Assay Detail
Binding
CHEMBL940882
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Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | H4 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 5.08 | 5.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL62136 | T091317 | — | 1 | 5.44 |
| CHEMBL249201 | — | — | 1 | 5.21 |
| CHEMBL248802 | — | — | 1 | 4.97 |
| CHEMBL248597 | — | — | 1 | 4.70 |
| CHEMBL248605 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL62136 | T091317 | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL249201 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL248802 | — | EC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL248597 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL248605 | — | EC50 | > | 20000.0 | nM | - |