Assay Detail
Binding
CHEMBL649634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards alpha-2 adrenergic receptor in rat frontal cortex homogenate using of [3H]clonidine as radioligand
5
Total Activities
5
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 | 5 | 6.13 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.89 |
| CHEMBL368324 | — | — | 1 | 6.68 |
| CHEMBL367045 | — | — | 1 | 5.99 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.57 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL368324 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL367045 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL715 | OLANZAPINE | Ki | = | 2870.0 | nM | 5.54 |