Assay Detail
Binding
CHEMBL674985
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Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3
14
Total Activities
14
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 and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.40 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 8.59 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.57 |
| CHEMBL98241 | — | — | 1 | 7.23 |
| CHEMBL318901 | — | — | 1 | 6.23 |
| CHEMBL317333 | — | — | 1 | 6.17 |
| CHEMBL420997 | — | — | 1 | 5.92 |
| CHEMBL319352 | — | — | 1 | 5.92 |
| CHEMBL97242 | — | — | 1 | 5.85 |
| CHEMBL93923 | — | — | 1 | 5.68 |
| CHEMBL95175 | — | — | 1 | 5.55 |
| CHEMBL327527 | — | — | 1 | 5.54 |
| CHEMBL313424 | — | — | 1 | 5.51 |
| CHEMBL97333 | — | — | 1 | - |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL98241 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL318901 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL317333 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL420997 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL319352 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL97242 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL93923 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL95175 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL327527 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL313424 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL97333 | — | Ki | > | 7100.0 | nM | - |
| CHEMBL2 | PRAZOSIN | Ki | > | 7100.0 | nM | - |