Assay Detail
Binding
CHEMBL3607040
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cell membranes by liquid scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.10 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3603932 | — | — | 1 | 7.40 |
| CHEMBL3603929 | — | — | 1 | 7.13 |
| CHEMBL3603934 | — | — | 1 | 7.00 |
| CHEMBL3603931 | — | — | 1 | 6.99 |
| CHEMBL3603933 | — | — | 1 | 6.63 |
| CHEMBL3603941 | — | — | 1 | 6.59 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.58 |
| CHEMBL3603939 | — | — | 1 | 6.57 |
| CHEMBL3603935 | — | — | 1 | 6.13 |
| CHEMBL3603942 | — | — | 1 | 6.12 |
| CHEMBL3603943 | — | — | 1 | 6.10 |
| CHEMBL3603937 | — | — | 1 | 5.89 |
| CHEMBL3603938 | — | — | 1 | 5.85 |
| CHEMBL3603945 | — | — | 1 | 5.68 |
| CHEMBL3603946 | — | — | 1 | 5.54 |
| CHEMBL3603936 | — | — | 1 | 5.44 |
| CHEMBL3603930 | — | — | 1 | 5.42 |
| CHEMBL3603947 | — | — | 1 | 5.30 |
| CHEMBL3603944 | — | — | 1 | 5.28 |
| CHEMBL3603948 | — | — | 1 | 5.25 |
| CHEMBL3603940 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3603932 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3603929 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL3603934 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3603931 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL3603933 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL3603941 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL3 | NICOTINE | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL3603939 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL3603935 | — | Ki | = | 749.0 | nM | 6.13 |
| CHEMBL3603942 | — | Ki | = | 752.0 | nM | 6.12 |
| CHEMBL3603943 | — | Ki | = | 793.0 | nM | 6.10 |
| CHEMBL3603937 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3603938 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL3603945 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL3603946 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL3603936 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL3603930 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL3603947 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL3603944 | — | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL3603948 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL3603940 | — | Ki | = | 7700.0 | nM | 5.11 |