Assay Detail
Binding
CHEMBL2330760
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Desensitization of human alpha4beta2 nACHR expressed in HEK293 cells assessed as inhibition of 86Rb+ efflux preincubated for 10 mins measured after 2 hrs by liquid scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| IC50 | 9 | 6.84 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024096 | — | — | 1 | 7.96 |
| CHEMBL2323570 | — | — | 1 | 7.29 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.03 |
| CHEMBL2323569 | — | — | 1 | 6.96 |
| CHEMBL2323571 | — | — | 1 | 6.89 |
| CHEMBL2323572 | — | — | 1 | 6.58 |
| CHEMBL2323566 | — | — | 1 | 6.58 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.43 |
| CHEMBL2323568 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024096 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2323570 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1076903 | VARENICLINE | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2323569 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2323571 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2323572 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2323566 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3 | NICOTINE | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2323568 | — | IC50 | = | 1600.0 | nM | 5.80 |