Assay Detail
Functional
CHEMBL957809
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine potency at 30 uM by calcium mobilization-based ACh concentration-response curve assay relative to control
3
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| FC | 1 | - | - |
| Activity | 1 | - | - |
| Ki | 1 | 9.68 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.68 |
| CHEMBL466253 | — | — | 1 | - |
| CHEMBL523685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL466253 | — | FC | = | 14.0 | — | - |
| CHEMBL523685 | — | Activity | - | — | - |