Assay Detail
Binding
CHEMBL4046981
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Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay
16
Total Activities
13
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
β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.93 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068561 | — | — | 2 | 7.34 |
| CHEMBL4103639 | — | — | 1 | 7.29 |
| CHEMBL4079375 | — | — | 1 | 7.17 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 7.14 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 7.05 |
| CHEMBL4063145 | — | — | 2 | 6.96 |
| CHEMBL4087217 | — | — | 1 | 6.89 |
| CHEMBL4085752 | — | — | 2 | 6.77 |
| CHEMBL4102646 | — | — | 1 | 6.52 |
| CHEMBL4065797 | — | — | 1 | 5.96 |
| CHEMBL4095881 | — | — | 1 | - |
| CHEMBL4094407 | — | — | 1 | - |
| CHEMBL4092462 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068561 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4103639 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4079375 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4068561 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL589 | ROPINIROLE | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4063145 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4063145 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4087217 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4085752 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4102646 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4065797 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4095881 | — | EC50 | - | — | - | |
| CHEMBL4085752 | — | EC50 | - | — | - | |
| CHEMBL4094407 | — | EC50 | - | — | - | |
| CHEMBL4092462 | — | EC50 | - | — | - |