Assay Detail
Binding
CHEMBL695164
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In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 8.02 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL176169 | — | — | 1 | 8.57 |
| CHEMBL367045 | — | — | 1 | 8.57 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.54 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.37 |
| CHEMBL368324 | — | — | 1 | 7.67 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL176169 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL367045 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL42 | CLOZAPINE | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL715 | OLANZAPINE | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL368324 | — | Ki | = | 21.3 | nM | 7.67 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 384.0 | nM | 6.42 |