Assay Detail
Binding
CHEMBL4667905
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Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells cotransfected with Notch1-VP16-GAL4 fusion and Gal4 luciferase reporter plasmid incubated for 24 hrs by luciferase reporter gene assay luminescence assay
13
Total Activities
13
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
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.47 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4759048 | — | — | 1 | 5.89 |
| CHEMBL4753654 | — | — | 1 | 5.75 |
| CHEMBL4792187 | — | — | 1 | 5.68 |
| CHEMBL4789381 | — | — | 1 | 5.47 |
| CHEMBL4762492 | — | — | 1 | 5.43 |
| CHEMBL4759943 | — | — | 1 | 5.43 |
| CHEMBL4762370 | — | — | 1 | 5.32 |
| CHEMBL4740837 | — | — | 1 | 5.29 |
| CHEMBL4747630 | — | — | 1 | 5.23 |
| CHEMBL4753079 | — | — | 1 | 5.19 |
| CHEMBL4798232 | — | — | 1 | - |
| CHEMBL4741014 | — | — | 1 | - |
| CHEMBL4785324 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4759048 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4753654 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4792187 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4789381 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4762492 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4759943 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4762370 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4740837 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4747630 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4753079 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4798232 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4741014 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4785324 | — | IC50 | > | 10000.0 | nM | - |