Assay Detail
Binding
CHEMBL862305
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Inhibition of dopamine re-uptake at human dopamine transporter expressed in HEK293 cells
40
Total Activities
40
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 dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.40 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206697 | — | — | 1 | 7.70 |
| CHEMBL203674 | — | — | 1 | 7.54 |
| CHEMBL381792 | — | — | 1 | 7.26 |
| CHEMBL202810 | — | — | 1 | 7.05 |
| CHEMBL383706 | — | — | 1 | 7.05 |
| CHEMBL203331 | — | — | 1 | 7.05 |
| CHEMBL382810 | — | — | 1 | 7.05 |
| CHEMBL206598 | — | — | 1 | 7.05 |
| CHEMBL203741 | — | — | 1 | 7.00 |
| CHEMBL381754 | — | — | 1 | 7.00 |
| CHEMBL206211 | — | — | 1 | 6.92 |
| CHEMBL438257 | — | — | 1 | 6.77 |
| CHEMBL439337 | — | — | 1 | 6.66 |
| CHEMBL380758 | — | — | 1 | 6.62 |
| CHEMBL383427 | — | — | 1 | 6.60 |
| CHEMBL380523 | — | — | 1 | 6.57 |
| CHEMBL203776 | — | — | 1 | 6.57 |
| CHEMBL205837 | — | — | 1 | 6.54 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 6.51 |
| CHEMBL206649 | — | — | 1 | 6.44 |
| CHEMBL204323 | — | — | 1 | 6.43 |
| CHEMBL206404 | — | — | 1 | 6.38 |
| CHEMBL378379 | — | — | 1 | 6.35 |
| CHEMBL204005 | — | — | 1 | 6.27 |
| CHEMBL411693 | — | — | 1 | 6.08 |
| CHEMBL205505 | — | — | 1 | 6.04 |
| CHEMBL382241 | — | — | 1 | 5.96 |
| CHEMBL383081 | — | — | 1 | 5.89 |
| CHEMBL203453 | — | — | 1 | 5.85 |
| CHEMBL203236 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206697 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL203674 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL381792 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL202810 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL383706 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL203331 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL382810 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL206598 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL203741 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL381754 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL206211 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL438257 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL439337 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL380758 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL383427 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL380523 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL203776 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL205837 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL809 | SERTRALINE | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL206649 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL204323 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL206404 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL378379 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL204005 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL411693 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL205505 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL382241 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL383081 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL203453 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL203236 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL204285 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL206599 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL202907 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL378804 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL381315 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL202910 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL382673 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL202755 | — | IC50 | - | — | - | |
| CHEMBL383128 | — | IC50 | - | — | - | |
| CHEMBL381331 | — | IC50 | - | — | - |