Assay Detail
Binding
CHEMBL5136916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-epibatidine from human alpha4beta2 nAChR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by overnight incubation with [3H]-epibatidine by gamma liquid scintilation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| 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 |
|---|---|---|---|
| Ki | 16 | 8.29 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200914 | — | — | 1 | 8.89 |
| CHEMBL5193143 | — | — | 1 | 8.89 |
| CHEMBL5177606 | — | — | 1 | 8.72 |
| CHEMBL5182114 | — | — | 1 | 8.72 |
| CHEMBL5201239 | — | — | 1 | 8.64 |
| CHEMBL5171118 | — | — | 1 | 8.52 |
| CHEMBL1257065 | STILONIUM IODIDE | 2.0 | 1 | 8.24 |
| CHEMBL5176690 | — | — | 1 | 8.20 |
| CHEMBL5190813 | — | — | 1 | 8.18 |
| CHEMBL5176101 | — | — | 1 | 8.13 |
| CHEMBL5178473 | — | — | 1 | 8.03 |
| CHEMBL5202770 | — | — | 1 | 7.97 |
| CHEMBL5193899 | — | — | 1 | 7.95 |
| CHEMBL5184266 | — | — | 1 | 7.92 |
| CHEMBL5174508 | — | — | 1 | 7.83 |
| CHEMBL5197631 | — | — | 1 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200914 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5193143 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5177606 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5182114 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5201239 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5171118 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1257065 | STILONIUM IODIDE | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL5176690 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL5190813 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL5176101 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL5178473 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL5202770 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL5193899 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL5184266 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5174508 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL5197631 | — | Ki | = | 18.6 | nM | 7.73 |