Assay Detail
Binding
CHEMBL830443
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Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates
16
Total Activities
15
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; alpha4/beta2 (CHEMBL1907596) ↗| 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 | 16 | 8.71 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | — | 2 | 10.82 |
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 10.30 |
| CHEMBL190589 | — | — | 1 | 10.30 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.14 |
| CHEMBL189064 | — | — | 1 | 9.82 |
| CHEMBL370464 | — | — | 1 | 8.68 |
| CHEMBL190524 | — | — | 1 | 8.62 |
| CHEMBL362789 | — | — | 1 | 8.57 |
| CHEMBL274525 | ABT-418 | — | 1 | 8.40 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 8.12 |
| CHEMBL193047 | — | — | 1 | 7.79 |
| CHEMBL190882 | — | — | 1 | 7.54 |
| CHEMBL365379 | — | — | 1 | 6.30 |
| CHEMBL190308 | — | — | 1 | 5.10 |
| CHEMBL433777 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL190589 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | = | 0.064 | nM | 10.19 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL189064 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL370464 | — | Ki | = | 2.07 | nM | 8.68 |
| CHEMBL190524 | — | Ki | = | 2.39 | nM | 8.62 |
| CHEMBL362789 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL274525 | ABT-418 | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL667 | ACETYLCHOLINE | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL193047 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL190882 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL365379 | — | Ki | = | 495.0 | nM | 6.30 |
| CHEMBL190308 | — | Ki | = | 7914.0 | nM | 5.10 |
| CHEMBL433777 | — | Ki | - | nM | - |