Assay Detail
Binding
CHEMBL1041760
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Displacement of [125I]RTI55 from cloned 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 |
|---|---|---|---|
| Ki | 38 | 5.50 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566050 | — | — | 1 | 6.28 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.08 |
| CHEMBL569465 | — | — | 1 | 5.93 |
| CHEMBL566418 | — | — | 1 | 5.75 |
| CHEMBL566208 | — | — | 1 | 5.65 |
| CHEMBL565594 | — | — | 1 | 5.64 |
| CHEMBL565593 | — | — | 1 | 5.59 |
| CHEMBL566830 | — | — | 1 | 5.51 |
| CHEMBL576622 | — | — | 1 | 5.50 |
| CHEMBL566886 | — | — | 1 | 5.50 |
| CHEMBL567479 | — | — | 1 | 5.42 |
| CHEMBL569700 | — | — | 1 | 5.40 |
| CHEMBL565382 | — | — | 1 | 5.37 |
| CHEMBL578815 | — | — | 1 | 5.35 |
| CHEMBL565845 | — | — | 1 | 5.34 |
| CHEMBL566420 | — | — | 1 | 5.32 |
| CHEMBL565844 | — | — | 1 | 5.29 |
| CHEMBL568140 | — | — | 1 | 5.27 |
| CHEMBL569699 | — | — | 1 | 5.24 |
| CHEMBL566618 | — | — | 1 | 5.24 |
| CHEMBL566207 | — | — | 1 | 5.17 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.16 |
| CHEMBL565396 | — | — | 1 | - |
| CHEMBL566193 | — | — | 1 | - |
| CHEMBL157455 | — | — | 1 | - |
| CHEMBL576063 | — | — | 1 | - |
| CHEMBL566832 | — | — | 1 | - |
| CHEMBL566000 | — | — | 1 | - |
| CHEMBL566001 | — | — | 1 | - |
| CHEMBL578610 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566050 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL370805 | COCAINE | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL569465 | — | Ki | = | 1171.0 | nM | 5.93 |
| CHEMBL566418 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL566208 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL565594 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL565593 | — | Ki | = | 2580.0 | nM | 5.59 |
| CHEMBL566830 | — | Ki | = | 3090.0 | nM | 5.51 |
| CHEMBL576622 | — | Ki | = | 3190.0 | nM | 5.50 |
| CHEMBL566886 | — | Ki | = | 3195.0 | nM | 5.50 |
| CHEMBL567479 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL569700 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL565382 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL578815 | — | Ki | = | 4476.0 | nM | 5.35 |
| CHEMBL565845 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL566420 | — | Ki | = | 4760.0 | nM | 5.32 |
| CHEMBL565844 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL568140 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL566618 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL569699 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL566207 | — | Ki | = | 6840.0 | nM | 5.17 |
| CHEMBL894 | BUPROPION | Ki | = | 6970.0 | nM | 5.16 |
| CHEMBL567482 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL567481 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL565386 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL578612 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL565397 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL567480 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL578611 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL577501 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL578610 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL566001 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL566000 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL566832 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL576063 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL157455 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL566193 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL565396 | — | Ki | > | 7140.0 | nM | - |