Assay Detail
Binding
CHEMBL744029
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Inhibition of [3H]NE uptake by rat frontal cortex Norepinephrine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.32 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306208 | — | — | 1 | 8.23 |
| CHEMBL14391 | — | — | 1 | 8.12 |
| CHEMBL82027 | — | — | 1 | 8.07 |
| CHEMBL340761 | — | — | 1 | 7.49 |
| CHEMBL1790051 | — | — | 1 | 7.43 |
| CHEMBL2079586 | — | — | 1 | 7.41 |
| CHEMBL127546 | — | — | 1 | 7.38 |
| CHEMBL321806 | — | — | 1 | 7.13 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.79 |
| CHEMBL14144 | — | — | 1 | 6.62 |
| CHEMBL127040 | — | — | 1 | 6.60 |
| CHEMBL340912 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306208 | — | Ki | = | 5.86 | nM | 8.23 |
| CHEMBL14391 | — | Ki | = | 7.51 | nM | 8.12 |
| CHEMBL82027 | — | Ki | = | 8.42 | nM | 8.07 |
| CHEMBL340761 | — | Ki | = | 32.73 | nM | 7.49 |
| CHEMBL1790051 | — | Ki | = | 37.2 | nM | 7.43 |
| CHEMBL2079586 | — | Ki | = | 38.59 | nM | 7.41 |
| CHEMBL127546 | — | Ki | = | 41.22 | nM | 7.38 |
| CHEMBL321806 | — | Ki | = | 73.43 | nM | 7.13 |
| CHEMBL370805 | COCAINE | Ki | = | 160.55 | nM | 6.79 |
| CHEMBL14144 | — | Ki | = | 242.29 | nM | 6.62 |
| CHEMBL127040 | — | Ki | = | 250.32 | nM | 6.60 |
| CHEMBL340912 | — | Ki | = | 277.66 | nM | 6.56 |