Assay Detail
Binding
CHEMBL4048906
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Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
10
Total Activities
5
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
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 |
|---|---|---|---|
| IC50 | 5 | 7.56 | 9.14 |
| Imax | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085780 | — | — | 2 | 9.14 |
| CHEMBL3354065 | — | — | 2 | 8.22 |
| CHEMBL267014 | L-745870 | — | 2 | 7.37 |
| CHEMBL3354073 | — | — | 2 | 6.82 |
| CHEMBL4072818 | — | — | 2 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085780 | — | IC50 | = | 0.7244 | nM | 9.14 |
| CHEMBL3354065 | — | IC50 | = | 6.026 | nM | 8.22 |
| CHEMBL267014 | L-745870 | IC50 | = | 42.66 | nM | 7.37 |
| CHEMBL3354073 | — | IC50 | = | 151.36 | nM | 6.82 |
| CHEMBL4072818 | — | IC50 | = | 575.44 | nM | 6.24 |
| CHEMBL3354065 | — | Imax | = | 72.0 | % | - |
| CHEMBL3354073 | — | Imax | = | 70.0 | % | - |
| CHEMBL4072818 | — | Imax | = | 94.0 | % | - |
| CHEMBL4085780 | — | Imax | = | 69.0 | % | - |
| CHEMBL267014 | L-745870 | Imax | = | 60.0 | % | - |