Assay Detail
Binding
CHEMBL647135
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Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | BHK |
| 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 | 8.78 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319352 | — | — | 1 | 9.64 |
| CHEMBL97242 | — | — | 1 | 9.46 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.43 |
| CHEMBL93923 | — | — | 1 | 9.31 |
| CHEMBL303313 | — | — | 1 | 9.25 |
| CHEMBL95175 | — | — | 1 | 9.25 |
| CHEMBL313424 | — | — | 1 | 9.21 |
| CHEMBL327527 | — | — | 1 | 9.10 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.03 |
| CHEMBL420997 | — | — | 1 | 9.00 |
| CHEMBL318901 | — | — | 1 | 8.89 |
| CHEMBL64875 | — | — | 1 | 8.85 |
| CHEMBL97333 | — | — | 1 | 8.66 |
| CHEMBL317333 | — | — | 1 | 8.41 |
| CHEMBL97698 | — | — | 1 | 8.29 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 8.17 |
| CHEMBL98241 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319352 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL97242 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL93923 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL303313 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL95175 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL313424 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL327527 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL420997 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL318901 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL64875 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL97333 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL317333 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL97698 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL98241 | — | Ki | = | 5900.0 | nM | 5.23 |