Assay Detail
Binding
CHEMBL745925
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for rat M1 acetylcholine receptor using [3H]pirenzepine displacement.
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.06 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 9.02 |
| CHEMBL3084883 | — | — | 1 | 8.96 |
| CHEMBL3084872 | — | — | 1 | 8.68 |
| CHEMBL3084881 | — | — | 1 | 8.57 |
| CHEMBL310310 | — | — | 2 | 8.44 |
| CHEMBL3084882 | — | — | 1 | 8.43 |
| CHEMBL3084880 | — | — | 1 | 8.38 |
| CHEMBL3084873 | — | — | 1 | 8.27 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 8.21 |
| CHEMBL3084899 | — | — | 1 | 8.15 |
| CHEMBL3084900 | — | — | 1 | 8.15 |
| CHEMBL3084898 | — | — | 1 | 7.90 |
| CHEMBL3084892 | — | — | 1 | 7.90 |
| CHEMBL3084896 | — | — | 1 | 7.48 |
| CHEMBL3084884 | — | — | 1 | 7.46 |
| CHEMBL3084867 | — | — | 1 | 7.40 |
| CHEMBL3084888 | — | — | 1 | 7.33 |
| CHEMBL3084897 | — | — | 1 | 7.15 |
| CHEMBL3084866 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL3084883 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3084872 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3084881 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL310310 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3084882 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL310310 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3084880 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3084873 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3084900 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3084899 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3084892 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL3084898 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL3084896 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3084884 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3084867 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL3084888 | — | Ki | = | 47.2 | nM | 7.33 |
| CHEMBL3084897 | — | Ki | = | 70.8 | nM | 7.15 |
| CHEMBL3084866 | — | Ki | = | 148.0 | nM | 6.83 |