Assay Detail
Functional
CHEMBL2061182
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human ganglionic nAChR alpha3beta4 expressed in human SHSY-5Y cells assessed as calcium flux by fluorescence analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Diazaspirocyclic compounds as selective ligands for the α4β2 nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 4.88 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2057714 | — | — | 1 | 5.58 |
| CHEMBL2057713 | — | — | 1 | 5.16 |
| CHEMBL2057712 | — | — | 1 | 4.51 |
| CHEMBL504652 | TC-2216 | 1.0 | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2057714 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2057713 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2057712 | — | EC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL504652 | TC-2216 | EC50 | = | 55000.0 | nM | 4.26 |