Assay Detail
Binding
CHEMBL839689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-nicotine binding to nicotinic acetylcholine receptor alpha4-beta2 in rat cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 5 | 7.92 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 9.77 |
| CHEMBL187992 | — | — | 1 | 8.49 |
| CHEMBL373144 | — | — | 1 | 7.19 |
| CHEMBL363791 | — | — | 1 | 7.12 |
| CHEMBL190750 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497939 | CYTISINICLINE | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL187992 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL373144 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL363791 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL190750 | — | Ki | = | 90.0 | nM | 7.05 |