Assay Detail
Binding
CHEMBL671250
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In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.06 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL351611 | — | — | 1 | 8.80 |
| CHEMBL165504 | — | — | 2 | 8.77 |
| CHEMBL350160 | — | — | 1 | 8.77 |
| CHEMBL163009 | — | — | 1 | 8.70 |
| CHEMBL159903 | — | — | 1 | 8.55 |
| CHEMBL161982 | — | — | 1 | 8.49 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.48 |
| CHEMBL66227 | — | — | 1 | 8.47 |
| CHEMBL166269 | — | — | 1 | 8.46 |
| CHEMBL162265 | — | — | 1 | 8.42 |
| CHEMBL166321 | — | — | 1 | 8.28 |
| CHEMBL351098 | — | — | 1 | 7.75 |
| CHEMBL349904 | — | — | 1 | 7.70 |
| CHEMBL349699 | — | — | 1 | 7.41 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.33 |
| CHEMBL162873 | — | — | 1 | 6.97 |
| CHEMBL165113 | — | — | 1 | 6.90 |
| CHEMBL161899 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL351611 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL165504 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL350160 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL163009 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL159903 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL161982 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL66227 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL166269 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL162265 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL165504 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL166321 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL351098 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL349904 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL349699 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL42 | CLOZAPINE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL162873 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL165113 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL161899 | — | Ki | = | 316.0 | nM | 6.50 |