Assay Detail
Binding
CHEMBL4619095
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of gamma secretase in human H4 cells overexpressing human APP695 harboring K595N/M596L Swedish double mutant assessed as reduction in total amyloid beta (1 to 42 residues) production measured after 24 hrs by AlphaLISA assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.56 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4645821 | — | — | 1 | 8.05 |
| CHEMBL4525398 | — | — | 1 | 7.96 |
| CHEMBL4634277 | — | — | 1 | 7.85 |
| CHEMBL4646084 | — | — | 1 | 7.85 |
| CHEMBL4634813 | — | — | 1 | 7.85 |
| CHEMBL4649661 | — | — | 1 | 7.85 |
| CHEMBL4635678 | — | — | 1 | 7.82 |
| CHEMBL4638029 | — | — | 1 | 7.82 |
| CHEMBL4638559 | — | — | 1 | 7.80 |
| CHEMBL4636270 | — | — | 1 | 7.72 |
| CHEMBL4647270 | — | — | 1 | 7.72 |
| CHEMBL4645645 | — | — | 1 | 7.64 |
| CHEMBL4638982 | — | — | 1 | 7.64 |
| CHEMBL4644229 | — | — | 1 | 7.60 |
| CHEMBL4644454 | — | — | 1 | 7.60 |
| CHEMBL4646041 | — | — | 1 | 7.58 |
| CHEMBL4647524 | — | — | 1 | 7.54 |
| CHEMBL4633835 | — | — | 1 | 7.52 |
| CHEMBL4637328 | — | — | 1 | 7.52 |
| CHEMBL4633563 | — | — | 1 | 7.51 |
| CHEMBL4635797 | — | — | 1 | 7.51 |
| CHEMBL4634104 | — | — | 1 | 7.50 |
| CHEMBL4643195 | — | — | 1 | 7.47 |
| CHEMBL4645134 | — | — | 1 | 7.41 |
| CHEMBL4634876 | — | — | 1 | 7.40 |
| CHEMBL4648911 | — | — | 1 | 7.36 |
| CHEMBL4649500 | — | — | 1 | 7.36 |
| CHEMBL4632791 | — | — | 1 | 7.31 |
| CHEMBL4646136 | — | — | 1 | 7.06 |
| CHEMBL4634397 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4645821 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4525398 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4634277 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4646084 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4634813 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4649661 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4635678 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4638029 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4638559 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4636270 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4647270 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4645645 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4638982 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4644229 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4644454 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4646041 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4647524 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4633835 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4637328 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4633563 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4635797 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4634104 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4643195 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4645134 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4634876 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4648911 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4649500 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4632791 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4646136 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4634397 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4636263 | — | IC50 | = | 237.0 | nM | 6.62 |