Assay Detail
Binding
CHEMBL2168701
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]iodoMLA from rat cerebral cortex alpha7 nAChR at 50 nM incubated for 2 hrs by microplate scintillation assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 8 | 6.61 | 7.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.49 |
| CHEMBL2164667 | — | — | 1 | 5.73 |
| CHEMBL2164666 | — | — | 1 | - |
| CHEMBL2164665 | — | — | 1 | - |
| CHEMBL2164664 | — | — | 1 | - |
| CHEMBL372638 | — | — | 1 | - |
| CHEMBL2164663 | — | — | 1 | - |
| CHEMBL361465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 32.5 | nM | 7.49 |
| CHEMBL2164667 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL2164666 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164665 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164664 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL372638 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164663 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL361465 | — | Ki | > | 2000.0 | nM | - |