Assay Detail
Binding
CHEMBL752660
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Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 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; alpha3/beta4 (CHEMBL1907593) ↗| 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 | 6.69 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 2 | 9.32 |
| CHEMBL59986 | — | — | 1 | 7.14 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 6.68 |
| CHEMBL55138 | — | — | 1 | 6.54 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.28 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | — | 1 | 6.10 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 6.09 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.32 |
| CHEMBL920 | CHOLINE | 0.5 | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL59986 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL55138 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL3 | NICOTINE | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL667 | ACETYLCHOLINE | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL14 | CARBACHOL | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL920 | CHOLINE | Ki | = | 48000.0 | nM | 4.32 |