Assay Detail
Binding
CHEMBL649214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | mesocricetus auratus (golden hamster) |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Alpha-1B adrenergic receptor (CHEMBL3122) ↗| Type | SINGLE PROTEIN |
| Organism | Mesocricetus auratus |
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 | 8.60 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303313 | — | — | 1 | 9.66 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.48 |
| CHEMBL318901 | — | — | 1 | 9.41 |
| CHEMBL97698 | — | — | 1 | 9.34 |
| CHEMBL97242 | — | — | 1 | 9.16 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 9.08 |
| CHEMBL64875 | — | — | 1 | 9.03 |
| CHEMBL319352 | — | — | 1 | 8.96 |
| CHEMBL95175 | — | — | 1 | 8.74 |
| CHEMBL313424 | — | — | 1 | 8.49 |
| CHEMBL420997 | — | — | 1 | 8.49 |
| CHEMBL93923 | — | — | 1 | 8.40 |
| CHEMBL317333 | — | — | 1 | 8.34 |
| CHEMBL327527 | — | — | 1 | 8.16 |
| CHEMBL97333 | — | — | 1 | 8.06 |
| CHEMBL98241 | — | — | 1 | 6.77 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303313 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL318901 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL97698 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL97242 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL2 | PRAZOSIN | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL64875 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL319352 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL95175 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL313424 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL420997 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL93923 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL317333 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL327527 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL97333 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL98241 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL597 | PHENTOLAMINE | Ki | = | 220.0 | nM | 6.66 |