Assay Detail
Binding
CHEMBL1261592
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Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 | 16 | 7.91 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 9.72 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 9.29 |
| CHEMBL1259174 | — | — | 1 | 8.60 |
| CHEMBL1259173 | — | — | 1 | 8.44 |
| CHEMBL1259189 | — | — | 1 | 8.35 |
| CHEMBL1259190 | — | — | 1 | 8.30 |
| CHEMBL64875 | — | — | 1 | 7.92 |
| CHEMBL303313 | — | — | 1 | 7.82 |
| CHEMBL1259172 | — | — | 1 | 7.19 |
| CHEMBL1259187 | — | — | 1 | 7.19 |
| CHEMBL319352 | — | — | 1 | 6.30 |
| CHEMBL328187 | — | — | 1 | 5.82 |
| CHEMBL1259144 | — | — | 1 | - |
| CHEMBL1259145 | — | — | 1 | - |
| CHEMBL1259188 | — | — | 1 | - |
| CHEMBL1259203 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64249 | CLOROTEPINE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL12713 | SERTINDOLE | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL1259174 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1259173 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1259189 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1259190 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL64875 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL303313 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1259172 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1259187 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL319352 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL328187 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1259144 | — | Ki | - | — | - | |
| CHEMBL1259145 | — | Ki | - | — | - | |
| CHEMBL1259188 | — | Ki | - | — | - | |
| CHEMBL1259203 | — | Ki | - | — | - |