821815 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1821814 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1821825 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1821827 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1821819 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1821830 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1821817 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1821826 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1821821 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1821818 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1821823 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1821812 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1821824 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1821811 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1821822 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1821828 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1821829 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1821816 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1821810 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL1821813 | — | IC50 | - | — | - | |
| CHEMBL1821809 | — | IC50 | - | — | - |