Assay Detail
ADMET
CHEMBL4046983
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Agonist activity at human D2SR expressed in HEK293 cell membranes co-expressing PTX insensitive variant of Galphao1 incubated for 30 mins by [35S]GTP-gammaS binding assay
16
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 6.67 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068561 | — | — | 2 | 7.26 |
| CHEMBL4063145 | — | — | 2 | 6.58 |
| CHEMBL589 | ROPINIROLE | 4.0 | 1 | 6.48 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 6.44 |
| CHEMBL4087217 | — | — | 1 | 6.01 |
| CHEMBL4103639 | — | — | 1 | - |
| CHEMBL4079375 | — | — | 1 | - |
| CHEMBL4095881 | — | — | 1 | - |
| CHEMBL4085752 | — | — | 2 | - |
| CHEMBL4094407 | — | — | 1 | - |
| CHEMBL4102646 | — | — | 1 | - |
| CHEMBL4092462 | — | — | 1 | - |
| CHEMBL4065797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068561 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4068561 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4063145 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL589 | ROPINIROLE | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4087217 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4103639 | — | EC50 | - | — | - | |
| CHEMBL4079375 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4095881 | — | EC50 | - | — | - | |
| CHEMBL4063145 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL4085752 | — | EC50 | - | — | - | |
| CHEMBL4085752 | — | EC50 | - | — | - | |
| CHEMBL4094407 | — | EC50 | - | — | - | |
| CHEMBL4102646 | — | EC50 | - | — | - | |
| CHEMBL4092462 | — | EC50 | - | — | - | |
| CHEMBL4065797 | — | EC50 | - | — | - |