Assay Detail
Binding
CHEMBL804695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT
18
Total Activities
18
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 serotonin transporter (CHEMBL228) ↗| 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 | 18 | 7.68 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.89 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 9.54 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 9.09 |
| CHEMBL543925 | — | — | 1 | 8.92 |
| CHEMBL539050 | — | — | 1 | 8.25 |
| CHEMBL545557 | — | — | 1 | 8.21 |
| CHEMBL539564 | — | — | 1 | 8.21 |
| CHEMBL544633 | — | — | 1 | 8.07 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.05 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 8.05 |
| CHEMBL538053 | — | — | 1 | 7.52 |
| CHEMBL542501 | — | — | 1 | 7.40 |
| CHEMBL540333 | — | — | 1 | 7.12 |
| CHEMBL539054 | — | — | 1 | 6.93 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 6.70 |
| CHEMBL555280 | — | — | 1 | 5.96 |
| CHEMBL542746 | — | — | 1 | 5.52 |
| CHEMBL306700 | VILOXAZINE | 4.0 | 1 | 4.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | Kd | = | 0.13 | nM | 9.89 |
| CHEMBL809 | SERTRALINE | Kd | = | 0.29 | nM | 9.54 |
| CHEMBL41 | FLUOXETINE | Kd | = | 0.81 | nM | 9.09 |
| CHEMBL543925 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL539050 | — | Kd | = | 5.59 | nM | 8.25 |
| CHEMBL545557 | — | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL539564 | — | Kd | = | 6.2 | nM | 8.21 |
| CHEMBL544633 | — | Kd | = | 8.5 | nM | 8.07 |
| CHEMBL641 | ATOMOXETINE | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL637 | VENLAFAXINE | Kd | = | 8.9 | nM | 8.05 |
| CHEMBL538053 | — | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL542501 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL540333 | — | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL539054 | — | Kd | = | 118.0 | nM | 6.93 |
| CHEMBL623 | NEFAZODONE | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL555280 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL542746 | — | Kd | = | 3050.0 | nM | 5.52 |
| CHEMBL306700 | VILOXAZINE | Kd | = | 17300.0 | nM | 4.76 |