Assay Detail
Binding
CHEMBL5136918
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response treated for 1 sec in presence of acetylcholine at holding potential of -70 mV by two electrode voltage-clamp assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.50 | 8.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5201239 | — | — | 1 | 8.83 |
| CHEMBL5178473 | — | — | 1 | 8.83 |
| CHEMBL1257065 | STILONIUM IODIDE | 2.0 | 1 | 8.70 |
| CHEMBL5190813 | — | — | 1 | 8.69 |
| CHEMBL5176101 | — | — | 1 | 8.64 |
| CHEMBL5174508 | — | — | 1 | 8.61 |
| CHEMBL5177606 | — | — | 1 | 8.56 |
| CHEMBL5176690 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5201239 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL5178473 | — | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL1257065 | STILONIUM IODIDE | IC50 | = | 1.99 | nM | 8.70 |
| CHEMBL5190813 | — | IC50 | = | 2.04 | nM | 8.69 |
| CHEMBL5176101 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL5174508 | — | IC50 | = | 2.45 | nM | 8.61 |
| CHEMBL5177606 | — | IC50 | = | 2.75 | nM | 8.56 |
| CHEMBL5176690 | — | IC50 | = | 78.2 | nM | 7.11 |