Assay Detail
Binding
CHEMBL674110
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Inhibition of [3H]cocaine binding to the dopamine transporter.
15
Total Activities
10
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 | 15 | 6.55 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL177269 | — | — | 1 | 7.70 |
| CHEMBL352575 | — | — | 3 | 7.50 |
| CHEMBL120901 | — | — | 3 | 7.19 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.86 |
| CHEMBL1237136 | — | — | 1 | 6.86 |
| CHEMBL607198 | — | — | 1 | 6.72 |
| CHEMBL177595 | — | — | 1 | 6.67 |
| CHEMBL1790051 | — | — | 2 | 5.92 |
| CHEMBL1947052 | — | — | 1 | 5.48 |
| CHEMBL367502 | — | — | 1 | 4.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL177269 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL352575 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL120901 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL120901 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL352575 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL370805 | COCAINE | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL1237136 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL120901 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL607198 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL177595 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL352575 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1790051 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1790051 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1947052 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL367502 | — | IC50 | = | 78200.0 | nM | 4.11 |