Assay Detail
Functional
CHEMBL3293227
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Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay
32
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Functionally selective dopamine D₂, D₃ receptor partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.50 | 7.01 |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3287406 | — | — | 2 | 7.01 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 6.96 |
| CHEMBL3287405 | — | — | 2 | 6.96 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 2 | 6.80 |
| CHEMBL3287390 | — | — | 2 | 6.75 |
| CHEMBL3287403 | — | — | 4 | 6.63 |
| CHEMBL3287399 | — | — | 2 | 6.47 |
| CHEMBL3287395 | — | — | 2 | 6.36 |
| CHEMBL59 | DOPAMINE | 4.0 | 2 | 6.33 |
| CHEMBL3287396 | — | — | 2 | 6.27 |
| CHEMBL3287397 | — | — | 2 | 6.19 |
| CHEMBL3287392 | — | — | 2 | 5.89 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 2 | 5.80 |
| CHEMBL3287402 | — | — | 2 | - |
| CHEMBL3287404 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3287406 | — | EC50 | = | 97.72 | nM | 7.01 |
| CHEMBL3287406 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3287405 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3287405 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3287390 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3287390 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL3287403 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL3287403 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3287403 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3287403 | — | EC50 | = | 275.42 | nM | 6.56 |
| CHEMBL3287399 | — | EC50 | = | 338.84 | nM | 6.47 |
| CHEMBL3287399 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3287395 | — | EC50 | = | 436.52 | nM | 6.36 |
| CHEMBL3287395 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL59 | DOPAMINE | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL59 | DOPAMINE | EC50 | = | 467.74 | nM | 6.33 |
| CHEMBL3287396 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3287396 | — | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL3287397 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3287397 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL3287392 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3287392 | — | EC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL3287404 | — | pEC50 | - | — | - | |
| CHEMBL3287402 | — | EC50 | - | — | - | |
| CHEMBL3287402 | — | pEC50 | - | — | - | |
| CHEMBL3287404 | — | EC50 | - | — | - |