Assay Detail
Binding
CHEMBL2383617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]cytisine from human alpha4beta2 nAChR overexpressed in human SHEP cells after 75 mins by liquid scintillation spectrometric analysis
27
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SHEP |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.71 | 9.22 |
| IC50 | 10 | 7.14 | 8.92 |
| Inhibition | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 2 | 9.22 |
| CHEMBL2381566 | — | — | 3 | 8.92 |
| CHEMBL2381570 | — | — | 3 | 8.09 |
| CHEMBL2381563 | — | — | 3 | 7.95 |
| CHEMBL2381567 | — | — | 2 | 7.81 |
| CHEMBL2381571 | — | — | 3 | 7.65 |
| CHEMBL2381568 | — | — | 3 | 7.63 |
| CHEMBL2381564 | — | — | 3 | 6.82 |
| CHEMBL2381565 | — | — | 3 | 6.66 |
| CHEMBL2381569 | — | — | 2 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3 | NICOTINE | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2381566 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2381566 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL2381570 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL2381563 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL2381567 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL2381571 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL2381568 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL2381570 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL2381563 | — | IC50 | = | 39.4 | nM | 7.41 |
| CHEMBL2381571 | — | IC50 | = | 78.4 | nM | 7.11 |
| CHEMBL2381568 | — | IC50 | = | 81.9 | nM | 7.09 |
| CHEMBL2381564 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL2381567 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL2381565 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL2381569 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL2381564 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL2381565 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL2381569 | — | IC50 | = | 1611.0 | nM | 5.79 |
| CHEMBL2381563 | — | Inhibition | - | % | - | |
| CHEMBL2381565 | — | Inhibition | - | % | - | |
| CHEMBL2381564 | — | Inhibition | - | % | - | |
| CHEMBL2381570 | — | Inhibition | - | % | - | |
| CHEMBL2381566 | — | Inhibition | - | % | - | |
| CHEMBL2381571 | — | Inhibition | - | % | - | |
| CHEMBL2381568 | — | Inhibition | - | % | - |