Assay Detail
Binding
CHEMBL3383647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
9
Total Activities
9
Compounds Tested
2
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 |
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 |
|---|---|---|---|
| EC50 | 6 | 6.87 | 7.80 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.80 |
| CHEMBL3354065 | — | — | 1 | 7.22 |
| CHEMBL3354073 | — | — | 1 | 6.95 |
| CHEMBL3354068 | — | — | 1 | 6.78 |
| CHEMBL3354074 | — | — | 1 | 6.64 |
| CHEMBL965 | CARBAMOYLCHOLINE | 4.0 | 1 | 5.80 |
| CHEMBL3354067 | — | — | 1 | - |
| CHEMBL3354069 | — | — | 1 | - |
| CHEMBL3354075 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3354065 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL3354073 | — | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL3354068 | — | EC50 | = | 165.96 | nM | 6.78 |
| CHEMBL3354074 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL965 | CARBAMOYLCHOLINE | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3354067 | — | pEC50 | - | — | - | |
| CHEMBL3354069 | — | pEC50 | - | — | - | |
| CHEMBL3354075 | — | pEC50 | - | — | - |