Assay Detail
Binding
CHEMBL3271085
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
3
Total Activities
3
Compounds Tested
1
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 |
|---|---|---|---|
| Ki | 3 | 5.71 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL382757 | — | — | 1 | 6.20 |
| CHEMBL43048 | MIDOMAFETAMINE | 3.0 | 1 | 5.84 |
| CHEMBL195390 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL382757 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL43048 | MIDOMAFETAMINE | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL195390 | — | Ki | = | 8210.0 | nM | 5.09 |