Assay Detail
Binding
CHEMBL1041763
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Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells
38
Total Activities
38
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 | Intermediate |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.01 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566050 | — | — | 1 | 7.37 |
| CHEMBL566418 | — | — | 1 | 7.07 |
| CHEMBL566208 | — | — | 1 | 6.87 |
| CHEMBL566618 | — | — | 1 | 6.66 |
| CHEMBL565594 | — | — | 1 | 6.44 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.42 |
| CHEMBL576622 | — | — | 1 | 6.40 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 6.35 |
| CHEMBL569465 | — | — | 1 | 6.33 |
| CHEMBL565844 | — | — | 1 | 6.05 |
| CHEMBL566886 | — | — | 1 | 6.01 |
| CHEMBL566830 | — | — | 1 | 5.90 |
| CHEMBL565845 | — | — | 1 | 5.79 |
| CHEMBL565382 | — | — | 1 | 5.70 |
| CHEMBL568140 | — | — | 1 | 5.68 |
| CHEMBL569700 | — | — | 1 | 5.67 |
| CHEMBL566207 | — | — | 1 | 5.39 |
| CHEMBL578815 | — | — | 1 | 5.34 |
| CHEMBL566420 | — | — | 1 | 5.32 |
| CHEMBL565593 | — | — | 1 | 5.31 |
| CHEMBL565396 | — | — | 1 | 5.19 |
| CHEMBL569699 | — | — | 1 | 5.06 |
| CHEMBL566001 | — | — | 1 | - |
| CHEMBL157455 | — | — | 1 | - |
| CHEMBL567479 | — | — | 1 | - |
| CHEMBL576063 | — | — | 1 | - |
| CHEMBL566832 | — | — | 1 | - |
| CHEMBL566000 | — | — | 1 | - |
| CHEMBL566193 | — | — | 1 | - |
| CHEMBL578610 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566050 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL566418 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL566208 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL566618 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL565594 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL370805 | COCAINE | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL576622 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL894 | BUPROPION | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL569465 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL565844 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL566886 | — | IC50 | = | 969.0 | nM | 6.01 |
| CHEMBL566830 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL565845 | — | IC50 | = | 1623.0 | nM | 5.79 |
| CHEMBL565382 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL568140 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL569700 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL566207 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL578815 | — | IC50 | = | 4603.0 | nM | 5.34 |
| CHEMBL566420 | — | IC50 | = | 4798.0 | nM | 5.32 |
| CHEMBL565593 | — | IC50 | = | 4890.0 | nM | 5.31 |
| CHEMBL565396 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL569699 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL567482 | — | IC50 | - | — | - | |
| CHEMBL567481 | — | IC50 | - | — | - | |
| CHEMBL565386 | — | IC50 | - | — | - | |
| CHEMBL578612 | — | IC50 | - | — | - | |
| CHEMBL565397 | — | IC50 | - | — | - | |
| CHEMBL567480 | — | IC50 | - | — | - | |
| CHEMBL578611 | — | IC50 | - | — | - | |
| CHEMBL577501 | — | IC50 | - | — | - | |
| CHEMBL578610 | — | IC50 | - | — | - | |
| CHEMBL566193 | — | IC50 | - | — | - | |
| CHEMBL566000 | — | IC50 | - | — | - | |
| CHEMBL566832 | — | IC50 | - | — | - | |
| CHEMBL576063 | — | IC50 | - | — | - | |
| CHEMBL567479 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL157455 | — | IC50 | - | — | - | |
| CHEMBL566001 | — | IC50 | - | — | - |