Assay Detail
Binding
CHEMBL1837503
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma-secretase-mediated notch cleavage in human SNC-204B8 cells after 16 hrs by luciferase reporter gene assay
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SNC-204B8 |
| 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 | 4.95 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL568933 | — | — | 1 | 6.06 |
| CHEMBL1837045 | — | — | 1 | 5.95 |
| CHEMBL1837046 | — | — | 1 | 5.95 |
| CHEMBL1837047 | — | — | 1 | 5.70 |
| CHEMBL1837061 | — | — | 1 | 5.65 |
| CHEMBL1837059 | — | — | 1 | 5.20 |
| CHEMBL1837048 | — | — | 1 | 5.18 |
| CHEMBL1837043 | — | — | 1 | 5.13 |
| CHEMBL1837060 | — | — | 1 | 5.05 |
| CHEMBL1837051 | — | — | 2 | 4.98 |
| CHEMBL1837042 | — | — | 1 | 4.96 |
| CHEMBL1837049 | — | — | 1 | 4.84 |
| CHEMBL1837053 | — | — | 1 | 4.74 |
| CHEMBL1837052 | — | — | 1 | 4.73 |
| CHEMBL1837044 | — | — | 1 | 4.57 |
| CHEMBL1837057 | — | — | 1 | 4.40 |
| CHEMBL1837055 | — | — | 1 | 4.40 |
| CHEMBL1837050 | — | — | 1 | 4.40 |
| CHEMBL1837056 | — | — | 1 | 4.39 |
| CHEMBL1837058 | — | — | 1 | 4.39 |
| CHEMBL1837054 | — | — | 1 | 4.39 |
| CHEMBL1837062 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL568933 | — | IC50 | = | 879.0 | nM | 6.06 |
| CHEMBL1837045 | — | IC50 | = | 1136.0 | nM | 5.95 |
| CHEMBL1837046 | — | IC50 | = | 1128.0 | nM | 5.95 |
| CHEMBL1837047 | — | IC50 | = | 2003.0 | nM | 5.70 |
| CHEMBL1837061 | — | IC50 | = | 2229.0 | nM | 5.65 |
| CHEMBL1837059 | — | IC50 | = | 6346.0 | nM | 5.20 |
| CHEMBL1837048 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1837043 | — | IC50 | = | 7471.0 | nM | 5.13 |
| CHEMBL1837060 | — | IC50 | = | 8989.0 | nM | 5.05 |
| CHEMBL1837051 | — | IC50 | = | 10457.0 | nM | 4.98 |
| CHEMBL1837042 | — | IC50 | = | 10932.0 | nM | 4.96 |
| CHEMBL1837049 | — | IC50 | = | 14431.0 | nM | 4.84 |
| CHEMBL1837053 | — | IC50 | = | 18385.0 | nM | 4.74 |
| CHEMBL1837052 | — | IC50 | = | 18719.0 | nM | 4.73 |
| CHEMBL1837044 | — | IC50 | = | 26719.0 | nM | 4.57 |
| CHEMBL1837051 | — | IC50 | = | 29717.0 | nM | 4.53 |
| CHEMBL1837050 | — | IC50 | = | 39698.0 | nM | 4.40 |
| CHEMBL1837055 | — | IC50 | = | 39836.0 | nM | 4.40 |
| CHEMBL1837057 | — | IC50 | = | 39980.0 | nM | 4.40 |
| CHEMBL1837054 | — | IC50 | = | 40902.0 | nM | 4.39 |
| CHEMBL1837056 | — | IC50 | = | 40248.0 | nM | 4.39 |
| CHEMBL1837058 | — | IC50 | = | 40716.0 | nM | 4.39 |
| CHEMBL1837062 | — | IC50 | = | 42636.0 | nM | 4.37 |