Assay Detail
Binding
CHEMBL5136915
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-epibatidine from human alpha3beta4 nAChR expressed in SH-EP1 cells membrane assessed as inhibition constant preincubated for 5 mins followed by overnight incubation with [3H]-epibatidine by gamma liquid scintilation counting analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-EP1 |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| 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 | 24 | 6.38 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5177606 | — | — | 1 | 7.48 |
| CHEMBL5176101 | — | — | 1 | 7.36 |
| CHEMBL5190813 | — | — | 1 | 7.11 |
| CHEMBL5182114 | — | — | 1 | 7.02 |
| CHEMBL5197631 | — | — | 1 | 6.83 |
| CHEMBL5192210 | — | — | 1 | 6.80 |
| CHEMBL5200914 | — | — | 1 | 6.80 |
| CHEMBL5181363 | — | — | 1 | 6.75 |
| CHEMBL5170445 | — | — | 1 | 6.59 |
| CHEMBL5193899 | — | — | 1 | 6.54 |
| CHEMBL5171118 | — | — | 1 | 6.43 |
| CHEMBL1257065 | STILONIUM IODIDE | 2.0 | 1 | 6.36 |
| CHEMBL5184266 | — | — | 1 | 6.26 |
| CHEMBL5202770 | — | — | 1 | 6.24 |
| CHEMBL5174508 | — | — | 1 | 6.18 |
| CHEMBL5182514 | — | — | 1 | 6.11 |
| CHEMBL5186396 | — | — | 1 | 6.10 |
| CHEMBL5176544 | — | — | 1 | 6.06 |
| CHEMBL5193143 | — | — | 1 | 5.90 |
| CHEMBL5191958 | — | — | 1 | 5.82 |
| CHEMBL5176690 | — | — | 1 | 5.80 |
| CHEMBL5178473 | — | — | 1 | 5.57 |
| CHEMBL5201239 | — | — | 1 | 5.55 |
| CHEMBL5195695 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5177606 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5176101 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL5190813 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL5182114 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL5197631 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL5192210 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL5200914 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL5181363 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL5170445 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL5193899 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL5171118 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL1257065 | STILONIUM IODIDE | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL5184266 | — | Ki | = | 546.0 | nM | 6.26 |
| CHEMBL5202770 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL5174508 | — | Ki | = | 662.0 | nM | 6.18 |
| CHEMBL5182514 | — | Ki | = | 783.0 | nM | 6.11 |
| CHEMBL5186396 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL5176544 | — | Ki | = | 875.0 | nM | 6.06 |
| CHEMBL5193143 | — | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL5191958 | — | Ki | = | 1527.0 | nM | 5.82 |
| CHEMBL5176690 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL5178473 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL5201239 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL5195695 | — | Ki | = | 3490.0 | nM | 5.46 |