Assay Detail
Binding
CHEMBL1837501
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma-secretase-mediated cleavage of amyloid precursor protein in human IMR32 cells after 2 hrs using MBPC-125 substrate by ELISA assay
23
Total Activities
22
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
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.51 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL568933 | — | — | 1 | 8.70 |
| CHEMBL1837046 | — | — | 1 | 8.40 |
| CHEMBL1837047 | — | — | 1 | 8.40 |
| CHEMBL1837061 | — | — | 1 | 8.30 |
| CHEMBL1837060 | — | — | 1 | 8.15 |
| CHEMBL1837059 | — | — | 1 | 8.10 |
| CHEMBL1837048 | — | — | 1 | 8.00 |
| CHEMBL1837042 | — | — | 1 | 7.85 |
| CHEMBL1837043 | — | — | 1 | 7.80 |
| CHEMBL1837045 | — | — | 1 | 7.68 |
| CHEMBL1837049 | — | — | 1 | 7.66 |
| CHEMBL1837050 | — | — | 1 | 7.55 |
| CHEMBL1837044 | — | — | 1 | 7.54 |
| CHEMBL1837053 | — | — | 1 | 7.54 |
| CHEMBL1837051 | — | — | 2 | 7.44 |
| CHEMBL1837052 | — | — | 1 | 7.04 |
| CHEMBL1837056 | — | — | 1 | 7.03 |
| CHEMBL1837057 | — | — | 1 | 6.83 |
| CHEMBL1837055 | — | — | 1 | 6.73 |
| CHEMBL1837054 | — | — | 1 | 6.36 |
| CHEMBL1837062 | — | — | 1 | 6.12 |
| CHEMBL1837058 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL568933 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1837046 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1837047 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1837061 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1837060 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1837059 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1837048 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1837042 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1837043 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1837045 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1837049 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1837050 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1837044 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1837053 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1837051 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1837051 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1837052 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL1837056 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1837057 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL1837055 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL1837054 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL1837062 | — | IC50 | = | 767.0 | nM | 6.12 |
| CHEMBL1837058 | — | IC50 | = | 888.0 | nM | 6.05 |