Assay Detail
Binding
CHEMBL4048908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human SP/Myc epitope-tagged muscarinic M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced RLuc8-fused Galphaq activation preincubated for 15 mins followed by carbachol induction measured after 2 mins by BRET assay
6
Total Activities
3
Compounds Tested
3
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 |
|---|---|---|---|
| Imax | 3 | - | - |
| IC50 | 2 | 7.12 | 8.66 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1187846 | — | — | 2 | 8.66 |
| CHEMBL4072818 | — | — | 2 | 5.58 |
| CHEMBL4085780 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1187846 | — | IC50 | = | 2.188 | nM | 8.66 |
| CHEMBL4072818 | — | IC50 | = | 2630.27 | nM | 5.58 |
| CHEMBL4085780 | — | pIC50 | - | — | - | |
| CHEMBL4072818 | — | Imax | = | 44.0 | % | - |
| CHEMBL4085780 | — | Imax | - | — | - | |
| CHEMBL1187846 | — | Imax | = | 71.0 | % | - |