Assay Detail
Binding
CHEMBL644957
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards alpha-1 adrenergic receptor in rat frontal cortex homogenate using of [3H]prazosin as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.43 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367045 | — | — | 1 | 9.30 |
| CHEMBL368324 | — | — | 1 | 9.09 |
| CHEMBL176169 | — | — | 1 | 8.38 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.05 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.92 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367045 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL368324 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL176169 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL42 | CLOZAPINE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL715 | OLANZAPINE | Ki | = | 15.0 | nM | 7.82 |