Assay Detail
Binding
CHEMBL2401297
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Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 7 — Homologous single protein target |
| 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 | 21 | 8.46 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | 2.0 | 1 | 9.89 |
| CHEMBL2396959 | — | — | 1 | 9.66 |
| CHEMBL2396964 | — | — | 1 | 9.52 |
| CHEMBL2396778 | — | — | 1 | 9.47 |
| CHEMBL2396952 | — | — | 2 | 9.40 |
| CHEMBL2396953 | — | — | 1 | 9.40 |
| CHEMBL2396960 | — | — | 1 | 9.24 |
| CHEMBL2396963 | — | — | 1 | 9.00 |
| CHEMBL2396965 | — | — | 1 | 8.96 |
| CHEMBL463981 | BEGACESTAT | 2.0 | 1 | 8.80 |
| CHEMBL2396961 | — | — | 1 | 8.73 |
| CHEMBL2396958 | — | — | 1 | 8.72 |
| CHEMBL2396966 | — | — | 1 | 8.34 |
| CHEMBL2396951 | — | — | 1 | 8.08 |
| CHEMBL2396972 | — | — | 1 | 8.03 |
| CHEMBL1837042 | — | — | 1 | 7.85 |
| CHEMBL2396971 | — | — | 1 | 7.33 |
| CHEMBL2396967 | — | — | 1 | 7.21 |
| CHEMBL2396962 | — | — | 1 | 6.91 |
| CHEMBL2396970 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL2396959 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL2396964 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2396778 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL2396952 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2396953 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2396960 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL2396963 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2396965 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL463981 | BEGACESTAT | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2396961 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL2396958 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2396966 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2396951 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2396972 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1837042 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2396971 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2396967 | — | IC50 | = | 60.9 | nM | 7.21 |
| CHEMBL2396962 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2396970 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL2396952 | — | IC50 | = | 674.0 | nM | 6.17 |