Assay Detail
Binding
CHEMBL709389
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Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat cortex.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.91 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | — | 1 | 7.22 |
| CHEMBL310852 | — | — | 1 | 7.10 |
| CHEMBL118240 | — | — | 1 | 6.92 |
| CHEMBL118292 | — | — | 1 | 6.37 |
| CHEMBL109815 | — | — | 1 | 6.15 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | — | 1 | 6.04 |
| CHEMBL333107 | — | — | 1 | 5.64 |
| CHEMBL41779 | — | — | 1 | 5.54 |
| CHEMBL118700 | — | — | 1 | 5.54 |
| CHEMBL331556 | — | — | 1 | 5.33 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.30 |
| CHEMBL119615 | — | — | 1 | 5.05 |
| CHEMBL442206 | — | — | 1 | 4.66 |
| CHEMBL119985 | — | — | 1 | - |
| CHEMBL120706 | — | — | 1 | - |
| CHEMBL325473 | — | — | 1 | - |
| CHEMBL118949 | — | — | 1 | - |
| CHEMBL119508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL310852 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL118240 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL118292 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL109815 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL333107 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL41779 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL118700 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL331556 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL14 | CARBACHOL | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL119615 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL442206 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL119985 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL120706 | — | Ki | = | 150000.0 | nM | - |
| CHEMBL325473 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL118949 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL119508 | — | Ki | > | 100000.0 | nM | - |