Assay Detail
Binding
CHEMBL711166
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Binding affinity at [3H]PZ radiolabeled muscarinic M1 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 M1 (CHEMBL276) ↗| 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 | 6.04 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL310852 | — | — | 1 | 7.40 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.92 |
| CHEMBL118240 | — | — | 1 | 6.89 |
| CHEMBL118292 | — | — | 1 | 6.60 |
| CHEMBL109815 | — | — | 1 | 6.54 |
| CHEMBL333107 | — | — | 1 | 6.29 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | — | 1 | 5.92 |
| CHEMBL331556 | — | — | 1 | 5.89 |
| CHEMBL118700 | — | — | 1 | 5.66 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.24 |
| CHEMBL41779 | — | — | 1 | 5.17 |
| CHEMBL119615 | — | — | 1 | 5.17 |
| CHEMBL120706 | — | — | 1 | 4.82 |
| CHEMBL119985 | — | — | 1 | - |
| CHEMBL325473 | — | — | 1 | - |
| CHEMBL442206 | — | — | 1 | - |
| CHEMBL118949 | — | — | 1 | - |
| CHEMBL119508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL310852 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL118240 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL118292 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL109815 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL333107 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL23957 | OXOTREMORINE METHIODIDE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL331556 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL118700 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL14 | CARBACHOL | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL41779 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL119615 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL120706 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL119985 | — | Ki | = | 1078000.0 | nM | - |
| CHEMBL325473 | — | Ki | = | 108300.0 | nM | - |
| CHEMBL442206 | — | Ki | = | 212000.0 | nM | - |
| CHEMBL118949 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL119508 | — | Ki | > | 109100.0 | nM | - |