Assay Detail
Binding
CHEMBL896440
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Inhibition of gamma secretase in APP-transfected CHO cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.64 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232938 | — | — | 1 | 8.38 |
| CHEMBL232182 | — | — | 1 | 8.24 |
| CHEMBL232936 | — | — | 1 | 8.21 |
| CHEMBL399204 | — | — | 1 | 8.17 |
| CHEMBL392265 | — | — | 1 | 7.96 |
| CHEMBL429438 | — | — | 1 | 7.90 |
| CHEMBL232346 | — | — | 1 | 7.89 |
| CHEMBL231941 | — | — | 1 | 7.85 |
| CHEMBL232138 | — | — | 1 | 7.82 |
| CHEMBL232739 | — | — | 1 | 7.82 |
| CHEMBL393520 | — | — | 1 | 7.72 |
| CHEMBL232183 | — | — | 1 | 7.71 |
| CHEMBL231984 | — | — | 1 | 7.70 |
| CHEMBL450279 | — | — | 1 | 7.68 |
| CHEMBL449960 | — | — | 1 | 7.68 |
| CHEMBL401045 | — | — | 1 | 7.58 |
| CHEMBL401044 | — | — | 1 | 7.55 |
| CHEMBL399819 | — | — | 1 | 7.09 |
| CHEMBL233172 | — | — | 1 | 7.02 |
| CHEMBL231725 | — | — | 1 | 6.94 |
| CHEMBL273493 | — | — | 1 | 6.55 |
| CHEMBL232367 | — | — | 1 | 6.55 |
| CHEMBL398379 | — | — | 1 | - |
| CHEMBL401434 | — | — | 1 | - |
| CHEMBL232968 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232938 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL232182 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL232936 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL399204 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL392265 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL429438 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL232346 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL231941 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL232138 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL232739 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL393520 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL232183 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL231984 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL450279 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL449960 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL401045 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL401044 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL399819 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL233172 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL231725 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL273493 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL232367 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL398379 | — | IC50 | - | — | - | |
| CHEMBL401434 | — | IC50 | - | — | - | |
| CHEMBL232968 | — | IC50 | - | — | - |