Assay Detail
Binding
CHEMBL3372143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against D3R in human U2OS cells assessed as inhibition of (+)-PD128907-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 | U2OS |
| 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 | 8.57 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 10.22 |
| CHEMBL3322994 | — | — | 1 | 9.70 |
| CHEMBL3323016 | — | — | 1 | 9.52 |
| CHEMBL3323017 | — | — | 1 | 9.52 |
| CHEMBL3323015 | — | — | 1 | 9.40 |
| CHEMBL3323011 | — | — | 1 | 9.22 |
| CHEMBL3322993 | — | — | 1 | 9.15 |
| CHEMBL3322995 | — | — | 1 | 8.74 |
| CHEMBL3323012 | — | — | 1 | 8.25 |
| CHEMBL3323117 | — | — | 1 | 8.17 |
| CHEMBL3323112 | — | — | 1 | 8.14 |
| CHEMBL3323013 | — | — | 1 | 8.07 |
| CHEMBL3323019 | — | — | 1 | 7.85 |
| CHEMBL3323114 | — | — | 1 | 7.54 |
| CHEMBL3322998 | — | — | 1 | 7.28 |
| CHEMBL3323003 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3322994 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3323016 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3323017 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3323015 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3323011 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3322993 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3322995 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3323012 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3323117 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3323112 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3323013 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3323019 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3323114 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3322998 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3323003 | — | IC50 | = | 409.0 | nM | 6.39 |