Assay Detail
Functional
CHEMBL871304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | L929 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the binding and activity at muscarinic receptor subtypes and chimeras.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Log EC50 | 7 | - | - |
| EC50 | 3 | 5.70 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216928 | — | — | 1 | 6.20 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.00 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 4.90 |
| CHEMBL219118 | — | — | 1 | - |
| CHEMBL376295 | — | — | 1 | - |
| CHEMBL216983 | — | — | 1 | - |
| CHEMBL386983 | — | — | 1 | - |
| CHEMBL216927 | — | — | 1 | - |
| CHEMBL218755 | — | — | 1 | - |
| CHEMBL373888 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216928 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL14 | CARBACHOL | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL21536 | XANOMELINE | EC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL219118 | — | Log EC50 | - | — | - | |
| CHEMBL376295 | — | Log EC50 | - | — | - | |
| CHEMBL216983 | — | Log EC50 | - | — | - | |
| CHEMBL386983 | — | Log EC50 | - | — | - | |
| CHEMBL216927 | — | Log EC50 | - | — | - | |
| CHEMBL218755 | — | Log EC50 | - | — | - | |
| CHEMBL373888 | — | Log EC50 | - | — | - |