Assay Detail
Binding
CHEMBL708731
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Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Submaxillary gland |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL320) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 9.21 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.92 |
| CHEMBL558910 | — | — | 1 | 9.80 |
| CHEMBL2112942 | — | — | 1 | 9.57 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL558910 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL2112942 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 28.0 | nM | 7.55 |