Assay Detail
Binding
CHEMBL3372144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human D2LR expressed in CHOK1 cells assessed as inhibition of pergolide-induced beta-arrestin translocation by beta-galactosidase based beta-arrestin recruitment assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.15 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 9.80 |
| CHEMBL3322993 | — | — | 1 | 8.18 |
| CHEMBL3323017 | — | — | 1 | 7.66 |
| CHEMBL3323015 | — | — | 1 | 7.43 |
| CHEMBL3323016 | — | — | 1 | 7.31 |
| CHEMBL3322995 | — | — | 1 | 7.22 |
| CHEMBL3322994 | — | — | 1 | 7.04 |
| CHEMBL3322998 | — | — | 1 | 6.79 |
| CHEMBL3323112 | — | — | 1 | 6.66 |
| CHEMBL3323003 | — | — | 1 | 6.61 |
| CHEMBL3323011 | — | — | 1 | 6.58 |
| CHEMBL3323114 | — | — | 1 | 6.55 |
| CHEMBL3323013 | — | — | 1 | 6.52 |
| CHEMBL3323019 | — | — | 1 | 6.51 |
| CHEMBL3323012 | — | — | 1 | 6.38 |
| CHEMBL3323117 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3322993 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3323017 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3323015 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3323016 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3322995 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3322994 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3322998 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL3323112 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL3323003 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL3323011 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3323114 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3323013 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL3323019 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL3323012 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL3323117 | — | IC50 | > | 500.0 | nM | - |