Assay Detail
Binding
CHEMBL709388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at [3H]QNB and GppNHp radiolabeled muscarinic M2 receptor in rat heart.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 16 | 5.48 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.80 |
| CHEMBL118240 | — | — | 1 | 6.46 |
| CHEMBL118292 | — | — | 1 | 6.37 |
| CHEMBL109815 | — | — | 1 | 5.96 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | — | 1 | 5.82 |
| CHEMBL41779 | — | — | 1 | 5.80 |
| CHEMBL118700 | — | — | 1 | 5.48 |
| CHEMBL333107 | — | — | 1 | 5.22 |
| CHEMBL119615 | — | — | 1 | 5.03 |
| CHEMBL442206 | — | — | 1 | 4.89 |
| CHEMBL331556 | — | — | 1 | 4.57 |
| CHEMBL119985 | — | — | 1 | 4.52 |
| CHEMBL119508 | — | — | 1 | 4.28 |
| CHEMBL118949 | — | — | 1 | - |
| CHEMBL120706 | — | — | 1 | - |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL118240 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL118292 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL109815 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL41779 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL118700 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL333107 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL119615 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL442206 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL331556 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL119985 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL119508 | — | Ki | = | 52000.0 | nM | 4.28 |
| CHEMBL118949 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL120706 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL14 | CARBACHOL | Ki | = | 160000.0 | nM | - |