Assay Detail
Binding
CHEMBL2327486
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Displacement of [3H]prazosine from rat alpha1D adrenoceptor expressed in CHO cells after 20 mins by scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel α₁-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.47 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.18 |
| CHEMBL319352 | — | — | 1 | 8.70 |
| CHEMBL1259203 | — | — | 1 | 8.60 |
| CHEMBL328187 | — | — | 1 | 8.07 |
| CHEMBL2326175 | — | — | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL319352 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1259203 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL328187 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL2326175 | — | Ki | = | 15.0 | nM | 7.82 |