Assay Detail
Binding
CHEMBL748020
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Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain.
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor (CHEMBL2094110) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.49 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.37 |
| CHEMBL262769 | — | — | 1 | 10.30 |
| CHEMBL59986 | — | — | 1 | 10.28 |
| CHEMBL440195 | — | — | 1 | 9.85 |
| CHEMBL84149 | — | — | 2 | 9.82 |
| CHEMBL293435 | — | — | 1 | 9.35 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.00 |
| CHEMBL168780 | — | — | 1 | 8.46 |
| CHEMBL354602 | — | — | 1 | 7.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL262769 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL59986 | — | Ki | = | 0.052 | nM | 10.28 |
| CHEMBL440195 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL84149 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL84149 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL293435 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL3 | NICOTINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL168780 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL354602 | — | Ki | = | 19.7 | nM | 7.71 |