Assay Detail
Binding
CHEMBL1772295
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma-secretase in human H4 cells expressing APP Swedish mutant assessed as inhibition of amyloid beta (1 to 40) production by whole cell assay
18
Total Activities
18
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
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 | 18 | 7.49 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1770916 | NIROGACESTAT | 4.0 | 1 | 8.92 |
| CHEMBL1770911 | — | — | 1 | 8.54 |
| CHEMBL1770912 | — | — | 1 | 8.48 |
| CHEMBL1770914 | — | — | 1 | 8.34 |
| CHEMBL1770917 | — | — | 1 | 8.31 |
| CHEMBL1770910 | — | — | 1 | 8.27 |
| CHEMBL1770915 | — | — | 1 | 8.16 |
| CHEMBL1770907 | — | — | 1 | 7.91 |
| CHEMBL1770913 | — | — | 1 | 7.71 |
| CHEMBL1770909 | — | — | 1 | 7.71 |
| CHEMBL1770908 | — | — | 1 | 7.33 |
| CHEMBL1770905 | — | — | 1 | 7.27 |
| CHEMBL1770906 | — | — | 1 | 6.81 |
| CHEMBL1770904 | — | — | 1 | 6.57 |
| CHEMBL1770901 | — | — | 1 | 6.51 |
| CHEMBL1770903 | — | — | 1 | 6.32 |
| CHEMBL1770902 | — | — | 1 | 6.12 |
| CHEMBL1770900 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1770916 | NIROGACESTAT | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1770911 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1770912 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1770914 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1770917 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1770910 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1770915 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1770907 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL1770913 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL1770909 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL1770908 | — | IC50 | = | 46.8 | nM | 7.33 |
| CHEMBL1770905 | — | IC50 | = | 53.9 | nM | 7.27 |
| CHEMBL1770906 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1770904 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL1770901 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1770903 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1770902 | — | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL1770900 | — | IC50 | = | 3100.0 | nM | 5.51 |