Assay Detail
Binding
CHEMBL990845
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Displacement of [3H]epibatidine from rat alpha2beta4 nAChR expressed in HEK293 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.74 | 10.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.02 |
| CHEMBL478029 | — | — | 1 | 9.29 |
| CHEMBL476140 | — | — | 1 | 9.18 |
| CHEMBL514372 | — | — | 1 | 9.08 |
| CHEMBL478447 | — | — | 1 | 8.11 |
| CHEMBL449437 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.095 | nM | 10.02 |
| CHEMBL478029 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL476140 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL514372 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL478447 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL449437 | — | Ki | = | 181.0 | nM | 6.74 |