Assay Detail
Functional
CHEMBL855411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| 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 |
|---|---|---|---|
| IC50 | 9 | 6.12 | 7.90 |
| Log IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216927 | — | — | 1 | 7.90 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.60 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.30 |
| CHEMBL386983 | — | — | 1 | 6.40 |
| CHEMBL216928 | — | — | 1 | 5.90 |
| CHEMBL219118 | — | — | 1 | 5.20 |
| CHEMBL218755 | — | — | 1 | 5.10 |
| CHEMBL373888 | — | — | 1 | 5.10 |
| CHEMBL216983 | — | — | 1 | 4.60 |
| CHEMBL376295 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216927 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL14 | CARBACHOL | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL386983 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL216928 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL219118 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL218755 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL373888 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL216983 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL376295 | — | Log IC50 | - | — | - |