Assay Detail
Binding
CHEMBL872892
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Inhibition of [3H]DA uptake by rat striatal dopamine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.99 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14391 | — | — | 1 | 8.71 |
| CHEMBL127546 | — | — | 1 | 8.55 |
| CHEMBL306208 | — | — | 1 | 8.43 |
| CHEMBL14144 | — | — | 1 | 8.28 |
| CHEMBL127040 | — | — | 1 | 8.22 |
| CHEMBL340761 | — | — | 1 | 8.16 |
| CHEMBL82027 | — | — | 1 | 8.15 |
| CHEMBL340912 | — | — | 1 | 8.04 |
| CHEMBL321806 | — | — | 1 | 7.82 |
| CHEMBL2079586 | — | — | 1 | 7.64 |
| CHEMBL1790051 | — | — | 1 | 7.30 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14391 | — | Ki | = | 1.96 | nM | 8.71 |
| CHEMBL127546 | — | Ki | = | 2.79 | nM | 8.55 |
| CHEMBL306208 | — | Ki | = | 3.68 | nM | 8.43 |
| CHEMBL14144 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL127040 | — | Ki | = | 6.04 | nM | 8.22 |
| CHEMBL340761 | — | Ki | = | 6.85 | nM | 8.16 |
| CHEMBL82027 | — | Ki | = | 7.02 | nM | 8.15 |
| CHEMBL340912 | — | Ki | = | 9.13 | nM | 8.04 |
| CHEMBL321806 | — | Ki | = | 15.31 | nM | 7.82 |
| CHEMBL2079586 | — | Ki | = | 22.95 | nM | 7.64 |
| CHEMBL1790051 | — | Ki | = | 49.8 | nM | 7.30 |
| CHEMBL370805 | COCAINE | Ki | = | 241.3 | nM | 6.62 |