Assay Detail
Functional
CHEMBL853697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
11
Total Activities
11
Compounds Tested
1
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 |
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 |
|---|---|---|---|
| EC50 | 11 | 6.39 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335542 | — | — | 1 | 8.10 |
| CHEMBL216927 | — | — | 1 | 7.20 |
| CHEMBL216928 | — | — | 1 | 6.60 |
| CHEMBL386983 | — | — | 1 | 6.60 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.50 |
| CHEMBL219118 | — | — | 1 | 6.30 |
| CHEMBL216983 | — | — | 1 | 6.10 |
| CHEMBL218755 | — | — | 1 | 6.10 |
| CHEMBL373888 | — | — | 1 | 6.00 |
| CHEMBL376295 | — | — | 1 | 5.50 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335542 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL216927 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL216928 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL386983 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL21536 | XANOMELINE | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL219118 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL216983 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL218755 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL373888 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL376295 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL14 | CARBACHOL | EC50 | = | 5011.87 | nM | 5.30 |