Assay Detail
Binding
CHEMBL3386127
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.65 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 8.94 |
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 8.89 |
| CHEMBL3354068 | — | — | 1 | 6.84 |
| CHEMBL3354065 | — | — | 1 | 6.75 |
| CHEMBL3354067 | — | — | 1 | 6.45 |
| CHEMBL3354074 | — | — | 1 | 6.10 |
| CHEMBL3354075 | — | — | 1 | 6.09 |
| CHEMBL3354073 | — | — | 1 | 5.79 |
| CHEMBL3354069 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | IC50 | = | 1.148 | nM | 8.94 |
| CHEMBL569713 | SCOPOLAMINE | IC50 | = | 1.288 | nM | 8.89 |
| CHEMBL3354068 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL3354065 | — | IC50 | = | 177.83 | nM | 6.75 |
| CHEMBL3354067 | — | IC50 | = | 354.81 | nM | 6.45 |
| CHEMBL3354074 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3354075 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL3354073 | — | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL3354069 | — | IC50 | = | 95499.26 | nM | 4.02 |