Assay Detail
Binding
CHEMBL4010171
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 Galphai3 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 | 8.47 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071185 | — | — | 1 | 9.14 |
| CHEMBL4090208 | — | — | 1 | 9.13 |
| CHEMBL4078348 | — | — | 1 | 9.10 |
| CHEMBL4097330 | — | — | 1 | 9.09 |
| CHEMBL4071868 | — | — | 1 | 9.03 |
| CHEMBL4098859 | — | — | 1 | 9.02 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 8.35 |
| CHEMBL4098803 | — | — | 1 | 8.30 |
| CHEMBL4060461 | — | — | 2 | 8.24 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.23 |
| CHEMBL4102616 | — | — | 1 | 8.02 |
| CHEMBL4094869 | — | — | 1 | 8.01 |
| CHEMBL4067439 | — | — | 1 | 8.00 |
| CHEMBL4069145 | — | — | 1 | 7.88 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | 7.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071185 | — | EC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4090208 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4078348 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4097330 | — | EC50 | = | 0.81 | nM | 9.09 |
| CHEMBL4071868 | — | EC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4098859 | — | EC50 | = | 0.96 | nM | 9.02 |
| CHEMBL59 | DOPAMINE | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4098803 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4060461 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4060461 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4102616 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4094869 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4067439 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4069145 | — | EC50 | = | 13.1 | nM | 7.88 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 17.5 | nM | 7.76 |