Assay Detail
Binding
CHEMBL745671
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Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Frontal cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.32 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 7.66 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.26 |
| CHEMBL368324 | — | — | 1 | 6.54 |
| CHEMBL2111782 | — | — | 1 | 5.64 |
| CHEMBL333455 | — | — | 1 | 5.63 |
| CHEMBL118919 | — | — | 1 | 5.20 |
| CHEMBL2111783 | — | — | 2 | - |
| 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 | = | 55.0 | nM | 7.26 |
| CHEMBL368324 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL2111782 | — | Ki | = | 2272.0 | nM | 5.64 |
| CHEMBL333455 | — | Ki | = | 2344.0 | nM | 5.63 |
| CHEMBL118919 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL2111783 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL54 | HALOPERIDOL | Ki | > | 10000.0 | nM | - |
| CHEMBL2111783 | — | Ki | > | 10000.0 | nM | - |