Assay Detail
Binding
CHEMBL998512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma-secretase expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.52 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL463981 | BEGACESTAT | 2.0 | 1 | 7.82 |
| CHEMBL458753 | — | — | 1 | 7.80 |
| CHEMBL480558 | GSI-136 | 1.0 | 1 | 7.60 |
| CHEMBL472151 | — | — | 1 | 6.53 |
| CHEMBL452797 | — | — | 1 | 6.53 |
| CHEMBL499573 | — | — | 1 | 5.66 |
| CHEMBL488228 | — | — | 1 | 5.26 |
| CHEMBL443344 | — | — | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL463981 | BEGACESTAT | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL458753 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL480558 | GSI-136 | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL472151 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL452797 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL499573 | — | IC50 | = | 2214.0 | nM | 5.66 |
| CHEMBL488228 | — | IC50 | = | 5449.0 | nM | 5.26 |
| CHEMBL443344 | — | IC50 | = | 10670.0 | nM | 4.97 |