Assay Detail
Binding
CHEMBL915413
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nisoxetine from NET
41
Total Activities
21
Compounds Tested
2
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
Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.52 | 8.29 |
| Ki | 20 | 6.77 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375888 | — | — | 2 | 8.51 |
| CHEMBL224819 | — | — | 2 | 7.79 |
| CHEMBL610897 | — | — | 2 | 7.66 |
| CHEMBL311347 | — | — | 2 | 7.66 |
| CHEMBL218082 | — | — | 2 | 7.64 |
| CHEMBL375889 | — | — | 2 | 7.50 |
| CHEMBL312037 | — | — | 2 | 7.44 |
| CHEMBL2096859 | — | — | 2 | 6.87 |
| CHEMBL373385 | — | — | 2 | 6.80 |
| CHEMBL2096858 | — | — | 2 | 6.65 |
| CHEMBL376899 | — | — | 2 | 6.57 |
| CHEMBL374712 | — | — | 2 | 6.55 |
| CHEMBL2096860 | — | — | 2 | 6.34 |
| CHEMBL2079586 | — | — | 2 | 6.30 |
| CHEMBL83729 | — | — | 2 | 6.26 |
| CHEMBL222705 | — | — | 2 | 6.13 |
| CHEMBL2096861 | — | — | 2 | 5.95 |
| CHEMBL221993 | — | — | 2 | 5.71 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 5.70 |
| CHEMBL2096857 | — | — | 2 | 5.36 |
| CHEMBL2096856 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375888 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL375888 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL224819 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL311347 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL610897 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL218082 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL375889 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL224819 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL311347 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL312037 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL218082 | — | IC50 | = | 37.4 | nM | 7.43 |
| CHEMBL610897 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL375889 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL312037 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2096859 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL373385 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2096858 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL373385 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL376899 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL2096859 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL374712 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2096858 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL2096860 | — | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL2079586 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL376899 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL83729 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL374712 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL222705 | — | Ki | = | 741.0 | nM | 6.13 |
| CHEMBL2096860 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2079586 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL83729 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2096861 | — | Ki | = | 1120.0 | nM | 5.95 |
| CHEMBL222705 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL221993 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL370805 | COCAINE | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL2096861 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL370805 | COCAINE | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL221993 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL2096857 | — | Ki | = | 4340.0 | nM | 5.36 |
| CHEMBL2096857 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2096856 | — | IC50 | > | 10000.0 | nM | - |