Assay Detail
Binding
CHEMBL703402
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Binding affinity at [3H]CD 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 | 7.32 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | — | 1 | 9.30 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | — | 1 | 9.11 |
| CHEMBL310852 | — | — | 1 | 8.40 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 8.40 |
| CHEMBL41779 | — | — | 1 | 8.20 |
| CHEMBL109815 | — | — | 1 | 7.82 |
| CHEMBL118292 | — | — | 1 | 7.64 |
| CHEMBL118700 | — | — | 1 | 7.26 |
| CHEMBL118240 | — | — | 1 | 7.25 |
| CHEMBL119615 | — | — | 1 | 7.15 |
| CHEMBL442206 | — | — | 1 | 6.58 |
| CHEMBL325473 | — | — | 1 | 6.35 |
| CHEMBL119985 | — | — | 1 | 6.20 |
| CHEMBL119508 | — | — | 1 | 6.01 |
| CHEMBL333107 | — | — | 1 | 5.82 |
| CHEMBL331556 | — | — | 1 | 5.60 |
| CHEMBL120706 | — | — | 1 | - |
| CHEMBL118949 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7634 | OXOTREMORINE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL310852 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL14 | CARBACHOL | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL41779 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL109815 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL118292 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL118700 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL118240 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL119615 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL442206 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL325473 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL119985 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL119508 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL333107 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL331556 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL120706 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL118949 | — | Ki | > | 10000.0 | nM | - |