Assay Detail
Binding
CHEMBL908432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Nicotine from alpha4beta2 nAChR in rat cortical membranes
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Epibatidine isomers and analogues: structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.84 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 10.72 |
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 10.70 |
| CHEMBL185667 | — | — | 2 | 10.35 |
| CHEMBL535619 | — | — | 1 | 10.25 |
| CHEMBL535389 | (+/-)-HOMOEPIBATIDINE | — | 1 | 9.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL185667 | — | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL535619 | — | Ki | = | 0.056 | nM | 10.25 |
| CHEMBL535389 | (+/-)-HOMOEPIBATIDINE | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL185667 | — | Ki | = | 40.0 | nM | 7.40 |