Assay Detail
Binding
CHEMBL744098
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for rat M1 acetylcholine receptor using [3H]-AF DX 384 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 M2 (CHEMBL309) ↗| 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 | 7.04 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 8.59 |
| CHEMBL3084883 | — | — | 1 | 7.82 |
| CHEMBL3084872 | — | — | 1 | 7.75 |
| CHEMBL3084880 | — | — | 1 | 7.72 |
| CHEMBL310310 | — | — | 2 | 7.44 |
| CHEMBL3084881 | — | — | 1 | 7.43 |
| CHEMBL3084882 | — | — | 1 | 7.41 |
| CHEMBL3084899 | — | — | 1 | 7.38 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | — | 1 | 7.31 |
| CHEMBL3084866 | — | — | 1 | 7.27 |
| CHEMBL3084897 | — | — | 1 | 7.18 |
| CHEMBL3084900 | — | — | 1 | 7.13 |
| CHEMBL3084892 | — | — | 1 | 6.85 |
| CHEMBL3084896 | — | — | 1 | 6.43 |
| CHEMBL3084898 | — | — | 1 | 6.15 |
| CHEMBL3084888 | — | — | 1 | 6.14 |
| CHEMBL3084867 | — | — | 1 | 6.00 |
| CHEMBL3084884 | — | — | 1 | 5.83 |
| CHEMBL3084873 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201203 | BENZTROPINE | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3084883 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3084872 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL3084880 | — | Ki | = | 18.9 | nM | 7.72 |
| CHEMBL310310 | — | Ki | = | 36.6 | nM | 7.44 |
| CHEMBL3084881 | — | Ki | = | 37.5 | nM | 7.43 |
| CHEMBL3084882 | — | Ki | = | 39.1 | nM | 7.41 |
| CHEMBL3084899 | — | Ki | = | 41.9 | nM | 7.38 |
| CHEMBL317757 | DIFLUOROBENZTROPINE | Ki | = | 48.8 | nM | 7.31 |
| CHEMBL3084866 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3084897 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL3084900 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL310310 | — | Ki | = | 87.4 | nM | 7.06 |
| CHEMBL3084892 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL3084896 | — | Ki | = | 369.0 | nM | 6.43 |
| CHEMBL3084898 | — | Ki | = | 703.0 | nM | 6.15 |
| CHEMBL3084888 | — | Ki | = | 716.0 | nM | 6.14 |
| CHEMBL3084867 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL3084884 | — | Ki | = | 1490.0 | nM | 5.83 |
| CHEMBL3084873 | — | Ki | = | 1510.0 | nM | 5.82 |