Assay Detail
Binding
CHEMBL745922
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Binding affinity towards Muscarinic acetylcholine receptor M1 using [3H]pirenzepine as radioligand was determined
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.25 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.94 |
| CHEMBL310650 | — | — | 1 | 6.88 |
| CHEMBL98279 | — | — | 1 | 6.58 |
| CHEMBL95775 | — | — | 1 | 6.45 |
| CHEMBL317362 | — | — | 1 | 5.72 |
| CHEMBL99038 | — | — | 1 | 5.57 |
| CHEMBL42553 | — | — | 1 | 5.50 |
| CHEMBL316634 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL310650 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL98279 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL95775 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL317362 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL99038 | — | Ki | = | 2680.0 | nM | 5.57 |
| CHEMBL42553 | — | Ki | = | 3140.0 | nM | 5.50 |
| CHEMBL316634 | — | Ki | = | 4380.0 | nM | 5.36 |