Assay Detail
Binding
CHEMBL3607042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha4beta2 nAChR expressed in rat GH4C1 cells assessed as induction of peak current amplitude at holding potential of -70 mV by whole-cell patch clamp assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | GH4-C1 |
| 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 Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 6.70 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024096 | — | — | 1 | 9.57 |
| CHEMBL3603947 | — | — | 1 | 7.89 |
| CHEMBL1917231 | — | — | 1 | 6.52 |
| CHEMBL3603929 | — | — | 1 | 5.36 |
| CHEMBL3603933 | — | — | 1 | 4.14 |
| CHEMBL3603939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024096 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3603947 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1917231 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3603929 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3603933 | — | EC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL3603939 | — | EC50 | - | — | - |