Assay Detail
Binding
CHEMBL832831
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Inhibitory activity against beta-secretase 1 (BACE1)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.94 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183546 | — | — | 1 | 8.41 |
| CHEMBL181826 | — | — | 1 | 8.33 |
| CHEMBL183494 | — | — | 1 | 8.09 |
| CHEMBL367139 | — | — | 1 | 7.80 |
| CHEMBL183059 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183546 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL181826 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL183494 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL367139 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL183059 | — | IC50 | = | 84.0 | nM | 7.08 |