Assay Detail
Binding
CHEMBL3271084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat brain cortical membrane after 3 hrs by liquid scintillation spectrometric analysis
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Molecular basis of the selective binding of MDMA enantiomers to the alpha4beta2 nicotinic receptor subtype: synthesis, pharmacological evaluation and mechanistic studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 3 | - | - |
| IC50 | 3 | 4.70 | 4.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382757 | — | — | 2 | 4.87 |
| CHEMBL43048 | MIDOMAFETAMINE | 3.0 | 2 | 4.52 |
| CHEMBL195390 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382757 | — | IC50 | = | 13450.0 | nM | 4.87 |
| CHEMBL43048 | MIDOMAFETAMINE | IC50 | = | 30400.0 | nM | 4.52 |
| CHEMBL382757 | — | Inhibition | - | % | - | |
| CHEMBL195390 | — | Inhibition | - | % | - | |
| CHEMBL43048 | MIDOMAFETAMINE | Inhibition | - | % | - | |
| CHEMBL195390 | — | IC50 | = | 172650.0 | nM | - |