Assay Detail
Binding
CHEMBL882459
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In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 using 0.5 nM [3H]epibatidine
14
Total Activities
14
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
Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 9.84 | 10.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197830 | — | — | 1 | 10.55 |
| CHEMBL198228 | — | — | 1 | 10.49 |
| CHEMBL372133 | — | — | 1 | 10.47 |
| CHEMBL291961 | — | — | 1 | 10.41 |
| CHEMBL372638 | — | — | 1 | 10.41 |
| CHEMBL197526 | — | — | 1 | 10.24 |
| CHEMBL185612 | — | — | 1 | 10.21 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.21 |
| CHEMBL185060 | — | — | 1 | 10.11 |
| CHEMBL372326 | — | — | 1 | 9.55 |
| CHEMBL58935 | — | — | 1 | 9.13 |
| CHEMBL382533 | — | — | 1 | 9.05 |
| CHEMBL197725 | — | — | 1 | 8.90 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197830 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL198228 | — | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL372133 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL291961 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL372638 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL197526 | — | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL185612 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.061 | nM | 10.21 |
| CHEMBL185060 | — | Ki | = | 0.078 | nM | 10.11 |
| CHEMBL372326 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL58935 | — | Ki | = | 0.733 | nM | 9.13 |
| CHEMBL382533 | — | Ki | = | 0.898 | nM | 9.05 |
| CHEMBL197725 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL3 | NICOTINE | Ki | = | 10.0 | nM | 8.00 |