Assay Detail
Binding
CHEMBL4010181
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Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 7.95 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4078348 | — | — | 1 | 8.89 |
| CHEMBL4071868 | — | — | 1 | 8.82 |
| CHEMBL4098859 | — | — | 1 | 8.77 |
| CHEMBL4090208 | — | — | 1 | 8.54 |
| CHEMBL4097330 | — | — | 1 | 8.52 |
| CHEMBL4071185 | — | — | 1 | 8.52 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 7.19 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 6.81 |
| CHEMBL4094869 | — | — | 1 | 6.79 |
| CHEMBL4102616 | — | — | 1 | 6.66 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
| CHEMBL4098803 | — | — | 1 | - |
| CHEMBL4067439 | — | — | 1 | - |
| CHEMBL4069145 | — | — | 1 | - |
| CHEMBL4060461 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4078348 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4071868 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4098859 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4090208 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4097330 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4071185 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL59 | DOPAMINE | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4094869 | — | EC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4102616 | — | EC50 | = | 218.0 | nM | 6.66 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | - | — | - | |
| CHEMBL4098803 | — | EC50 | - | — | - | |
| CHEMBL4067439 | — | EC50 | - | — | - | |
| CHEMBL4069145 | — | EC50 | - | — | - | |
| CHEMBL4060461 | — | EC50 | - | — | - | |
| CHEMBL4060461 | — | EC50 | - | — | - |