Assay Detail
Binding
CHEMBL3373417
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha7 nAChR expressed in GH3 cells by Ca2+/Fluo-4 assay
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | GH3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Semisynthetic analogues of toxiferine I and their pharmacological properties at α7 nAChRs, muscle-type nAChRs, and the allosteric binding site of muscarinic M2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.57 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3337862 | — | — | 2 | 6.23 |
| CHEMBL3337866 | — | — | 2 | 6.09 |
| CHEMBL3337861 | — | — | 2 | 5.66 |
| CHEMBL3337863 | — | — | 2 | 5.51 |
| CHEMBL3337865 | — | — | 2 | 5.48 |
| CHEMBL3355097 | — | — | 2 | 5.38 |
| CHEMBL3355098 | — | — | 2 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3337862 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3337862 | — | IC50 | = | 602.56 | nM | 6.22 |
| CHEMBL3337866 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL3337866 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3337861 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3337861 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL3337863 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3337863 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL3337865 | — | IC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL3337865 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3355097 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL3355097 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3355098 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3355098 | — | IC50 | = | 21379.62 | nM | 4.67 |