Assay Detail
Binding
CHEMBL745931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at Muscarinic acetylcholine receptor M1 in Rat brain homogenate 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
Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.22 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.94 |
| CHEMBL3084929 | — | — | 1 | 6.87 |
| CHEMBL417249 | — | — | 1 | 6.75 |
| CHEMBL11776 | — | — | 1 | 6.69 |
| CHEMBL12377 | — | — | 1 | 6.56 |
| CHEMBL3084934 | — | — | 1 | 6.52 |
| CHEMBL1907642 | — | — | 1 | 6.41 |
| CHEMBL11493 | — | — | 1 | 6.40 |
| CHEMBL2308105 | — | — | 1 | 6.24 |
| CHEMBL3085021 | — | — | 1 | 5.90 |
| CHEMBL1907825 | — | — | 1 | 5.84 |
| CHEMBL12004 | — | — | 1 | 5.75 |
| CHEMBL1907826 | — | — | 1 | 5.72 |
| CHEMBL429015 | — | — | 1 | 5.66 |
| CHEMBL1907641 | — | — | 1 | 5.63 |
| CHEMBL267562 | — | — | 1 | 5.41 |
| CHEMBL275802 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL3084929 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL417249 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL11776 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL12377 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL3084934 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL1907642 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL11493 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL2308105 | — | Ki | = | 575.5 | nM | 6.24 |
| CHEMBL3085021 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL1907825 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL12004 | — | Ki | = | 1790.0 | nM | 5.75 |
| CHEMBL1907826 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL429015 | — | Ki | = | 2180.0 | nM | 5.66 |
| CHEMBL1907641 | — | Ki | = | 2360.0 | nM | 5.63 |
| CHEMBL267562 | — | Ki | = | 3880.0 | nM | 5.41 |
| CHEMBL275802 | — | Ki | = | 4020.0 | nM | 5.40 |