Assay Detail
Binding
CHEMBL1000460
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Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortical membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.57 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL503604 | EXO-EPIBOXIDINE | — | 1 | 9.40 |
| CHEMBL274525 | ABT-418 | — | 1 | 7.70 |
| CHEMBL449716 | — | — | 1 | 7.30 |
| CHEMBL504313 | ENDO-EPIBOXIDINE | — | 1 | 7.16 |
| CHEMBL525968 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL503604 | EXO-EPIBOXIDINE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL274525 | ABT-418 | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL449716 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL504313 | ENDO-EPIBOXIDINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL525968 | — | Ki | = | 514.0 | nM | 6.29 |