Assay Detail
Binding
CHEMBL1921609
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Inhibition of gamma secretase in human H4 cells overexpressing human APP assessed as reduction in amyloid beta-42 secretion after 22 hrs
32
Total Activities
32
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
Aminothiazoles as γ-secretase modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.40 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1915569 | — | — | 1 | 7.36 |
| CHEMBL1915568 | — | — | 1 | 7.28 |
| CHEMBL1915575 | — | — | 1 | 7.07 |
| CHEMBL1915571 | — | — | 1 | 6.91 |
| CHEMBL1915583 | — | — | 1 | 6.90 |
| CHEMBL1915582 | — | — | 1 | 6.88 |
| CHEMBL1915567 | — | — | 1 | 6.88 |
| CHEMBL1915562 | — | — | 1 | 6.87 |
| CHEMBL1915570 | — | — | 1 | 6.68 |
| CHEMBL1915559 | — | — | 1 | 6.67 |
| CHEMBL1915580 | — | — | 1 | 6.67 |
| CHEMBL1915578 | — | — | 1 | 6.61 |
| CHEMBL1915579 | — | — | 1 | 6.60 |
| CHEMBL1915754 | — | — | 1 | 6.50 |
| CHEMBL1915561 | — | — | 1 | 6.47 |
| CHEMBL1915755 | — | — | 1 | 6.42 |
| CHEMBL1915756 | — | — | 1 | 6.32 |
| CHEMBL1915752 | — | — | 1 | 6.19 |
| CHEMBL1915573 | — | — | 1 | 6.17 |
| CHEMBL1915572 | — | — | 1 | 6.13 |
| CHEMBL1915564 | — | — | 1 | 6.10 |
| CHEMBL1915558 | — | — | 1 | 6.09 |
| CHEMBL1915565 | — | — | 1 | 6.06 |
| CHEMBL1915566 | — | — | 1 | 6.05 |
| CHEMBL1915577 | — | — | 1 | 6.00 |
| CHEMBL1915757 | — | — | 1 | 5.54 |
| CHEMBL1915581 | — | — | 1 | 5.47 |
| CHEMBL1915576 | — | — | 1 | 5.46 |
| CHEMBL1915753 | — | — | 1 | 5.26 |
| CHEMBL1915574 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1915569 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1915568 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1915575 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1915571 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL1915583 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL1915582 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL1915567 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL1915562 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL1915570 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL1915559 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL1915580 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL1915578 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL1915579 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL1915754 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL1915561 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL1915755 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL1915756 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL1915752 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL1915573 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL1915572 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL1915564 | — | IC50 | = | 789.0 | nM | 6.10 |
| CHEMBL1915558 | — | IC50 | = | 815.0 | nM | 6.09 |
| CHEMBL1915565 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1915566 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL1915577 | — | IC50 | = | 999.0 | nM | 6.00 |
| CHEMBL1915757 | — | IC50 | = | 2868.0 | nM | 5.54 |
| CHEMBL1915581 | — | IC50 | = | 3358.0 | nM | 5.47 |
| CHEMBL1915576 | — | IC50 | = | 3431.0 | nM | 5.46 |
| CHEMBL1915753 | — | IC50 | = | 5548.0 | nM | 5.26 |
| CHEMBL1915574 | — | IC50 | > | 1250.0 | nM | - |
| CHEMBL1915563 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL1915560 | — | IC50 | > | 40000.0 | nM | - |