Assay Detail
Binding
CHEMBL751379
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Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter
19
Total Activities
19
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 noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 19 | 6.27 | 8.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.69 |
| CHEMBL539564 | — | — | 1 | 7.68 |
| CHEMBL543925 | — | — | 1 | 7.52 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 7.40 |
| CHEMBL539050 | — | — | 1 | 7.36 |
| CHEMBL545557 | — | — | 1 | 7.26 |
| CHEMBL306700 | VILOXAZINE | 4.0 | 1 | 6.81 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.62 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 6.44 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 6.38 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 5.97 |
| CHEMBL540333 | — | — | 1 | 5.81 |
| CHEMBL538053 | — | — | 1 | 5.75 |
| CHEMBL556025 | — | — | 1 | 5.65 |
| CHEMBL542501 | — | — | 1 | 5.46 |
| CHEMBL542746 | — | — | 1 | 4.90 |
| CHEMBL539054 | — | — | 1 | 4.65 |
| CHEMBL544633 | — | — | 1 | 4.45 |
| CHEMBL555280 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | Kd | = | 2.03 | nM | 8.69 |
| CHEMBL539564 | — | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL543925 | — | Kd | = | 29.9 | nM | 7.52 |
| CHEMBL490 | PAROXETINE | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL539050 | — | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL545557 | — | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL306700 | VILOXAZINE | Kd | = | 155.0 | nM | 6.81 |
| CHEMBL41 | FLUOXETINE | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL623 | NEFAZODONE | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL809 | SERTRALINE | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL637 | VENLAFAXINE | Kd | = | 1060.0 | nM | 5.97 |
| CHEMBL540333 | — | Kd | = | 1540.0 | nM | 5.81 |
| CHEMBL538053 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL556025 | — | Kd | = | 2250.0 | nM | 5.65 |
| CHEMBL542501 | — | Kd | = | 3430.0 | nM | 5.46 |
| CHEMBL542746 | — | Kd | = | 12500.0 | nM | 4.90 |
| CHEMBL539054 | — | Kd | = | 22500.0 | nM | 4.65 |
| CHEMBL544633 | — | Kd | = | 35800.0 | nM | 4.45 |
| CHEMBL555280 | — | Kd | = | 47900.0 | nM | 4.32 |