Assay Detail
Binding
CHEMBL645992
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Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells
17
Total Activities
17
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 | 17 | 8.50 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.82 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.70 |
| CHEMBL64875 | — | — | 1 | 9.33 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.18 |
| CHEMBL97698 | — | — | 1 | 9.07 |
| CHEMBL98241 | — | — | 1 | 8.85 |
| CHEMBL319352 | — | — | 1 | 8.70 |
| CHEMBL97242 | — | — | 1 | 8.57 |
| CHEMBL318901 | — | — | 1 | 8.51 |
| CHEMBL93923 | — | — | 1 | 8.32 |
| CHEMBL327527 | — | — | 1 | 8.23 |
| CHEMBL313424 | — | — | 1 | 8.10 |
| CHEMBL420997 | — | — | 1 | 8.05 |
| CHEMBL97333 | — | — | 1 | 7.82 |
| CHEMBL317333 | — | — | 1 | 7.70 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 7.35 |
| CHEMBL95175 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL64875 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL97698 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL98241 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL319352 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL97242 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL318901 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL93923 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL327527 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL313424 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL420997 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL97333 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL317333 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL95175 | — | Ki | = | 52.0 | nM | 7.28 |