Assay Detail
Binding
CHEMBL940880
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Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay
10
Total Activities
10
Compounds Tested
2
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 |
|---|---|---|---|
| IC50 | 9 | 4.72 | 4.72 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392028 | — | — | 1 | 4.72 |
| CHEMBL247693 | — | — | 1 | - |
| CHEMBL249202 | — | — | 1 | - |
| CHEMBL249201 | — | — | 1 | - |
| CHEMBL248802 | — | — | 1 | - |
| CHEMBL62136 | T091317 | — | 1 | - |
| CHEMBL385554 | — | — | 1 | - |
| CHEMBL248605 | — | — | 1 | - |
| CHEMBL248597 | — | — | 1 | - |
| CHEMBL218756 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392028 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL247693 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL249202 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL249201 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL248802 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL62136 | T091317 | IC50 | > | 40000.0 | nM | - |
| CHEMBL385554 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL248605 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL248597 | — | Activity | - | — | - | |
| CHEMBL218756 | — | IC50 | > | 40000.0 | nM | - |