Assay Detail
Binding
CHEMBL2320840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.99 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2314606 | — | — | 1 | 8.92 |
| CHEMBL2314603 | — | — | 1 | 8.82 |
| CHEMBL2314617 | — | — | 1 | 8.60 |
| CHEMBL2159511 | — | — | 1 | 8.40 |
| CHEMBL2159510 | — | — | 1 | 8.30 |
| CHEMBL2159509 | — | — | 1 | 8.10 |
| CHEMBL2314602 | — | — | 1 | 8.05 |
| CHEMBL2314610 | — | — | 1 | 7.96 |
| CHEMBL2314618 | — | — | 1 | 7.96 |
| CHEMBL2314601 | — | — | 1 | 7.89 |
| CHEMBL2314608 | — | — | 1 | 7.89 |
| CHEMBL2314613 | — | — | 1 | 7.85 |
| CHEMBL2314607 | — | — | 1 | 7.66 |
| CHEMBL2314616 | — | — | 1 | 7.60 |
| CHEMBL2314604 | — | — | 1 | 7.42 |
| CHEMBL2314612 | — | — | 1 | 6.40 |
| CHEMBL2314609 | — | — | 1 | - |
| CHEMBL2314605 | — | — | 1 | - |
| CHEMBL2314611 | — | — | 1 | - |
| CHEMBL2314614 | — | — | 1 | - |
| CHEMBL2314615 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2314606 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2314603 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2314617 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2159511 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2159510 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2159509 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2314602 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2314610 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2314618 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2314601 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2314608 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2314613 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2314607 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2314616 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2314604 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2314612 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2314609 | — | IC50 | - | — | - | |
| CHEMBL2314605 | — | IC50 | - | — | - | |
| CHEMBL2314611 | — | IC50 | - | — | - | |
| CHEMBL2314614 | — | IC50 | - | — | - | |
| CHEMBL2314615 | — | IC50 | - | — | - |