Assay Detail
Binding
CHEMBL4048907
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
3
Total Activities
3
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 |
Publication
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.31 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072818 | — | — | 1 | 6.73 |
| CHEMBL4085780 | — | — | 1 | 6.19 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072818 | — | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL4085780 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL14 | CARBACHOL | EC50 | = | 954.99 | nM | 6.02 |