Assay Detail
Binding
CHEMBL752511
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Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 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
Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.80 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL67078 | — | — | 1 | 7.32 |
| CHEMBL63703 | — | — | 1 | 7.06 |
| CHEMBL67203 | — | — | 1 | 7.01 |
| CHEMBL26320 | — | — | 1 | 6.78 |
| CHEMBL67024 | — | — | 1 | 6.77 |
| CHEMBL443797 | — | — | 1 | 6.75 |
| CHEMBL417035 | — | — | 1 | 6.72 |
| CHEMBL417049 | — | — | 1 | 6.70 |
| CHEMBL66112 | — | — | 1 | 6.70 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.64 |
| CHEMBL421867 | — | — | 1 | 6.64 |
| CHEMBL69380 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL67078 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL63703 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL67203 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL26320 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL67024 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL443797 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL417035 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL417049 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL66112 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL370805 | COCAINE | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL421867 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL69380 | — | IC50 | = | 350.0 | nM | 6.46 |