Assay Detail
Binding
CHEMBL3293231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 12 | 8.06 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 9.15 |
| CHEMBL2028019 | CARIPRAZINE | 4.0 | 2 | 8.78 |
| CHEMBL3287403 | — | — | 2 | 8.42 |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 2 | 7.96 |
| CHEMBL3287402 | — | — | 2 | 7.66 |
| CHEMBL3287397 | — | — | 2 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2028019 | CARIPRAZINE | IC50 | = | 1.66 | nM | 8.78 |
| CHEMBL2028019 | CARIPRAZINE | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3287403 | — | IC50 | = | 3.802 | nM | 8.42 |
| CHEMBL3287403 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | = | 11.22 | nM | 7.95 |
| CHEMBL3287402 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3287402 | — | IC50 | = | 28.84 | nM | 7.54 |
| CHEMBL3287397 | — | IC50 | = | 363.08 | nM | 6.44 |
| CHEMBL3287397 | — | IC50 | = | 360.0 | nM | 6.44 |