Assay Detail
Binding
CHEMBL898943
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Inhibition of human gamma secretase assessed as amyloid-beta40 peptide production in HEK293 cells by ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.47 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392113 | — | — | 1 | 10.82 |
| CHEMBL235659 | — | — | 1 | 10.70 |
| CHEMBL235869 | — | — | 1 | 10.43 |
| CHEMBL393542 | — | — | 1 | 10.05 |
| CHEMBL235648 | — | — | 1 | 8.70 |
| CHEMBL428374 | — | — | 1 | 8.52 |
| CHEMBL235216 | — | — | 1 | 8.52 |
| CHEMBL235427 | — | — | 1 | 8.51 |
| CHEMBL430169 | — | — | 1 | 8.28 |
| CHEMBL267960 | — | — | 1 | 8.24 |
| CHEMBL235226 | — | — | 1 | 8.07 |
| CHEMBL267959 | — | — | 1 | 8.06 |
| CHEMBL400637 | — | — | 1 | 7.92 |
| CHEMBL391420 | — | — | 1 | 7.66 |
| CHEMBL236083 | — | — | 1 | 7.66 |
| CHEMBL235646 | — | — | 1 | 6.21 |
| CHEMBL267226 | — | — | 1 | 5.57 |
| CHEMBL400638 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392113 | — | IC50 | = | 0.015 | nM | 10.82 |
| CHEMBL235659 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL235869 | — | IC50 | = | 0.037 | nM | 10.43 |
| CHEMBL393542 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL235648 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL428374 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL235216 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL235427 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL430169 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL267960 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL235226 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL267959 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL400637 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL391420 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL236083 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL235646 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL267226 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL400638 | — | IC50 | > | 20.0 | nM | - |