Assay Detail
Binding
CHEMBL874099
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Binding affinity towards rat alpha2-beta4 nACh receptor 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 7.37 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 2 | 10.06 |
| CHEMBL497939 | CYTISINICLINE | 3.0 | 1 | 8.26 |
| CHEMBL59986 | — | — | 1 | 7.77 |
| CHEMBL55138 | — | — | 1 | 7.33 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.89 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 6.75 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.19 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | — | 1 | 5.89 |
| CHEMBL920 | CHOLINE | 0.5 | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.087 | nM | 10.06 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL497939 | CYTISINICLINE | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL59986 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL55138 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL3 | NICOTINE | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL667 | ACETYLCHOLINE | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL14 | CARBACHOL | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL47814 | DIMETHYLPHENYLPIPERAZINIUM IODIDE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL920 | CHOLINE | Ki | = | 21000.0 | nM | 4.68 |