Assay Detail
Binding
CHEMBL5316641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Epibatidine from alpha4beta2 nAChR (unknown origin) expressed in HEK293 cell membrane assessed as inhibition constant by beta counter method
33
Total Activities
33
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
Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 5.06 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4287656 | — | — | 1 | 5.92 |
| CHEMBL5423336 | — | — | 1 | 5.75 |
| CHEMBL5396579 | — | — | 1 | 5.35 |
| CHEMBL5393773 | — | — | 1 | 5.29 |
| CHEMBL5403618 | — | — | 1 | 5.14 |
| CHEMBL5415255 | — | — | 1 | 5.12 |
| CHEMBL5407945 | — | — | 1 | 5.01 |
| CHEMBL5418191 | — | — | 1 | 5.00 |
| CHEMBL5415576 | — | — | 1 | 4.98 |
| CHEMBL5435415 | — | — | 1 | 4.93 |
| CHEMBL5396724 | — | — | 1 | 4.72 |
| CHEMBL5415788 | — | — | 1 | 4.71 |
| CHEMBL5406306 | — | — | 1 | 4.66 |
| CHEMBL5436520 | — | — | 1 | 4.64 |
| CHEMBL5435510 | — | — | 1 | 4.62 |
| CHEMBL5416363 | — | — | 1 | - |
| CHEMBL5412463 | — | — | 1 | - |
| CHEMBL5396300 | — | — | 1 | - |
| CHEMBL5425014 | — | — | 1 | - |
| CHEMBL5428774 | — | — | 1 | - |
| CHEMBL1257065 | STILONIUM IODIDE | 2.0 | 1 | - |
| CHEMBL5395819 | — | — | 1 | - |
| CHEMBL5400651 | — | — | 1 | - |
| CHEMBL5417751 | — | — | 1 | - |
| CHEMBL5409285 | — | — | 1 | - |
| CHEMBL5433741 | — | — | 1 | - |
| CHEMBL5416962 | — | — | 1 | - |
| CHEMBL5408237 | — | — | 1 | - |
| CHEMBL5432840 | — | — | 1 | - |
| CHEMBL5415738 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4287656 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL5423336 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL5396579 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL5393773 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL5403618 | — | Ki | = | 7240.0 | nM | 5.14 |
| CHEMBL5415255 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL5407945 | — | Ki | = | 9820.0 | nM | 5.01 |
| CHEMBL5418191 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL5415576 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL5435415 | — | Ki | = | 11800.0 | nM | 4.93 |
| CHEMBL5396724 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL5415788 | — | Ki | = | 19400.0 | nM | 4.71 |
| CHEMBL5406306 | — | Ki | = | 21800.0 | nM | 4.66 |
| CHEMBL5436520 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL5435510 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL5178473 | — | Ki | = | 9300.0 | nM | - |
| CHEMBL5399641 | — | Ki | - | — | - | |
| CHEMBL5415482 | — | Ki | - | — | - | |
| CHEMBL5416363 | — | Ki | - | — | - | |
| CHEMBL5412463 | — | Ki | - | — | - | |
| CHEMBL5396300 | — | Ki | - | — | - | |
| CHEMBL5425014 | — | Ki | - | — | - | |
| CHEMBL5428774 | — | Ki | - | — | - | |
| CHEMBL1257065 | STILONIUM IODIDE | Ki | = | 5700.0 | nM | - |
| CHEMBL5395819 | — | Ki | - | — | - | |
| CHEMBL5400651 | — | Ki | - | — | - | |
| CHEMBL5417751 | — | Ki | - | — | - | |
| CHEMBL5409285 | — | Ki | - | — | - | |
| CHEMBL5433741 | — | Ki | - | — | - | |
| CHEMBL5416962 | — | Ki | - | — | - | |
| CHEMBL5408237 | — | Ki | - | — | - | |
| CHEMBL5432840 | — | Ki | - | — | - | |
| CHEMBL5415738 | — | Ki | - | — | - |