Assay Detail
Binding
CHEMBL1013551
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Displacement of [3H]nisoxetine from NET
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of 3-phenyltropane analogues with high affinity for the dopamine and serotonin transporters and low affinity for the norepinephrine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.04 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457865 | — | — | 1 | 7.66 |
| CHEMBL513090 | — | — | 1 | 6.80 |
| CHEMBL457415 | — | — | 1 | 6.75 |
| CHEMBL458072 | — | — | 1 | 6.57 |
| CHEMBL457866 | — | — | 1 | 6.48 |
| CHEMBL512202 | — | — | 1 | 5.96 |
| CHEMBL457635 | — | — | 1 | 5.91 |
| CHEMBL457655 | — | — | 1 | 5.84 |
| CHEMBL458488 | — | — | 1 | 5.77 |
| CHEMBL514424 | — | — | 1 | 5.73 |
| CHEMBL515988 | — | — | 1 | 5.70 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | 4.0 | 1 | 5.70 |
| CHEMBL459332 | — | — | 1 | 5.69 |
| CHEMBL458080 | — | — | 1 | 5.66 |
| CHEMBL459333 | — | — | 1 | 5.58 |
| CHEMBL516933 | — | — | 1 | 5.57 |
| CHEMBL458282 | — | — | 1 | 5.39 |
| CHEMBL457416 | — | — | 1 | - |
| CHEMBL455937 | — | — | 1 | - |
| CHEMBL461241 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457865 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL513090 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL457415 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL458072 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL457866 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL512202 | — | Ki | = | 1110.0 | nM | 5.96 |
| CHEMBL457635 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL457655 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL458488 | — | Ki | = | 1690.0 | nM | 5.77 |
| CHEMBL514424 | — | Ki | = | 1850.0 | nM | 5.73 |
| CHEMBL515988 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL459332 | — | Ki | = | 2040.0 | nM | 5.69 |
| CHEMBL458080 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL459333 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL516933 | — | Ki | = | 2710.0 | nM | 5.57 |
| CHEMBL458282 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL457416 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL455937 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL461241 | — | Ki | > | 3000.0 | nM | - |