Assay Detail
Binding
CHEMBL4011220
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Antagonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as reduction in quinpirole-mediated beta-arrestin 2 recruitment preincubated for 15 mins followed by quinpirole addition measured for 1 sec 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 | 6.48 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3797209 | — | — | 1 | 6.80 |
| CHEMBL4068455 | — | — | 1 | 6.15 |
| CHEMBL4097572 | — | — | 1 | - |
| CHEMBL4076129 | — | — | 1 | - |
| CHEMBL4077430 | — | — | 1 | - |
| CHEMBL4100734 | — | — | 1 | - |
| CHEMBL4100322 | — | — | 1 | - |
| CHEMBL4085282 | — | — | 1 | - |
| CHEMBL4095452 | — | — | 1 | - |
| CHEMBL4093477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3797209 | — | IC50 | = | 157.8 | nM | 6.80 |
| CHEMBL4068455 | — | IC50 | = | 712.9 | nM | 6.15 |
| CHEMBL4097572 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4076129 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4077430 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4100734 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4100322 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4085282 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4095452 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4093477 | — | IC50 | > | 5000.0 | nM | - |