Assay Detail
Binding
CHEMBL5041725
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BACE1 (1 to 454 residues) (unknown origin) using APP harboring Swedish Lys/Met mutant-derived peptide as substrate by FRET assay
14
Total Activities
14
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
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.37 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5093303 | — | — | 1 | 8.85 |
| CHEMBL5084378 | — | — | 1 | 8.77 |
| CHEMBL5082406 | — | — | 1 | 8.64 |
| CHEMBL5075933 | — | — | 1 | 8.59 |
| CHEMBL5085412 | — | — | 1 | 8.55 |
| CHEMBL5074068 | — | — | 1 | 8.54 |
| CHEMBL2152899 | — | — | 1 | 8.43 |
| CHEMBL5077699 | — | — | 1 | 8.43 |
| CHEMBL5093195 | — | — | 1 | 8.35 |
| CHEMBL4521954 | — | — | 1 | 8.34 |
| CHEMBL5073381 | — | — | 1 | 8.26 |
| CHEMBL5088449 | — | — | 1 | 7.94 |
| CHEMBL5085521 | — | — | 1 | 7.89 |
| CHEMBL4525199 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5093303 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5084378 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5082406 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5075933 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5085412 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5074068 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2152899 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5077699 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5093195 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4521954 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5073381 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5088449 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5085521 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4525199 | — | IC50 | = | 28.8 | nM | 7.54 |