Assay Detail
Binding
CHEMBL754326
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Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats
21
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.27 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | 4.0 | 1 | 9.10 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.00 |
| CHEMBL152935 | — | — | 2 | 7.87 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 7.86 |
| CHEMBL152141 | — | — | 2 | 7.76 |
| CHEMBL345277 | — | — | 2 | 7.72 |
| CHEMBL149641 | — | — | 2 | 7.65 |
| CHEMBL348704 | — | — | 2 | 7.61 |
| CHEMBL356400 | — | — | 2 | 7.36 |
| CHEMBL153093 | — | — | 2 | 7.06 |
| CHEMBL152254 | — | — | 1 | 6.95 |
| CHEMBL150932 | — | — | 1 | 6.38 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 6.18 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL781 | MAZINDOL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL295467 | NISOXETINE | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL152935 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL14370 | REBOXETINE | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL152141 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL345277 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL149641 | — | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL348704 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL149641 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL356400 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL345277 | — | Ki | = | 48.1 | nM | 7.32 |
| CHEMBL356400 | — | Ki | = | 55.8 | nM | 7.25 |
| CHEMBL153093 | — | Ki | = | 86.9 | nM | 7.06 |
| CHEMBL152935 | — | Ki | = | 98.3 | nM | 7.01 |
| CHEMBL152254 | — | Ki | = | 111.4 | nM | 6.95 |
| CHEMBL152141 | — | Ki | = | 127.8 | nM | 6.89 |
| CHEMBL153093 | — | Ki | = | 179.9 | nM | 6.75 |
| CHEMBL348704 | — | Ki | = | 385.9 | nM | 6.41 |
| CHEMBL150932 | — | Ki | = | 416.6 | nM | 6.38 |
| CHEMBL490 | PAROXETINE | Ki | = | 659.6 | nM | 6.18 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 719.0 | nM | 6.14 |