Assay Detail
Binding
CHEMBL948141
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Inhibition of NET mediated norepinephrine uptake
25
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.59 | 6.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272533 | — | — | 1 | 6.79 |
| CHEMBL270642 | — | — | 1 | 6.28 |
| CHEMBL256163 | — | — | 1 | 6.05 |
| CHEMBL403388 | — | — | 1 | 6.00 |
| CHEMBL258336 | — | — | 2 | 5.82 |
| CHEMBL258338 | — | — | 1 | 5.80 |
| CHEMBL402116 | — | — | 2 | 5.65 |
| CHEMBL404197 | — | — | 1 | 5.42 |
| CHEMBL272063 | — | — | 1 | 5.42 |
| CHEMBL256227 | — | — | 1 | 5.41 |
| CHEMBL1237044 | TRAMADOL | 4.0 | 1 | 5.41 |
| CHEMBL256902 | — | — | 1 | 5.41 |
| CHEMBL257083 | — | — | 1 | 5.41 |
| CHEMBL255196 | — | — | 1 | 5.35 |
| CHEMBL257264 | — | — | 1 | 5.23 |
| CHEMBL270786 | — | — | 1 | 5.20 |
| CHEMBL258140 | — | — | 1 | 5.17 |
| CHEMBL407563 | — | — | 1 | 5.05 |
| CHEMBL270570 | — | — | 1 | - |
| CHEMBL255768 | — | — | 1 | - |
| CHEMBL257265 | — | — | 1 | - |
| CHEMBL256371 | — | — | 1 | - |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272533 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL270642 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL256163 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL403388 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL258336 | — | IC50 | = | 1518.0 | nM | 5.82 |
| CHEMBL258338 | — | IC50 | = | 1565.0 | nM | 5.80 |
| CHEMBL402116 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL404197 | — | IC50 | = | 3776.0 | nM | 5.42 |
| CHEMBL258336 | — | IC50 | = | 3789.0 | nM | 5.42 |
| CHEMBL272063 | — | IC50 | = | 3776.0 | nM | 5.42 |
| CHEMBL256902 | — | IC50 | = | 3861.0 | nM | 5.41 |
| CHEMBL1237044 | TRAMADOL | IC50 | = | 3861.0 | nM | 5.41 |
| CHEMBL257083 | — | IC50 | = | 3873.0 | nM | 5.41 |
| CHEMBL256227 | — | IC50 | = | 3867.0 | nM | 5.41 |
| CHEMBL255196 | — | IC50 | = | 4495.0 | nM | 5.35 |
| CHEMBL257264 | — | IC50 | = | 5948.0 | nM | 5.23 |
| CHEMBL270786 | — | IC50 | = | 6248.0 | nM | 5.20 |
| CHEMBL258140 | — | IC50 | = | 6688.0 | nM | 5.17 |
| CHEMBL407563 | — | IC50 | = | 8999.0 | nM | 5.05 |
| CHEMBL270570 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL255768 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL257265 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL256371 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL402116 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | IC50 | > | 10000.0 | nM | - |