Assay Detail
Binding
CHEMBL5031862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] JNJ-962 from BACE2 (unknown origin) expressed in HEK293 cell membranes assessed as inhibition constant at pH 6.2 by scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.16 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4557670 | — | — | 1 | 9.92 |
| CHEMBL5075689 | — | — | 1 | 8.02 |
| CHEMBL3301601 | VERUBECESTAT | 3.0 | 1 | 7.96 |
| CHEMBL3916243 | ATABECESTAT | 2.0 | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4557670 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL5075689 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL3301601 | VERUBECESTAT | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL3916243 | ATABECESTAT | Ki | = | 185.0 | nM | 6.73 |