Assay Detail
Binding
CHEMBL2160914
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Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.87 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159511 | — | — | 1 | 8.40 |
| CHEMBL2159510 | — | — | 1 | 8.30 |
| CHEMBL2159509 | — | — | 2 | 8.10 |
| CHEMBL2159689 | — | — | 1 | 8.10 |
| CHEMBL2159687 | — | — | 1 | 7.75 |
| CHEMBL2159691 | — | — | 1 | 7.43 |
| CHEMBL2159690 | — | — | 1 | 7.32 |
| CHEMBL2159686 | — | — | 1 | - |
| CHEMBL2159688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159511 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2159510 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2159509 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2159689 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2159687 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2159509 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2159691 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2159690 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2159686 | — | IC50 | - | — | - | |
| CHEMBL2159688 | — | IC50 | - | — | - |