Assay Detail
Binding
CHEMBL945183
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Inhibition of dopamine uptake at human DAT in human HEK293 cells
27
Total Activities
27
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 | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.58 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486044 | — | — | 1 | 6.75 |
| CHEMBL486043 | — | — | 1 | 6.22 |
| CHEMBL453321 | — | — | 1 | 6.00 |
| CHEMBL447598 | — | — | 1 | 6.00 |
| CHEMBL453061 | — | — | 1 | 6.00 |
| CHEMBL530334 | — | — | 1 | 5.70 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 5.62 |
| CHEMBL488424 | — | — | 1 | 5.62 |
| CHEMBL486235 | — | — | 1 | 5.60 |
| CHEMBL486236 | — | — | 1 | 5.60 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 5.52 |
| CHEMBL520201 | — | — | 1 | 5.47 |
| CHEMBL488222 | — | — | 1 | 5.40 |
| CHEMBL520736 | — | — | 1 | 5.35 |
| CHEMBL446570 | — | — | 1 | 5.34 |
| CHEMBL445185 | — | — | 1 | 5.30 |
| CHEMBL525249 | — | — | 1 | 5.22 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.22 |
| CHEMBL487690 | — | — | 1 | 5.16 |
| CHEMBL486045 | — | — | 1 | 5.10 |
| CHEMBL521392 | — | — | 1 | 5.00 |
| CHEMBL486237 | — | — | 1 | - |
| CHEMBL488049 | — | — | 1 | - |
| CHEMBL487869 | — | — | 1 | - |
| CHEMBL487691 | — | — | 1 | - |
| CHEMBL453062 | — | — | 1 | - |
| CHEMBL520735 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486044 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL486043 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL453321 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL447598 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL453061 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL530334 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL488424 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL486235 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL486236 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL520201 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL488222 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL520736 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL446570 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL445185 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL525249 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL487690 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL486045 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL521392 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL486237 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL488049 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL487869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL487691 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL453062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL520735 | — | IC50 | > | 10000.0 | nM | - |