Assay Detail
Binding
CHEMBL2330767
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Epibatidine from rat alpha4beta4 nACHR expressed in HEK293 cell membranes by liquid scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta4 (CHEMBL1907595) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.10 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.55 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.40 |
| CHEMBL2024096 | — | — | 1 | 7.28 |
| CHEMBL2323569 | — | — | 1 | 6.12 |
| CHEMBL2323571 | — | — | 1 | 5.52 |
| CHEMBL2323570 | — | — | 1 | 5.48 |
| CHEMBL2323566 | — | — | 1 | 5.46 |
| CHEMBL2323572 | — | — | 1 | 5.43 |
| CHEMBL2323568 | — | — | 1 | 4.64 |
| CHEMBL2323573 | — | — | 1 | - |
| CHEMBL2323567 | — | — | 1 | - |
| CHEMBL2323565 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3 | NICOTINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2024096 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL2323569 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL2323571 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL2323570 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL2323566 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL2323572 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL2323568 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL2323573 | — | Ki | - | — | - | |
| CHEMBL2323567 | — | Ki | = | 270000.0 | nM | - |
| CHEMBL2323565 | — | Ki | = | 160000.0 | nM | - |