Assay Detail
Functional
CHEMBL3293229
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Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
32
Total Activities
15
Compounds Tested
1
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 | 32 | 7.74 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3287397 | — | — | 2 | 8.72 |
| CHEMBL3287402 | — | — | 2 | 8.30 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 8.24 |
| CHEMBL3287396 | — | — | 2 | 8.23 |
| CHEMBL59 | DOPAMINE | 4.0 | 2 | 8.03 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 2 | 8.01 |
| CHEMBL3287405 | — | — | 2 | 7.92 |
| CHEMBL3287404 | — | — | 2 | 7.82 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 2 | 7.71 |
| CHEMBL3287403 | — | — | 4 | 7.41 |
| CHEMBL3287392 | — | — | 2 | 7.39 |
| CHEMBL3287406 | — | — | 2 | 7.39 |
| CHEMBL3287395 | — | — | 2 | 7.25 |
| CHEMBL3287390 | — | — | 2 | 7.18 |
| CHEMBL3287399 | — | — | 2 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3287397 | — | EC50 | = | 1.905 | nM | 8.72 |
| CHEMBL3287397 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3287402 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3287402 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 5.754 | nM | 8.24 |
| CHEMBL2028019 | CARIPRAZINE | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3287396 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3287396 | — | EC50 | = | 5.888 | nM | 8.23 |
| CHEMBL59 | DOPAMINE | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL59 | DOPAMINE | EC50 | = | 9.333 | nM | 8.03 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL3287405 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3287405 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL3287404 | — | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL3287404 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL1112 | ARIPIPRAZOLE | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3287403 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3287403 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL3287392 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3287406 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3287406 | — | EC50 | = | 40.74 | nM | 7.39 |
| CHEMBL3287392 | — | EC50 | = | 41.69 | nM | 7.38 |
| CHEMBL3287403 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3287403 | — | EC50 | = | 42.66 | nM | 7.37 |
| CHEMBL3287395 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL3287395 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3287390 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3287390 | — | EC50 | = | 66.07 | nM | 7.18 |
| CHEMBL3287399 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3287399 | — | EC50 | = | 112.2 | nM | 6.95 |