Assay Detail
Binding
CHEMBL745813
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In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB
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 |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.56 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.66 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.27 |
| CHEMBL368324 | — | — | 1 | 6.54 |
| CHEMBL367045 | — | — | 1 | 5.68 |
| CHEMBL176169 | — | — | 1 | 5.64 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL42 | CLOZAPINE | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL368324 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL367045 | — | Ki | = | 2070.0 | nM | 5.68 |
| CHEMBL176169 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL54 | HALOPERIDOL | Ki | > | 10000.0 | nM | - |