Assay Detail
Binding
CHEMBL859710
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Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.26 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112065 | — | — | 1 | 9.52 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 9.39 |
| CHEMBL110365 | — | — | 1 | 9.28 |
| CHEMBL300780 | — | — | 1 | 8.77 |
| CHEMBL305362 | — | — | 1 | 8.70 |
| CHEMBL426414 | — | — | 1 | 8.47 |
| CHEMBL25236 | BP-897 | — | 1 | 8.34 |
| CHEMBL168357 | — | — | 1 | 8.16 |
| CHEMBL154508 | — | — | 1 | 8.10 |
| CHEMBL168948 | — | — | 1 | 7.97 |
| CHEMBL114541 | — | — | 1 | 7.92 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.80 |
| CHEMBL277301 | — | — | 1 | 7.69 |
| CHEMBL361228 | — | — | 1 | 7.64 |
| CHEMBL169766 | — | — | 1 | 7.49 |
| CHEMBL26188 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112065 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL240773 | QUINPIROLE | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL110365 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL300780 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL305362 | — | Ki | = | 1.98 | nM | 8.70 |
| CHEMBL426414 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL25236 | BP-897 | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL168357 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL154508 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL168948 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL114541 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL277301 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL361228 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL169766 | — | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL26188 | — | Ki | = | 128.0 | nM | 6.89 |