Assay Detail
Binding
CHEMBL990842
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Displacement of [3H]epibatidine from nAChR in rat cerebral cortex membrane
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 11 | 9.43 | 10.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.35 |
| CHEMBL478029 | — | — | 1 | 10.30 |
| CHEMBL476140 | — | — | 3 | 10.30 |
| CHEMBL514372 | — | — | 3 | 9.96 |
| CHEMBL478447 | — | — | 2 | 9.51 |
| CHEMBL515332 | — | — | 1 | 8.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL478029 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL476140 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL514372 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL476140 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL478447 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL514372 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL515332 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL478447 | — | Ki | = | 4.67 | nM | 8.33 |
| CHEMBL476140 | — | Ki | = | 7.35 | nM | 8.13 |
| CHEMBL514372 | — | Ki | = | 0.14 | — | - |