Assay Detail
Binding
CHEMBL898939
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Inhibition of human gamma secretase in HEK293 cells by reporter gene assay
19
Total Activities
19
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 | 19 | 8.48 | 10.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235869 | — | — | 1 | 10.62 |
| CHEMBL235659 | — | — | 1 | 10.38 |
| CHEMBL392113 | — | — | 1 | 10.12 |
| CHEMBL393542 | — | — | 1 | 9.68 |
| CHEMBL235648 | — | — | 1 | 8.80 |
| CHEMBL428374 | — | — | 1 | 8.77 |
| CHEMBL235226 | — | — | 1 | 8.77 |
| CHEMBL235216 | — | — | 1 | 8.48 |
| CHEMBL267960 | — | — | 1 | 8.20 |
| CHEMBL267959 | — | — | 1 | 8.15 |
| CHEMBL235427 | — | — | 1 | 8.06 |
| CHEMBL391420 | — | — | 1 | 8.00 |
| CHEMBL400637 | — | — | 1 | 7.85 |
| CHEMBL400638 | — | — | 1 | 7.70 |
| CHEMBL235646 | — | — | 1 | 6.24 |
| CHEMBL267226 | — | — | 1 | 5.82 |
| CHEMBL430169 | — | — | 1 | - |
| CHEMBL235870 | — | — | 1 | - |
| CHEMBL236083 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235869 | — | IC50 | = | 0.024 | nM | 10.62 |
| CHEMBL235659 | — | IC50 | = | 0.042 | nM | 10.38 |
| CHEMBL392113 | — | IC50 | = | 0.075 | nM | 10.12 |
| CHEMBL393542 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL235648 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL428374 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL235226 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL235216 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL267960 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL267959 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL235427 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL391420 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL400637 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL400638 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL235646 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL267226 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL430169 | — | IC50 | > | 25.0 | nM | - |
| CHEMBL235870 | — | IC50 | = | 0.002 | nM | - |
| CHEMBL236083 | — | IC50 | > | 25.0 | nM | - |