Assay Detail
Functional
CHEMBL4010161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
40
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 | 40 | 7.83 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069145 | — | — | 2 | 9.49 |
| CHEMBL4078348 | — | — | 2 | 9.37 |
| CHEMBL4097330 | — | — | 2 | 9.32 |
| CHEMBL4069091 | — | — | 1 | 8.42 |
| CHEMBL4098236 | — | — | 2 | 8.11 |
| CHEMBL4087187 | — | — | 2 | 8.02 |
| CHEMBL4060461 | — | — | 4 | 7.75 |
| CHEMBL4067439 | — | — | 2 | 7.73 |
| CHEMBL4063235 | — | — | 2 | 7.72 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 2 | 7.71 |
| CHEMBL4099711 | — | — | 2 | 7.57 |
| CHEMBL4098803 | — | — | 2 | 7.54 |
| CHEMBL4079301 | — | — | 2 | 7.51 |
| CHEMBL4060403 | — | — | 1 | 7.43 |
| CHEMBL4096353 | — | — | 1 | 7.42 |
| CHEMBL4070091 | — | — | 1 | 7.38 |
| CHEMBL4091155 | — | — | 1 | 7.35 |
| CHEMBL4072821 | — | — | 2 | 7.30 |
| CHEMBL4080762 | — | — | 2 | 7.25 |
| CHEMBL4091064 | — | — | 1 | 7.21 |
| CHEMBL4063282 | — | — | 1 | 7.18 |
| CHEMBL4105030 | — | — | 2 | 7.16 |
| CHEMBL4088639 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069145 | — | EC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4069145 | — | EC50 | = | 0.3236 | nM | 9.49 |
| CHEMBL4078348 | — | EC50 | = | 0.4266 | nM | 9.37 |
| CHEMBL4078348 | — | EC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4097330 | — | EC50 | = | 0.48 | nM | 9.32 |
| CHEMBL4097330 | — | EC50 | = | 0.4786 | nM | 9.32 |
| CHEMBL4069091 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4098236 | — | EC50 | = | 7.762 | nM | 8.11 |
| CHEMBL4098236 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4087187 | — | EC50 | = | 9.55 | nM | 8.02 |
| CHEMBL4087187 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4060461 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4060461 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL4067439 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL4063235 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4067439 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4063235 | — | EC50 | = | 19.05 | nM | 7.72 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4099711 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL4099711 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4098803 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4098803 | — | EC50 | = | 28.84 | nM | 7.54 |
| CHEMBL4079301 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4079301 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL4060403 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4096353 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4060461 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4060461 | — | EC50 | = | 40.74 | nM | 7.39 |
| CHEMBL4070091 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4091155 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4072821 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4072821 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4080762 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4080762 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4091064 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4063282 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4105030 | — | EC50 | = | 69.18 | nM | 7.16 |
| CHEMBL4105030 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4088639 | — | EC50 | = | 79.0 | nM | 7.10 |