Assay Detail
Binding
CHEMBL1010576
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Inhibition of human recombinant Arg235 region of BACE1 by FRET assay
10
Total Activities
10
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
Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.47 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL453211 | — | — | 1 | 8.05 |
| CHEMBL507541 | — | — | 1 | 8.00 |
| CHEMBL501242 | — | — | 1 | 7.89 |
| CHEMBL445281 | — | — | 1 | 7.82 |
| CHEMBL448015 | — | — | 1 | 7.66 |
| CHEMBL504917 | — | — | 1 | 7.62 |
| CHEMBL400043 | — | — | 1 | 7.30 |
| CHEMBL399840 | — | — | 1 | 7.02 |
| CHEMBL399839 | — | — | 1 | 6.85 |
| CHEMBL253865 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL453211 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL507541 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL501242 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL445281 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL448015 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL504917 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL400043 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL399840 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL399839 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL253865 | — | IC50 | = | 360.0 | nM | 6.44 |