Assay Detail
Binding
CHEMBL672590
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Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane
24
Total Activities
24
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
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.02 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130477 | — | — | 1 | 9.00 |
| CHEMBL544370 | — | — | 1 | 8.71 |
| CHEMBL133043 | — | — | 1 | 8.60 |
| CHEMBL130668 | — | — | 1 | 8.47 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 8.09 |
| CHEMBL132955 | — | — | 1 | 7.87 |
| CHEMBL442765 | — | — | 1 | 7.24 |
| CHEMBL336761 | — | — | 1 | 7.20 |
| CHEMBL133902 | — | — | 1 | 7.18 |
| CHEMBL338721 | — | — | 1 | 7.15 |
| CHEMBL130372 | — | — | 1 | 7.06 |
| CHEMBL336313 | — | — | 1 | 7.06 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 7.05 |
| CHEMBL339648 | — | — | 1 | 7.03 |
| CHEMBL424640 | — | — | 1 | 7.00 |
| CHEMBL555778 | — | — | 1 | 6.66 |
| CHEMBL133287 | — | — | 1 | 6.64 |
| CHEMBL131637 | — | — | 1 | 6.54 |
| CHEMBL130747 | — | — | 1 | 6.20 |
| CHEMBL134129 | — | — | 1 | 6.00 |
| CHEMBL132180 | — | — | 1 | 5.56 |
| CHEMBL132419 | — | — | 1 | 5.48 |
| CHEMBL132988 | — | — | 1 | 5.43 |
| CHEMBL336624 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130477 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL544370 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL133043 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL130668 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL781 | MAZINDOL | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL132955 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL442765 | — | IC50 | = | 57.1 | nM | 7.24 |
| CHEMBL336761 | — | IC50 | = | 62.5 | nM | 7.20 |
| CHEMBL133902 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL338721 | — | IC50 | = | 71.5 | nM | 7.15 |
| CHEMBL130372 | — | IC50 | = | 87.4 | nM | 7.06 |
| CHEMBL336313 | — | IC50 | = | 86.4 | nM | 7.06 |
| CHEMBL370805 | COCAINE | IC50 | = | 89.1 | nM | 7.05 |
| CHEMBL339648 | — | IC50 | = | 93.3 | nM | 7.03 |
| CHEMBL424640 | — | IC50 | = | 99.8 | nM | 7.00 |
| CHEMBL555778 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL133287 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL131637 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL130747 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL134129 | — | IC50 | = | 1009.0 | nM | 6.00 |
| CHEMBL132180 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL132419 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL132988 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL336624 | — | IC50 | = | 6890.0 | nM | 5.16 |