Assay Detail
Binding
CHEMBL672588
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Ability to inhibit binding of [3H]WIN-35428 to dopamine transporter in rat caudate putamen
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Effects of two-carbon bridge region methoxylation of benztropine: discovery of novel chiral ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.76 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL424565 | — | — | 1 | 7.60 |
| CHEMBL168814 | — | — | 1 | 7.50 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.05 |
| CHEMBL355286 | — | — | 1 | 7.02 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 1 | 6.93 |
| CHEMBL355258 | — | — | 1 | 6.19 |
| CHEMBL168371 | — | — | 1 | 6.12 |
| CHEMBL3084973 | — | — | 1 | 5.70 |
| CHEMBL3084972 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL424565 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL168814 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL370805 | COCAINE | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL355286 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL355258 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL168371 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3084973 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3084972 | — | IC50 | > | 10000.0 | nM | - |