Assay Detail
Binding
CHEMBL2025957
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] epibatidine from rat alpha4beta4 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; alpha4/beta4 (CHEMBL1907595) ↗| 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 | 6.92 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.64 |
| CHEMBL2024088 | — | — | 1 | 7.54 |
| CHEMBL2024094 | — | — | 1 | 7.30 |
| CHEMBL2024087 | — | — | 1 | 7.08 |
| CHEMBL2024095 | — | — | 1 | 7.01 |
| CHEMBL2024092 | — | — | 1 | 6.79 |
| CHEMBL2024091 | — | — | 1 | 6.63 |
| CHEMBL2024090 | — | — | 1 | 6.55 |
| CHEMBL2024089 | — | — | 1 | 6.36 |
| CHEMBL2024093 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2024088 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2024094 | — | Ki | = | 50.2 | nM | 7.30 |
| CHEMBL2024087 | — | Ki | = | 82.6 | nM | 7.08 |
| CHEMBL2024095 | — | Ki | = | 96.5 | nM | 7.01 |
| CHEMBL2024092 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL2024091 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL2024090 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL2024089 | — | Ki | = | 441.0 | nM | 6.36 |
| CHEMBL2024093 | — | Ki | = | 551.0 | nM | 6.26 |