Assay Detail
Binding
CHEMBL755477
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In vitro binding affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membrane using [3H]cytisine as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.89 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59986 | — | — | 1 | 8.82 |
| CHEMBL72789 | — | — | 1 | 8.74 |
| CHEMBL71085 | — | — | 1 | 8.72 |
| CHEMBL71666 | — | — | 1 | 8.72 |
| CHEMBL74068 | — | — | 1 | 8.66 |
| CHEMBL72320 | — | — | 1 | 8.62 |
| CHEMBL72262 | — | — | 1 | 8.62 |
| CHEMBL70335 | — | — | 1 | 8.55 |
| CHEMBL303889 | — | — | 1 | 8.52 |
| CHEMBL72605 | — | — | 1 | 8.52 |
| CHEMBL304604 | — | — | 1 | 8.40 |
| CHEMBL71255 | — | — | 1 | 8.40 |
| CHEMBL72284 | — | — | 1 | 8.35 |
| CHEMBL69725 | — | — | 1 | 8.18 |
| CHEMBL62765 | — | — | 1 | 8.17 |
| CHEMBL72523 | — | — | 1 | 8.10 |
| CHEMBL70737 | — | — | 1 | 7.70 |
| CHEMBL273218 | — | — | 1 | 7.00 |
| CHEMBL70717 | — | — | 1 | 6.77 |
| CHEMBL71068 | — | — | 1 | 6.77 |
| CHEMBL71067 | — | — | 1 | 6.77 |
| CHEMBL9965 | — | — | 1 | 6.72 |
| CHEMBL74466 | — | — | 1 | 6.66 |
| CHEMBL68563 | — | — | 1 | 6.51 |
| CHEMBL305073 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59986 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL72789 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL71085 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL71666 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL74068 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL72320 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL72262 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL70335 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL303889 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL72605 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL304604 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL71255 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL72284 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL69725 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL62765 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL72523 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL70737 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL273218 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL70717 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL71068 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL71067 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL9965 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL74466 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL68563 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL305073 | — | IC50 | = | 500.0 | nM | 6.30 |