Assay Detail
Functional
CHEMBL853706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human M2 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
10
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| IC50 | 7 | 7.17 | 9.30 |
| Log IC50 | 2 | - | - |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216927 | — | — | 1 | 9.30 |
| CHEMBL216983 | — | — | 1 | 8.10 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.20 |
| CHEMBL373888 | — | — | 1 | 7.10 |
| CHEMBL216928 | — | — | 1 | 6.60 |
| CHEMBL386983 | — | — | 1 | 6.40 |
| CHEMBL218755 | — | — | 1 | 5.50 |
| CHEMBL219118 | — | — | 1 | - |
| CHEMBL376295 | — | — | 1 | - |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216927 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL216983 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL14 | CARBACHOL | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL373888 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL216928 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL386983 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL218755 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL219118 | — | Activity | - | — | - | |
| CHEMBL376295 | — | Log IC50 | - | — | - | |
| CHEMBL21536 | XANOMELINE | Log IC50 | - | — | - |