Assay Detail
Binding
CHEMBL839749
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Inhibition of [3H]epibatidine binding to nicotinic acetylcholine receptor alpha3-beta4 of IMR32 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.06 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.28 |
| CHEMBL191867 | — | — | 1 | 6.15 |
| CHEMBL187992 | — | — | 1 | 6.09 |
| CHEMBL365965 | — | — | 1 | 6.09 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 6.08 |
| CHEMBL190826 | — | — | 1 | 6.01 |
| CHEMBL373359 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL191867 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL187992 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL365965 | — | Ki | = | 810.0 | nM | 6.09 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL190826 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL373359 | — | Ki | = | 1900.0 | nM | 5.72 |