Assay Detail
Binding
CHEMBL648041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-prazosin binding to Alpha-1 adrenergic receptor in rat frontal cortex homogenate
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.32 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333455 | — | — | 1 | 9.40 |
| CHEMBL368324 | — | — | 1 | 9.09 |
| CHEMBL118919 | — | — | 1 | 8.54 |
| CHEMBL2111783 | — | — | 2 | 8.35 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.05 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.92 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.84 |
| CHEMBL2111782 | — | — | 1 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333455 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL368324 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL118919 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2111783 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL42 | CLOZAPINE | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2111783 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL715 | OLANZAPINE | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL2111782 | — | Ki | = | 18.8 | nM | 7.73 |