Assay Detail
Binding
CHEMBL745664
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Ability to displace [3H]pirenzepine radioligand for the Muscarinic acetylcholine receptor M1 in rat brain
9
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.01 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.94 |
| CHEMBL21859 | — | — | 2 | 6.88 |
| CHEMBL281388 | — | — | 2 | 5.73 |
| CHEMBL428704 | — | — | 2 | 5.57 |
| CHEMBL283154 | — | — | 2 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL21859 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL21859 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL281388 | — | Ki | = | 1860.0 | nM | 5.73 |
| CHEMBL281388 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL428704 | — | Ki | = | 2680.0 | nM | 5.57 |
| CHEMBL283154 | — | Ki | = | 4380.0 | nM | 5.36 |
| CHEMBL283154 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL428704 | — | Ki | = | 7640.0 | nM | 5.12 |