Assay Detail
Binding
CHEMBL872674
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability of compound to compete with 50 pM of 5-[125I]iodo-A-85,380 for receptor binding sites in rat brain membranes at room temperature
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
5-substituted derivatives of 6-halogeno-3-((2-(S)-azetidinyl)methoxy)pyridine and 6-halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridine with low picomolar affinity for alpha4beta2 nicotinic acetylcholine receptor and wide range of lipophilicity: potential probes for imaging with positron emission tomography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 10.56 | 10.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83608 | — | — | 1 | 10.93 |
| CHEMBL83986 | — | — | 1 | 10.75 |
| CHEMBL84154 | — | — | 1 | 10.71 |
| CHEMBL79737 | — | — | 1 | 10.68 |
| CHEMBL439766 | — | — | 1 | 10.47 |
| CHEMBL308538 | — | — | 1 | 10.21 |
| CHEMBL79854 | — | — | 1 | 10.18 |
| CHEMBL79702 | — | — | 1 | - |
| CHEMBL86050 | — | — | 1 | - |
| CHEMBL80040 | — | — | 1 | - |
| CHEMBL309292 | — | — | 1 | - |
| CHEMBL79332 | — | — | 1 | - |
| CHEMBL79387 | — | — | 1 | - |
| CHEMBL83444 | — | — | 1 | - |
| CHEMBL79594 | — | — | 1 | - |
| CHEMBL313877 | — | — | 1 | - |
| CHEMBL312132 | — | — | 1 | - |
| CHEMBL314718 | — | — | 1 | - |
| CHEMBL310197 | — | — | 1 | - |
| CHEMBL86051 | — | — | 1 | - |
| CHEMBL6623 | EPIBATIDINE | — | 1 | - |
| CHEMBL79515 | — | — | 1 | - |
| CHEMBL83738 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83608 | — | Ki | = | 0.0117 | nM | 10.93 |
| CHEMBL83986 | — | Ki | = | 0.0179 | nM | 10.75 |
| CHEMBL84154 | — | Ki | = | 0.0195 | nM | 10.71 |
| CHEMBL79737 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL439766 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL308538 | — | Ki | = | 0.061 | nM | 10.21 |
| CHEMBL79854 | — | Ki | = | 0.066 | nM | 10.18 |
| CHEMBL79702 | — | Ki | = | 0.0066 | nM | - |
| CHEMBL86050 | — | Ki | = | 0.004 | nM | - |
| CHEMBL80040 | — | Ki | = | 0.009 | nM | - |
| CHEMBL309292 | — | Ki | = | 0.0088 | nM | - |
| CHEMBL79332 | — | Ki | = | 0.0031 | nM | - |
| CHEMBL79387 | — | Ki | = | 0.0033 | nM | - |
| CHEMBL83444 | — | Ki | = | 0.0049 | nM | - |
| CHEMBL79594 | — | Ki | = | 0.0048 | nM | - |
| CHEMBL313877 | — | Ki | = | 0.0052 | nM | - |
| CHEMBL312132 | — | Ki | = | 0.0081 | nM | - |
| CHEMBL314718 | — | Ki | = | 0.0045 | nM | - |
| CHEMBL310197 | — | Ki | = | 0.0094 | nM | - |
| CHEMBL86051 | — | Ki | = | 0.0043 | nM | - |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.009 | nM | - |
| CHEMBL79515 | — | Ki | = | 0.0056 | nM | - |
| CHEMBL83738 | — | Ki | = | 0.0077 | nM | - |