Assay Detail
Functional
CHEMBL939028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 |
|---|---|---|---|
| EC50 | 2 | 5.55 | 5.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL503735 | — | — | 1 | 5.55 |
| CHEMBL523685 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL503735 | — | EC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL523685 | — | EC50 | - | — | - |