Assay Detail
Binding
CHEMBL865923
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Inhibition of reuptake of Norepinephrine
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Derivatives of tramadol for increased duration of effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.58 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1237044 | TRAMADOL | 4.0 | 1 | 6.10 |
| CHEMBL379021 | — | — | 1 | 5.70 |
| CHEMBL438627 | — | — | 1 | 5.50 |
| CHEMBL201531 | — | — | 1 | 5.44 |
| CHEMBL201556 | — | — | 1 | 5.17 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1237044 | TRAMADOL | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL379021 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL438627 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL201531 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL201556 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | IC50 | > | 10000.0 | nM | - |