Assay Detail
Binding
CHEMBL675166
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Inhibition of [3H]cocaine binding to the dopamine transporter.
22
Total Activities
16
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 | 22 | 6.50 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 8.05 |
| CHEMBL1790051 | — | — | 3 | 7.66 |
| CHEMBL48225 | — | — | 1 | 7.64 |
| CHEMBL2079586 | — | — | 1 | 7.57 |
| CHEMBL176708 | — | — | 1 | 7.44 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.44 |
| CHEMBL159325 | — | — | 1 | 7.43 |
| CHEMBL279556 | — | — | 1 | 7.38 |
| CHEMBL416818 | — | — | 1 | 7.37 |
| CHEMBL368314 | — | — | 1 | 7.07 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 6.92 |
| CHEMBL172482 | — | — | 2 | 6.57 |
| CHEMBL425862 | — | — | 1 | 5.99 |
| CHEMBL120901 | — | — | 4 | 5.07 |
| CHEMBL1947052 | — | — | 1 | 4.64 |
| CHEMBL284394 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1790051 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL48225 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2079586 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL176708 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL159325 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL279556 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL416818 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1790051 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL368314 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL273575 | NOMIFENSINE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL172482 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL172482 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL425862 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL120901 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL120901 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL120901 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL1947052 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1790051 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL284394 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL120901 | — | IC50 | = | 109000.0 | nM | - |