Assay Detail
Binding
CHEMBL1261587
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Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells
37
Total Activities
37
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
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 | 37 | 9.42 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1259217 | — | — | 1 | 10.17 |
| CHEMBL1259113 | — | — | 1 | 10.09 |
| CHEMBL1258988 | — | — | 1 | 10.07 |
| CHEMBL1259144 | — | — | 1 | 10.06 |
| CHEMBL1259112 | — | — | 1 | 10.02 |
| CHEMBL1259145 | — | — | 1 | 9.92 |
| CHEMBL1259190 | — | — | 1 | 9.80 |
| CHEMBL1259216 | — | — | 1 | 9.77 |
| CHEMBL1259172 | — | — | 1 | 9.74 |
| CHEMBL1259023 | — | — | 1 | 9.72 |
| CHEMBL1259042 | — | — | 1 | 9.70 |
| CHEMBL319352 | — | — | 1 | 9.64 |
| CHEMBL1258987 | — | — | 1 | 9.62 |
| CHEMBL1259006 | — | — | 1 | 9.62 |
| CHEMBL1259232 | — | — | 1 | 9.59 |
| CHEMBL303313 | — | — | 1 | 9.55 |
| CHEMBL1259174 | — | — | 1 | 9.47 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.43 |
| CHEMBL1259231 | — | — | 1 | 9.39 |
| CHEMBL1259173 | — | — | 1 | 9.38 |
| CHEMBL1259189 | — | — | 1 | 9.37 |
| CHEMBL1259043 | — | — | 1 | 9.30 |
| CHEMBL1259005 | — | — | 1 | 9.28 |
| CHEMBL1259203 | — | — | 1 | 9.28 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 9.18 |
| CHEMBL1259188 | — | — | 1 | 9.18 |
| CHEMBL1259187 | — | — | 1 | 9.17 |
| CHEMBL64875 | — | — | 1 | 9.15 |
| CHEMBL1259062 | — | — | 1 | 9.06 |
| CHEMBL1259063 | — | — | 1 | 9.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1259217 | — | Ki | = | 0.067 | nM | 10.17 |
| CHEMBL1259113 | — | Ki | = | 0.082 | nM | 10.09 |
| CHEMBL1258988 | — | Ki | = | 0.086 | nM | 10.07 |
| CHEMBL1259144 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL1259112 | — | Ki | = | 0.096 | nM | 10.02 |
| CHEMBL1259145 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1259190 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1259216 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL1259172 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL1259023 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL1259042 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL319352 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL1258987 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL1259006 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL1259232 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL303313 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1259174 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL1259231 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL1259173 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL1259189 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL1259043 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1259005 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL1259203 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL64249 | CLOROTEPINE | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL1259188 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL1259187 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL64875 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL1259062 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL1259063 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1259097 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1259079 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1259158 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1259024 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1259080 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1259098 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL328187 | — | Ki | = | 3.0 | nM | 8.52 |