Assay Detail
Functional
CHEMBL4011214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 7.25 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3798179 | — | — | 1 | 9.52 |
| CHEMBL3797209 | — | — | 1 | 9.00 |
| CHEMBL4096422 | — | — | 1 | 8.51 |
| CHEMBL434665 | — | — | 1 | 8.04 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 7.96 |
| CHEMBL4059581 | — | — | 1 | 7.59 |
| CHEMBL419792 | SUMANIROLE | 3.0 | 1 | 7.49 |
| CHEMBL4068455 | — | — | 1 | 7.27 |
| CHEMBL3800633 | — | — | 1 | 7.18 |
| CHEMBL4077430 | — | — | 1 | 6.59 |
| CHEMBL4085282 | — | — | 1 | 6.55 |
| CHEMBL4093477 | — | — | 1 | 6.47 |
| CHEMBL4076129 | — | — | 1 | 6.15 |
| CHEMBL4095452 | — | — | 1 | 6.00 |
| CHEMBL4100322 | — | — | 1 | 5.91 |
| CHEMBL4100734 | — | — | 1 | 5.84 |
| CHEMBL4097572 | — | — | 1 | - |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3798179 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3797209 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4096422 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL434665 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4059581 | — | EC50 | = | 25.6 | nM | 7.59 |
| CHEMBL419792 | SUMANIROLE | EC50 | = | 32.2 | nM | 7.49 |
| CHEMBL4068455 | — | EC50 | = | 53.8 | nM | 7.27 |
| CHEMBL3800633 | — | EC50 | = | 65.9 | nM | 7.18 |
| CHEMBL4077430 | — | EC50 | = | 255.3 | nM | 6.59 |
| CHEMBL4085282 | — | EC50 | = | 279.3 | nM | 6.55 |
| CHEMBL4093477 | — | EC50 | = | 338.1 | nM | 6.47 |
| CHEMBL4076129 | — | EC50 | = | 709.6 | nM | 6.15 |
| CHEMBL4095452 | — | EC50 | = | 1004.6 | nM | 6.00 |
| CHEMBL4100322 | — | EC50 | = | 1227.4 | nM | 5.91 |
| CHEMBL4100734 | — | EC50 | = | 1458.8 | nM | 5.84 |
| CHEMBL4097572 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | > | 5000.0 | nM | - |