Assay Detail
Binding
CHEMBL3607038
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cortex membranes by liquid scintillation counting method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 23 | 6.81 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3603929 | — | — | 1 | 8.96 |
| CHEMBL3603934 | — | — | 1 | 8.60 |
| CHEMBL3603933 | — | — | 1 | 8.43 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.40 |
| CHEMBL3603932 | — | — | 1 | 8.15 |
| CHEMBL3603931 | — | — | 1 | 8.07 |
| CHEMBL3603941 | — | — | 1 | 7.96 |
| CHEMBL3603939 | — | — | 1 | 7.72 |
| CHEMBL3603947 | — | — | 1 | 7.57 |
| CHEMBL72031 | — | — | 1 | 7.28 |
| CHEMBL75446 | — | — | 1 | 7.00 |
| CHEMBL3603942 | — | — | 1 | 6.72 |
| CHEMBL3603945 | — | — | 1 | 6.59 |
| CHEMBL3603930 | — | — | 1 | 6.39 |
| CHEMBL3603946 | — | — | 1 | 6.21 |
| CHEMBL3603948 | — | — | 1 | 6.06 |
| CHEMBL3603940 | — | — | 1 | 5.97 |
| CHEMBL3603937 | — | — | 1 | 5.81 |
| CHEMBL3603938 | — | — | 1 | 5.34 |
| CHEMBL3603943 | — | — | 1 | 5.14 |
| CHEMBL3603944 | — | — | 1 | 5.05 |
| CHEMBL3603935 | — | — | 1 | 5.03 |
| CHEMBL3603936 | — | — | 1 | 4.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3603929 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3603934 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3603933 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3 | NICOTINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3603932 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3603931 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL3603941 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL3603939 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL3603947 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL72031 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL75446 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL3603942 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL3603945 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL3603930 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL3603946 | — | Ki | = | 613.0 | nM | 6.21 |
| CHEMBL3603948 | — | Ki | = | 877.0 | nM | 6.06 |
| CHEMBL3603940 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL3603937 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL3603938 | — | Ki | = | 4590.0 | nM | 5.34 |
| CHEMBL3603943 | — | Ki | = | 7280.0 | nM | 5.14 |
| CHEMBL3603944 | — | Ki | = | 8960.0 | nM | 5.05 |
| CHEMBL3603935 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL3603936 | — | Ki | = | 53500.0 | nM | 4.27 |