Assay Detail
Binding
CHEMBL1024552
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Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells
42
Total Activities
34
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 | Intermediate |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.45 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562244 | — | — | 1 | 8.70 |
| CHEMBL563030 | — | — | 2 | 8.52 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 8.30 |
| CHEMBL559456 | — | — | 3 | 8.22 |
| CHEMBL550779 | — | — | 1 | 8.10 |
| CHEMBL551573 | — | — | 2 | 8.05 |
| CHEMBL549825 | — | — | 2 | 8.05 |
| CHEMBL549761 | — | — | 1 | 7.89 |
| CHEMBL563495 | — | — | 2 | 7.85 |
| CHEMBL559081 | — | — | 3 | 7.85 |
| CHEMBL541226 | — | — | 1 | 7.80 |
| CHEMBL549965 | — | — | 1 | 7.64 |
| CHEMBL550696 | — | — | 1 | 7.64 |
| CHEMBL552046 | — | — | 1 | 7.64 |
| CHEMBL563987 | — | — | 1 | 7.62 |
| CHEMBL564100 | — | — | 1 | 7.52 |
| CHEMBL563404 | — | — | 1 | 7.48 |
| CHEMBL562691 | — | — | 1 | 7.46 |
| CHEMBL562854 | — | — | 1 | 7.38 |
| CHEMBL563852 | — | — | 1 | 7.35 |
| CHEMBL556268 | — | — | 1 | 7.32 |
| CHEMBL559654 | — | — | 1 | 7.08 |
| CHEMBL550289 | — | — | 1 | 7.04 |
| CHEMBL551556 | — | — | 1 | 6.97 |
| CHEMBL150932 | — | — | 1 | 6.92 |
| CHEMBL560049 | — | — | 1 | 6.67 |
| CHEMBL551443 | — | — | 1 | 6.39 |
| CHEMBL562444 | — | — | 1 | 5.31 |
| CHEMBL564631 | — | — | 1 | 5.23 |
| CHEMBL560050 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562244 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL563030 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL559456 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL559456 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL550779 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL551573 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL549825 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL549761 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL563030 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL559081 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL563495 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL541226 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL559081 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL552046 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL549965 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL550696 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL563987 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL564100 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL563404 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL562691 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL549825 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL562854 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL563495 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL551573 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL563852 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL556268 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL559654 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL550289 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL551556 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL150932 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL559456 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL560049 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL559081 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL551443 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL562444 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL564631 | — | IC50 | = | 5850.0 | nM | 5.23 |
| CHEMBL556888 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL562108 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL560050 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL551646 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL540978 | — | IC50 | > | 400.0 | nM | - |