Assay Detail
Binding
CHEMBL745923
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at muscarinic M1 receptor in rat brain by [3H]pirenzepine displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.00 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.94 |
| CHEMBL3084884 | — | — | 1 | 7.32 |
| CHEMBL326706 | — | — | 1 | 6.47 |
| CHEMBL115370 | — | — | 1 | 6.43 |
| CHEMBL325826 | — | — | 1 | 6.41 |
| CHEMBL112528 | — | — | 1 | 6.41 |
| CHEMBL115253 | — | — | 1 | 6.25 |
| CHEMBL2308105 | — | — | 1 | 6.24 |
| CHEMBL327055 | — | — | 1 | 6.21 |
| CHEMBL324518 | — | — | 1 | 5.91 |
| CHEMBL3085021 | — | — | 1 | 5.90 |
| CHEMBL115311 | — | — | 1 | 5.62 |
| CHEMBL3085020 | — | — | 1 | 5.48 |
| CHEMBL326604 | — | — | 1 | 5.38 |
| CHEMBL111928 | — | — | 1 | 5.03 |
| CHEMBL115710 | — | — | 1 | 4.80 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL3084884 | — | Ki | = | 47.9 | nM | 7.32 |
| CHEMBL326706 | — | Ki | = | 336.0 | nM | 6.47 |
| CHEMBL115370 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL325826 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL112528 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL115253 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL2308105 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL327055 | — | Ki | = | 613.0 | nM | 6.21 |
| CHEMBL324518 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL3085021 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL115311 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL3085020 | — | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL326604 | — | Ki | = | 4140.0 | nM | 5.38 |
| CHEMBL111928 | — | Ki | = | 9280.0 | nM | 5.03 |
| CHEMBL115710 | — | Ki | = | 15800.0 | nM | 4.80 |
| CHEMBL370805 | COCAINE | Ki | = | 61400.0 | nM | 4.21 |