Assay Detail
Binding
CHEMBL4010175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET 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 | 9.14 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097330 | — | — | 1 | 9.96 |
| CHEMBL4090208 | — | — | 1 | 9.96 |
| CHEMBL4078348 | — | — | 1 | 9.92 |
| CHEMBL4071185 | — | — | 1 | 9.92 |
| CHEMBL4071868 | — | — | 1 | 9.80 |
| CHEMBL4098859 | — | — | 1 | 9.77 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 9.11 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.92 |
| CHEMBL4094869 | — | — | 1 | 8.77 |
| CHEMBL4098803 | — | — | 1 | 8.72 |
| CHEMBL4060461 | — | — | 2 | 8.70 |
| CHEMBL4102616 | — | — | 1 | 8.66 |
| CHEMBL4067439 | — | — | 1 | 8.59 |
| CHEMBL4069145 | — | — | 1 | 8.37 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097330 | — | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4090208 | — | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4078348 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4071185 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4071868 | — | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4098859 | — | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL59 | DOPAMINE | EC50 | = | 0.78 | nM | 9.11 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4094869 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4098803 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4060461 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4060461 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4102616 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4067439 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4069145 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 4.8 | nM | 8.32 |