Assay Detail
Binding
CHEMBL2025952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] epibatidine from rat alpha2beta4 nAChR by beta scintillation counting
10
Total Activities
10
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; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.47 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024088 | — | — | 1 | 7.19 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.16 |
| CHEMBL2024094 | — | — | 1 | 6.63 |
| CHEMBL2024093 | — | — | 1 | 6.62 |
| CHEMBL2024087 | — | — | 1 | 6.60 |
| CHEMBL2024090 | — | — | 1 | 6.58 |
| CHEMBL2024095 | — | — | 1 | 6.39 |
| CHEMBL2024091 | — | — | 1 | 6.14 |
| CHEMBL2024089 | — | — | 1 | 5.72 |
| CHEMBL2024092 | — | — | 1 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024088 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3 | NICOTINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2024094 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL2024093 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL2024087 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL2024090 | — | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL2024095 | — | Ki | = | 405.0 | nM | 6.39 |
| CHEMBL2024091 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL2024089 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL2024092 | — | Ki | = | 2330.0 | nM | 5.63 |