Assay Detail
Binding
CHEMBL829040
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Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.01 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 9.42 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 9.42 |
| CHEMBL190589 | — | — | 1 | 7.13 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 6.05 |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | — | 2 | - |
| CHEMBL370464 | — | — | 1 | - |
| CHEMBL190524 | — | — | 1 | - |
| CHEMBL193047 | — | — | 1 | - |
| CHEMBL190882 | — | — | 1 | - |
| CHEMBL365379 | — | — | 1 | - |
| CHEMBL190308 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL190589 | — | Ki | = | 73.6 | nM | 7.13 |
| CHEMBL667 | ACETYLCHOLINE | Ki | = | 881.0 | nM | 6.05 |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | - | nM | - | |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | - | nM | - | |
| CHEMBL370464 | — | Ki | - | nM | - | |
| CHEMBL190524 | — | Ki | - | nM | - | |
| CHEMBL193047 | — | Ki | - | nM | - | |
| CHEMBL190882 | — | Ki | - | nM | - | |
| CHEMBL365379 | — | Ki | - | nM | - | |
| CHEMBL190308 | — | Ki | - | nM | - |