Assay Detail
Binding
CHEMBL2327489
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Displacement of [3H]prazosine from bovine alpha1A adrenoceptor expressed in BHK cells after 20 mins by scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Cell Type | BHK |
| 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 | 16 | 8.65 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2326175 | — | — | 1 | 9.80 |
| CHEMBL319352 | — | — | 1 | 9.64 |
| CHEMBL2325935 | — | — | 1 | 9.55 |
| CHEMBL2325926 | — | — | 1 | 9.49 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.43 |
| CHEMBL1259203 | — | — | 1 | 9.28 |
| CHEMBL2326176 | — | — | 1 | 9.27 |
| CHEMBL2325932 | — | — | 1 | 8.64 |
| CHEMBL2325928 | — | — | 1 | 8.57 |
| CHEMBL328187 | — | — | 1 | 8.52 |
| CHEMBL2325930 | — | — | 1 | 8.00 |
| CHEMBL2325934 | — | — | 1 | 7.72 |
| CHEMBL2325927 | — | — | 1 | 7.72 |
| CHEMBL2325933 | — | — | 1 | 7.66 |
| CHEMBL2325931 | — | — | 1 | 7.62 |
| CHEMBL2325929 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2326175 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL319352 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL2325935 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL2325926 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL1259203 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL2326176 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL2325932 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL2325928 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL328187 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2325930 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2325934 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2325927 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2325933 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2325931 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2325929 | — | Ki | = | 38.0 | nM | 7.42 |