Assay Detail
Binding
CHEMBL4679293
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at human alpha4beta2 transfected in rat GH4-C1 cells at holding potential of -70 mV by whole cell patch clamp electrophysiology method
4
Total Activities
4
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
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.17 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741357 | — | — | 1 | 8.30 |
| CHEMBL1917231 | — | — | 1 | 6.52 |
| CHEMBL4095303 | — | — | 1 | 5.00 |
| CHEMBL4785648 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741357 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1917231 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4095303 | — | EC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL4785648 | — | EC50 | = | 14000.0 | nM | 4.85 |