Assay Detail
Binding
CHEMBL1261588
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Displacement of [3H]prozosin from hamster cloned alpha-1b receptor
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mesocricetus auratus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Alpha-1B adrenergic receptor (CHEMBL3122) ↗| Type | SINGLE PROTEIN |
| Organism | Mesocricetus auratus |
Publication
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 9.23 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1259113 | — | — | 1 | 10.41 |
| CHEMBL1259144 | — | — | 1 | 10.09 |
| CHEMBL1259112 | — | — | 1 | 10.06 |
| CHEMBL1259042 | — | — | 1 | 9.77 |
| CHEMBL1259190 | — | — | 1 | 9.70 |
| CHEMBL1258987 | — | — | 1 | 9.70 |
| CHEMBL1259232 | — | — | 1 | 9.60 |
| CHEMBL1259023 | — | — | 1 | 9.59 |
| CHEMBL1259189 | — | — | 1 | 9.57 |
| CHEMBL1259145 | — | — | 1 | 9.51 |
| CHEMBL1259231 | — | — | 1 | 9.49 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.48 |
| CHEMBL1259216 | — | — | 1 | 9.46 |
| CHEMBL1259217 | — | — | 1 | 9.44 |
| CHEMBL1259043 | — | — | 1 | 9.40 |
| CHEMBL1259174 | — | — | 1 | 9.38 |
| CHEMBL64875 | — | — | 1 | 9.38 |
| CHEMBL1259158 | — | — | 1 | 9.28 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 9.25 |
| CHEMBL1259188 | — | — | 1 | 9.25 |
| CHEMBL1259005 | — | — | 1 | 9.14 |
| CHEMBL1259079 | — | — | 1 | 9.09 |
| CHEMBL1259173 | — | — | 1 | 9.05 |
| CHEMBL1259063 | — | — | 1 | 9.02 |
| CHEMBL319352 | — | — | 1 | 8.96 |
| CHEMBL1259172 | — | — | 1 | 8.96 |
| CHEMBL1258988 | — | — | 1 | 8.92 |
| CHEMBL1259080 | — | — | 1 | 8.92 |
| CHEMBL1259006 | — | — | 1 | 8.80 |
| CHEMBL1259098 | — | — | 1 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1259113 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL1259144 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL1259112 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL1259042 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL1259190 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1258987 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1259232 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1259023 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL1259189 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL1259145 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL1259231 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL1259216 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL1259217 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL1259043 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1259174 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL64875 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL1259158 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL1259188 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL64249 | CLOROTEPINE | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL1259005 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL1259079 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL1259173 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1259063 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL319352 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1259172 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1258988 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1259080 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1259006 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1259098 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1259203 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1259024 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1259187 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1259062 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL328187 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1259097 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL1259128 | — | Ki | - | — | - | |
| CHEMBL1259129 | — | Ki | - | — | - | |
| CHEMBL303313 | — | Ki | = | 0.009 | nM | - |