Assay Detail
Binding
CHEMBL1772294
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma-secretase in human HeLa cells assessed as inhibition of amyloid beta (1 to 40) production by DELFIA-based immunoassay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.07 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770910 | — | — | 1 | 8.39 |
| CHEMBL1770907 | — | — | 1 | 8.05 |
| CHEMBL1770909 | — | — | 1 | 7.71 |
| CHEMBL1770908 | — | — | 1 | 7.51 |
| CHEMBL1770905 | — | — | 1 | 7.07 |
| CHEMBL1770906 | — | — | 1 | 7.03 |
| CHEMBL1770904 | — | — | 1 | 6.83 |
| CHEMBL1770902 | — | — | 1 | 6.60 |
| CHEMBL1770903 | — | — | 1 | 6.30 |
| CHEMBL1770901 | — | — | 1 | 5.21 |
| CHEMBL1770900 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770910 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1770907 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL1770909 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL1770908 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1770905 | — | IC50 | = | 85.7 | nM | 7.07 |
| CHEMBL1770906 | — | IC50 | = | 93.3 | nM | 7.03 |
| CHEMBL1770904 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL1770902 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1770903 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL1770901 | — | IC50 | = | 6120.0 | nM | 5.21 |
| CHEMBL1770900 | — | IC50 | > | 10000.0 | nM | - |