Assay Detail
Binding
CHEMBL4011218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
18
Total Activities
18
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 |
|---|---|---|---|
| EC50 | 18 | 6.49 | 7.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3797209 | — | — | 1 | 7.69 |
| CHEMBL4096422 | — | — | 1 | 7.13 |
| CHEMBL434665 | — | — | 1 | 6.91 |
| CHEMBL4085282 | — | — | 1 | 6.86 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 6.83 |
| CHEMBL3798179 | — | — | 1 | 6.81 |
| CHEMBL4059581 | — | — | 1 | 6.71 |
| CHEMBL3800633 | — | — | 1 | 6.68 |
| CHEMBL4068455 | — | — | 1 | 6.57 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 6.30 |
| CHEMBL4093477 | — | — | 1 | 6.03 |
| CHEMBL4077430 | — | — | 1 | 5.82 |
| CHEMBL4095452 | — | — | 1 | 5.73 |
| CHEMBL4100322 | — | — | 1 | 5.61 |
| CHEMBL4076129 | — | — | 1 | 5.60 |
| CHEMBL4100734 | — | — | 1 | - |
| CHEMBL4097572 | — | — | 1 | - |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3797209 | — | EC50 | = | 20.5 | nM | 7.69 |
| CHEMBL4096422 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL434665 | — | EC50 | = | 121.9 | nM | 6.91 |
| CHEMBL4085282 | — | EC50 | = | 139.0 | nM | 6.86 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 147.6 | nM | 6.83 |
| CHEMBL3798179 | — | EC50 | = | 154.5 | nM | 6.81 |
| CHEMBL4059581 | — | EC50 | = | 196.8 | nM | 6.71 |
| CHEMBL3800633 | — | EC50 | = | 209.9 | nM | 6.68 |
| CHEMBL4068455 | — | EC50 | = | 269.8 | nM | 6.57 |
| CHEMBL419792 | SUMANIROLE | EC50 | = | 501.2 | nM | 6.30 |
| CHEMBL4093477 | — | EC50 | = | 944.0 | nM | 6.03 |
| CHEMBL4077430 | — | EC50 | = | 1499.7 | nM | 5.82 |
| CHEMBL4095452 | — | EC50 | = | 1870.7 | nM | 5.73 |
| CHEMBL4100322 | — | EC50 | = | 2471.7 | nM | 5.61 |
| CHEMBL4076129 | — | EC50 | = | 2529.3 | nM | 5.60 |
| CHEMBL4100734 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4097572 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | > | 5000.0 | nM | - |