Assay Detail
Binding
CHEMBL2187563
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Inhibition of BACE1-mediated amyloid beta 40 release in C57/BL6 mouse primary cortical neurons after overnight incubation by ELISA
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | Cerebral cortex neuron |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.42 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152903 | — | — | 1 | 8.59 |
| CHEMBL2177304 | — | — | 1 | 8.47 |
| CHEMBL2177919 | — | — | 1 | 7.52 |
| CHEMBL2177917 | — | — | 1 | 7.40 |
| CHEMBL2177913 | AZD-3839 | 1.0 | 1 | 7.29 |
| CHEMBL2177914 | — | — | 1 | 7.28 |
| CHEMBL2177904 | — | — | 1 | 7.17 |
| CHEMBL2177909 | — | — | 1 | 6.69 |
| CHEMBL2177906 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152903 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2177304 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2177919 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2177917 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2177913 | AZD-3839 | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2177914 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2177904 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2177909 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL2177906 | — | IC50 | = | 436.0 | nM | 6.36 |