Assay Detail
Binding
CHEMBL929226
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Inhibition of [3H]NA uptake at human recombinant NA transporter expressed in HEK293 cells
23
Total Activities
23
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 noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.29 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247733 | — | — | 1 | 8.15 |
| CHEMBL402000 | — | — | 1 | 7.75 |
| CHEMBL403441 | — | — | 1 | 7.75 |
| CHEMBL403251 | — | — | 1 | 7.66 |
| CHEMBL260036 | — | — | 1 | 7.60 |
| CHEMBL403080 | — | — | 1 | 7.58 |
| CHEMBL256136 | — | — | 1 | 7.58 |
| CHEMBL256970 | — | — | 1 | 7.58 |
| CHEMBL256293 | — | — | 1 | 7.52 |
| CHEMBL402345 | — | — | 1 | 7.50 |
| CHEMBL401596 | — | — | 1 | 7.44 |
| CHEMBL402371 | — | — | 1 | 7.42 |
| CHEMBL257593 | — | — | 1 | 7.33 |
| CHEMBL256137 | — | — | 1 | 7.29 |
| CHEMBL403078 | — | — | 1 | 7.08 |
| CHEMBL256135 | — | — | 1 | 7.07 |
| CHEMBL257592 | — | — | 1 | 7.07 |
| CHEMBL259136 | — | — | 1 | 6.80 |
| CHEMBL256511 | — | — | 1 | 6.61 |
| CHEMBL260038 | — | — | 1 | 6.59 |
| CHEMBL258449 | — | — | 1 | 6.55 |
| CHEMBL260037 | — | — | 1 | 6.41 |
| CHEMBL260039 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247733 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL402000 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL403441 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL403251 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL260036 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL403080 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL256136 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL256970 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL256293 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL402345 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL401596 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL402371 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL257593 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL256137 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL403078 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL256135 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL257592 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL259136 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL256511 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL260038 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL258449 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL260037 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL260039 | — | IC50 | > | 400.0 | nM | - |