Assay Detail
Binding
CHEMBL2401295
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Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetulus griseus |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.10 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | 2.0 | 1 | 7.15 |
| CHEMBL2396778 | — | — | 1 | 7.09 |
| CHEMBL2396959 | — | — | 1 | 6.95 |
| CHEMBL2396953 | — | — | 1 | 6.84 |
| CHEMBL2396964 | — | — | 1 | 6.80 |
| CHEMBL2396952 | — | — | 2 | 6.60 |
| CHEMBL2396960 | — | — | 1 | 6.57 |
| CHEMBL463981 | BEGACESTAT | 2.0 | 1 | 6.45 |
| CHEMBL2396954 | — | — | 1 | 6.33 |
| CHEMBL2396963 | — | — | 1 | 6.28 |
| CHEMBL2396958 | — | — | 1 | 6.22 |
| CHEMBL2396957 | — | — | 1 | 6.01 |
| CHEMBL2396965 | — | — | 1 | 5.96 |
| CHEMBL2396961 | — | — | 1 | 5.74 |
| CHEMBL2396956 | — | — | 1 | 5.47 |
| CHEMBL2396955 | — | — | 1 | 5.39 |
| CHEMBL2396966 | — | — | 1 | 5.25 |
| CHEMBL2396969 | — | — | 1 | 5.09 |
| CHEMBL1837042 | — | — | 1 | 4.96 |
| CHEMBL2396951 | — | — | 1 | 4.94 |
| CHEMBL2396962 | — | — | 1 | - |
| CHEMBL2396967 | — | — | 1 | - |
| CHEMBL2396968 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2396778 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2396959 | — | IC50 | = | 113.33 | nM | 6.95 |
| CHEMBL2396953 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL2396964 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2396952 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2396960 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL463981 | BEGACESTAT | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL2396954 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL2396963 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL2396958 | — | IC50 | = | 595.0 | nM | 6.22 |
| CHEMBL2396957 | — | IC50 | = | 971.0 | nM | 6.01 |
| CHEMBL2396965 | — | IC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL2396961 | — | IC50 | = | 1831.0 | nM | 5.74 |
| CHEMBL2396956 | — | IC50 | = | 3346.0 | nM | 5.47 |
| CHEMBL2396955 | — | IC50 | = | 4101.0 | nM | 5.39 |
| CHEMBL2396966 | — | IC50 | = | 5621.0 | nM | 5.25 |
| CHEMBL2396969 | — | IC50 | = | 8043.0 | nM | 5.09 |
| CHEMBL1837042 | — | IC50 | = | 10932.0 | nM | 4.96 |
| CHEMBL2396951 | — | IC50 | = | 11397.0 | nM | 4.94 |
| CHEMBL2396962 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL2396967 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL2396968 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL2396952 | — | IC50 | > | 400000.0 | nM | - |