Assay Detail
Binding
CHEMBL896441
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Displacement of [3H]succinamide from gamma secretase in THP1 cell membranes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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 |
|---|---|---|---|
| Ki | 26 | 8.15 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232938 | — | — | 1 | 9.05 |
| CHEMBL399204 | — | — | 1 | 8.96 |
| CHEMBL401044 | — | — | 1 | 8.92 |
| CHEMBL450279 | — | — | 1 | 8.89 |
| CHEMBL232182 | — | — | 1 | 8.85 |
| CHEMBL429438 | — | — | 1 | 8.70 |
| CHEMBL232936 | — | — | 1 | 8.68 |
| CHEMBL232346 | — | — | 1 | 8.66 |
| CHEMBL429441 | — | — | 1 | 8.59 |
| CHEMBL401045 | — | — | 1 | 8.52 |
| CHEMBL392265 | — | — | 1 | 8.51 |
| CHEMBL449960 | — | — | 1 | 8.46 |
| CHEMBL232739 | — | — | 1 | 8.41 |
| CHEMBL232138 | — | — | 1 | 8.40 |
| CHEMBL231941 | — | — | 1 | 8.31 |
| CHEMBL232183 | — | — | 1 | 8.21 |
| CHEMBL233172 | — | — | 1 | 8.00 |
| CHEMBL231984 | — | — | 1 | 7.96 |
| CHEMBL231725 | — | — | 1 | 7.87 |
| CHEMBL399819 | — | — | 1 | 7.82 |
| CHEMBL232367 | — | — | 1 | 7.66 |
| CHEMBL232968 | — | — | 1 | 7.44 |
| CHEMBL393520 | — | — | 1 | 7.39 |
| CHEMBL273493 | — | — | 1 | 6.96 |
| CHEMBL398379 | — | — | 1 | 6.64 |
| CHEMBL401434 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232938 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL399204 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL401044 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL450279 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL232182 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL429438 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL232936 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL232346 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL429441 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL401045 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL392265 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL449960 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL232739 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL232138 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL231941 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL232183 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL233172 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL231984 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL231725 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL399819 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL232367 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL232968 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL393520 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL273493 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL398379 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL401434 | — | Ki | = | 1000.0 | nM | 6.00 |