Assay Detail
Binding
CHEMBL750088
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Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand
10
Total Activities
9
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/beta2 (CHEMBL1907592) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.48 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 2 | 10.59 |
| CHEMBL55138 | — | — | 1 | 10.51 |
| CHEMBL59986 | — | — | 1 | 10.13 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.85 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 7.96 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.82 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | — | 1 | 7.55 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.68 |
| CHEMBL920 | CHOLINE | 0.5 | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL55138 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL59986 | — | Ki | = | 0.074 | nM | 10.13 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL667 | ACETYLCHOLINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3 | NICOTINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL14 | CARBACHOL | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL920 | CHOLINE | Ki | = | 18000.0 | nM | 4.75 |