Assay Detail
Binding
CHEMBL2168702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat cerebral cortex alpha4beta2* nAChR incubated for 4 hrs by liquid scintillation assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.85 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306959 | — | — | 1 | 10.59 |
| CHEMBL2164666 | — | — | 1 | 10.52 |
| CHEMBL2164667 | — | — | 1 | 9.92 |
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 9.92 |
| CHEMBL2164664 | — | — | 1 | 9.77 |
| CHEMBL372638 | — | — | 1 | 9.72 |
| CHEMBL2164663 | — | — | 1 | 9.36 |
| CHEMBL2164665 | — | — | 1 | 9.03 |
| CHEMBL361465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306959 | — | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL2164666 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL2164667 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1076903 | VARENICLINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL2164664 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL372638 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL2164663 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL2164665 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL361465 | — | Ki | = | 0.009 | nM | - |