Assay Detail
Binding
CHEMBL4011222
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Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 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 | 6.46 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3797209 | — | — | 1 | 7.78 |
| CHEMBL434665 | — | — | 1 | 6.95 |
| CHEMBL3798179 | — | — | 1 | 6.90 |
| CHEMBL3800633 | — | — | 1 | 6.79 |
| CHEMBL4068455 | — | — | 1 | 6.73 |
| CHEMBL4096422 | — | — | 1 | 6.72 |
| CHEMBL4059581 | — | — | 1 | 6.71 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 6.45 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 6.26 |
| CHEMBL4100734 | — | — | 1 | 6.24 |
| CHEMBL4085282 | — | — | 1 | 6.17 |
| CHEMBL4077430 | — | — | 1 | 6.15 |
| CHEMBL4093477 | — | — | 1 | 5.94 |
| CHEMBL4100322 | — | — | 1 | 5.73 |
| CHEMBL4095452 | — | — | 1 | 5.40 |
| CHEMBL4076129 | — | — | 1 | - |
| CHEMBL4097572 | — | — | 1 | - |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3797209 | — | EC50 | = | 16.8 | nM | 7.78 |
| CHEMBL434665 | — | EC50 | = | 111.2 | nM | 6.95 |
| CHEMBL3798179 | — | EC50 | = | 124.7 | nM | 6.90 |
| CHEMBL3800633 | — | EC50 | = | 163.3 | nM | 6.79 |
| CHEMBL4068455 | — | EC50 | = | 184.9 | nM | 6.73 |
| CHEMBL4096422 | — | EC50 | = | 188.8 | nM | 6.72 |
| CHEMBL4059581 | — | EC50 | = | 194.5 | nM | 6.71 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 353.2 | nM | 6.45 |
| CHEMBL419792 | SUMANIROLE | EC50 | = | 543.3 | nM | 6.26 |
| CHEMBL4100734 | — | EC50 | = | 570.2 | nM | 6.24 |
| CHEMBL4085282 | — | EC50 | = | 677.6 | nM | 6.17 |
| CHEMBL4077430 | — | EC50 | = | 712.9 | nM | 6.15 |
| CHEMBL4093477 | — | EC50 | = | 1153.5 | nM | 5.94 |
| CHEMBL4100322 | — | EC50 | = | 1853.5 | nM | 5.73 |
| CHEMBL4095452 | — | EC50 | = | 3981.1 | nM | 5.40 |
| CHEMBL4076129 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL4097572 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | > | 5000.0 | nM | - |