Assay Detail
Binding
CHEMBL750809
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Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.88 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429772 | — | — | 1 | 8.26 |
| CHEMBL2112889 | — | — | 1 | 8.12 |
| CHEMBL21112 | — | — | 1 | 7.73 |
| CHEMBL300226 | — | — | 1 | 7.44 |
| CHEMBL610897 | — | — | 1 | 7.43 |
| CHEMBL279657 | — | — | 1 | 7.07 |
| CHEMBL2112860 | — | — | 1 | 6.91 |
| CHEMBL2112877 | — | — | 1 | 6.88 |
| CHEMBL21256 | — | — | 1 | 6.86 |
| CHEMBL610894 | — | — | 1 | 6.54 |
| CHEMBL2079586 | — | — | 1 | 6.08 |
| CHEMBL1790051 | — | — | 1 | 6.04 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.48 |
| CHEMBL50157 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429772 | — | IC50 | = | 5.45 | nM | 8.26 |
| CHEMBL2112889 | — | IC50 | = | 7.54 | nM | 8.12 |
| CHEMBL21112 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL300226 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL610897 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL279657 | — | IC50 | = | 84.5 | nM | 7.07 |
| CHEMBL2112860 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2112877 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL21256 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL610894 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL2079586 | — | IC50 | = | 834.0 | nM | 6.08 |
| CHEMBL1790051 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL370805 | COCAINE | IC50 | = | 3298.0 | nM | 5.48 |
| CHEMBL50157 | — | IC50 | = | 3907.0 | nM | 5.41 |