Assay Detail
Binding
CHEMBL2401298
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Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA
17
Total Activities
16
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 | 17 | 7.03 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | 2.0 | 1 | 8.82 |
| CHEMBL2396778 | — | — | 1 | 8.28 |
| CHEMBL463981 | BEGACESTAT | 2.0 | 1 | 7.98 |
| CHEMBL2396964 | — | — | 1 | 7.92 |
| CHEMBL2396959 | — | — | 1 | 7.85 |
| CHEMBL2396953 | — | — | 1 | 7.75 |
| CHEMBL2396952 | — | — | 2 | 7.44 |
| CHEMBL2396960 | — | — | 1 | 7.35 |
| CHEMBL2396963 | — | — | 1 | 7.31 |
| CHEMBL2396958 | — | — | 1 | 6.93 |
| CHEMBL2396965 | — | — | 1 | 6.90 |
| CHEMBL2396961 | — | — | 1 | 6.78 |
| CHEMBL2396966 | — | — | 1 | 6.72 |
| CHEMBL2396951 | — | — | 1 | 6.18 |
| CHEMBL2396967 | — | — | 1 | 5.55 |
| CHEMBL2396962 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2396778 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL463981 | BEGACESTAT | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL2396964 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2396959 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2396953 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2396952 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2396960 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2396963 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2396958 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL2396965 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL2396961 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL2396966 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2396951 | — | IC50 | = | 662.0 | nM | 6.18 |
| CHEMBL2396967 | — | IC50 | = | 2827.0 | nM | 5.55 |
| CHEMBL2396962 | — | IC50 | = | 6998.0 | nM | 5.16 |
| CHEMBL2396952 | — | IC50 | = | 30305.0 | nM | 4.52 |