Assay Detail
Binding
CHEMBL677380
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Displacement of [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue
25
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.03 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.50 |
| CHEMBL136499 | — | — | 1 | 7.48 |
| CHEMBL1790051 | — | — | 1 | 7.48 |
| CHEMBL3085521 | — | — | 3 | 7.24 |
| CHEMBL545080 | — | — | 2 | 7.22 |
| CHEMBL339395 | — | — | 1 | 7.04 |
| CHEMBL132958 | — | — | 1 | 6.68 |
| CHEMBL3085520 | — | — | 2 | 6.51 |
| CHEMBL336186 | — | — | 1 | 5.81 |
| CHEMBL545778 | — | — | 1 | 5.51 |
| CHEMBL539809 | — | — | 2 | 5.51 |
| CHEMBL3085523 | — | — | 1 | 5.51 |
| CHEMBL336345 | — | — | 2 | 5.39 |
| CHEMBL542492 | — | — | 1 | 5.32 |
| CHEMBL544145 | — | — | 2 | 5.23 |
| CHEMBL3084338 | — | — | 1 | 5.12 |
| CHEMBL3085519 | — | — | 2 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL136499 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL1790051 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3085521 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL545080 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL339395 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL545080 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL132958 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL3085521 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL3085520 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL3085521 | — | Ki | = | 531.0 | nM | 6.28 |
| CHEMBL3085520 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL336186 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL545778 | — | Ki | = | 3080.0 | nM | 5.51 |
| CHEMBL539809 | — | Ki | = | 3110.0 | nM | 5.51 |
| CHEMBL3085523 | — | Ki | = | 3080.0 | nM | 5.51 |
| CHEMBL336345 | — | Ki | = | 4108.0 | nM | 5.39 |
| CHEMBL542492 | — | Ki | = | 4830.0 | nM | 5.32 |
| CHEMBL544145 | — | Ki | = | 5850.0 | nM | 5.23 |
| CHEMBL539809 | — | Ki | = | 6210.0 | nM | 5.21 |
| CHEMBL336345 | — | Ki | = | 7240.0 | nM | 5.14 |
| CHEMBL3084338 | — | Ki | = | 7590.0 | nM | 5.12 |
| CHEMBL3085519 | — | Ki | = | 8580.0 | nM | 5.07 |
| CHEMBL3085519 | — | Ki | = | 19700.0 | nM | 4.71 |
| CHEMBL544145 | — | Ki | = | 57300.0 | nM | 4.24 |