Assay Detail
Binding
CHEMBL828170
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Inhibition of [3H]nisoxetine binding to rat cerebral cortex norepinephrine transporter
20
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.53 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365738 | — | — | 1 | 9.07 |
| CHEMBL371607 | — | — | 1 | 8.39 |
| CHEMBL195738 | — | — | 1 | 8.37 |
| CHEMBL81525 | — | — | 2 | 8.27 |
| CHEMBL366159 | — | — | 1 | 8.20 |
| CHEMBL80262 | — | — | 2 | 8.14 |
| CHEMBL80515 | — | — | 2 | 8.01 |
| CHEMBL192924 | — | — | 1 | 8.01 |
| CHEMBL306208 | — | — | 2 | 7.43 |
| CHEMBL192195 | — | — | 1 | 7.35 |
| CHEMBL82027 | — | — | 2 | 7.22 |
| CHEMBL192035 | — | — | 1 | 6.83 |
| CHEMBL2079586 | — | — | 2 | 6.08 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365738 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL371607 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL195738 | — | IC50 | = | 4.23 | nM | 8.37 |
| CHEMBL81525 | — | IC50 | = | 5.41 | nM | 8.27 |
| CHEMBL81525 | — | IC50 | = | 5.45 | nM | 8.26 |
| CHEMBL366159 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL80262 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL80262 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL80515 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL192924 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL80515 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL306208 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL192195 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL306208 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL82027 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL192035 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL82027 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2079586 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL2079586 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL370805 | COCAINE | IC50 | = | 3300.0 | nM | 5.48 |