Assay Detail
Binding
CHEMBL756266
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Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.37 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL336100 | — | — | 1 | 9.05 |
| CHEMBL336940 | — | — | 1 | 8.17 |
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 7.75 |
| CHEMBL130477 | — | — | 1 | 7.75 |
| CHEMBL132082 | — | — | 1 | 7.64 |
| CHEMBL132954 | — | — | 1 | 7.64 |
| CHEMBL132955 | — | — | 1 | 7.40 |
| CHEMBL133043 | — | — | 1 | 7.08 |
| CHEMBL133902 | — | — | 1 | 7.00 |
| CHEMBL336613 | — | — | 1 | 6.77 |
| CHEMBL130668 | — | — | 1 | 6.42 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL336100 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL336940 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL781 | MAZINDOL | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL130477 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL132082 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL132954 | — | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL132955 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL133043 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL133902 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL336613 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL130668 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL370805 | COCAINE | Ki | = | 1940.0 | nM | 5.71 |