Assay Detail
Binding
CHEMBL2383618
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Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR overexpressed in human SH-SY5Y cells after 120 mins by liquid scintillation spectrometric analysis
25
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 5.03 | 5.96 |
| IC50 | 9 | 4.73 | 5.64 |
| Inhibition | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2381566 | — | — | 3 | 5.96 |
| CHEMBL3 | NICOTINE | 4.0 | 2 | 5.42 |
| CHEMBL2381563 | — | — | 3 | 5.35 |
| CHEMBL2381568 | — | — | 3 | 5.17 |
| CHEMBL2381571 | — | — | 3 | 4.98 |
| CHEMBL2381564 | — | — | 3 | 4.53 |
| CHEMBL2381567 | — | — | 2 | 4.53 |
| CHEMBL2381565 | — | — | 3 | 4.31 |
| CHEMBL2381570 | — | — | 1 | - |
| CHEMBL2381569 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2381566 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL2381566 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3 | NICOTINE | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL2381563 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL2381568 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL3 | NICOTINE | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2381563 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL2381571 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL2381568 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL2381571 | — | IC50 | = | 21100.0 | nM | 4.68 |
| CHEMBL2381564 | — | Ki | = | 29300.0 | nM | 4.53 |
| CHEMBL2381567 | — | Ki | = | 29500.0 | nM | 4.53 |
| CHEMBL2381565 | — | Ki | = | 48700.0 | nM | 4.31 |
| CHEMBL2381567 | — | IC50 | = | 59100.0 | nM | 4.23 |
| CHEMBL2381564 | — | IC50 | = | 58500.0 | nM | 4.23 |
| CHEMBL2381565 | — | IC50 | = | 97300.0 | nM | 4.01 |
| CHEMBL2381571 | — | Inhibition | - | % | - | |
| CHEMBL2381570 | — | Inhibition | - | % | - | |
| CHEMBL2381563 | — | Inhibition | - | % | - | |
| CHEMBL2381569 | — | Ki | = | 232000.0 | nM | - |
| CHEMBL2381564 | — | Inhibition | - | % | - | |
| CHEMBL2381566 | — | Inhibition | - | % | - | |
| CHEMBL2381569 | — | IC50 | = | 464000.0 | nM | - |
| CHEMBL2381568 | — | Inhibition | - | % | - | |
| CHEMBL2381565 | — | Inhibition | - | % | - |