Assay Detail
Binding
CHEMBL675008
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Inhibition of [3H]GBR-12935 binding to the dopamine transporter.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.44 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.52 |
| CHEMBL284394 | — | — | 1 | 8.40 |
| CHEMBL176442 | — | — | 1 | 8.33 |
| CHEMBL176566 | — | — | 1 | 8.05 |
| CHEMBL279556 | — | — | 1 | 7.70 |
| CHEMBL362395 | — | — | 1 | 7.14 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.11 |
| CHEMBL172482 | — | — | 1 | 7.04 |
| CHEMBL3143431 | — | — | 1 | 7.03 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 6.94 |
| CHEMBL426954 | — | — | 1 | 6.56 |
| CHEMBL159325 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL284394 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL176442 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL176566 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL279556 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL362395 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL781 | MAZINDOL | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL172482 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3143431 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL273575 | NOMIFENSINE | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL426954 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL159325 | — | IC50 | = | 330.0 | nM | 6.48 |