Assay Detail
Binding
CHEMBL915899
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Displacement of [3H]nisoxetine from NET
33
Total Activities
16
Compounds Tested
2
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
Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.74 | 7.22 |
| Ki | 16 | 5.98 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312037 | — | — | 4 | 7.44 |
| CHEMBL225235 | — | — | 2 | 7.21 |
| CHEMBL224062 | — | — | 2 | 6.72 |
| CHEMBL224771 | — | — | 2 | 6.55 |
| CHEMBL2096877 | — | — | 2 | 6.41 |
| CHEMBL388850 | — | — | 2 | 6.26 |
| CHEMBL83729 | — | — | 2 | 6.26 |
| CHEMBL2096874 | — | — | 2 | 6.20 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 5.70 |
| CHEMBL2096876 | — | — | 2 | 5.55 |
| CHEMBL2096875 | — | — | 2 | 5.54 |
| CHEMBL387758 | — | — | 2 | 5.43 |
| CHEMBL388605 | — | — | 2 | 5.22 |
| CHEMBL426178 | — | — | 2 | 5.11 |
| CHEMBL388825 | — | — | 2 | 4.34 |
| CHEMBL2096878 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312037 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL312037 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL225235 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL225235 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL224062 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL224771 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL224062 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL2096877 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL224771 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL83729 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL388850 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2096874 | — | Ki | = | 626.0 | nM | 6.20 |
| CHEMBL2096877 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL388850 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL83729 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2096874 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL312037 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL370805 | COCAINE | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL2096876 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL2096875 | — | Ki | = | 2920.0 | nM | 5.54 |
| CHEMBL370805 | COCAINE | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL387758 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL312037 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL2096876 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2096875 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL388605 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL387758 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL426178 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL388605 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL426178 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL388825 | — | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL388825 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL2096878 | — | IC50 | - | — | - |