Assay Detail
Binding
CHEMBL4011224
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human dopamine D2 receptor expressed in forskolin stimulated-HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 assessed as inhibition of quinpirole-induced Galphai1 activation by BRET assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine D2 Receptor (D2R) Biased Agonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.55 | 6.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3797209 | — | — | 1 | 6.03 |
| CHEMBL4093477 | — | — | 1 | 5.53 |
| CHEMBL4068455 | — | — | 1 | 5.44 |
| CHEMBL4077430 | — | — | 1 | 5.39 |
| CHEMBL4076129 | — | — | 1 | 5.35 |
| CHEMBL4097572 | — | — | 1 | - |
| CHEMBL4100734 | — | — | 1 | - |
| CHEMBL4100322 | — | — | 1 | - |
| CHEMBL4085282 | — | — | 1 | - |
| CHEMBL4095452 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3797209 | — | IC50 | = | 931.1 | nM | 6.03 |
| CHEMBL4093477 | — | IC50 | = | 2971.7 | nM | 5.53 |
| CHEMBL4068455 | — | IC50 | = | 3647.5 | nM | 5.44 |
| CHEMBL4077430 | — | IC50 | = | 4102.0 | nM | 5.39 |
| CHEMBL4076129 | — | IC50 | = | 4487.5 | nM | 5.35 |
| CHEMBL4097572 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4100734 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4100322 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4085282 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4095452 | — | IC50 | > | 5000.0 | nM | - |