Assay Detail
Binding
CHEMBL754327
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Displacement of [3H]nisoxetine from rat brain norepinephrine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.71 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL315166 | — | — | 1 | 6.40 |
| CHEMBL314424 | — | — | 1 | 6.27 |
| CHEMBL330021 | — | — | 1 | 6.17 |
| CHEMBL313179 | — | — | 1 | 5.99 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 5.90 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 5.67 |
| CHEMBL316244 | — | — | 1 | 5.44 |
| CHEMBL87841 | — | — | 1 | 5.28 |
| CHEMBL314433 | — | — | 1 | 5.17 |
| CHEMBL433340 | — | — | 1 | 4.77 |
| CHEMBL86830 | — | — | 1 | - |
| CHEMBL84971 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL315166 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL314424 | — | Ki | = | 532.0 | nM | 6.27 |
| CHEMBL330021 | — | Ki | = | 682.0 | nM | 6.17 |
| CHEMBL313179 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL281594 | VANOXERINE | Ki | = | 1270.0 | nM | 5.90 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 2160.0 | nM | 5.67 |
| CHEMBL316244 | — | Ki | = | 3640.0 | nM | 5.44 |
| CHEMBL87841 | — | Ki | = | 5210.0 | nM | 5.28 |
| CHEMBL314433 | — | Ki | = | 6810.0 | nM | 5.17 |
| CHEMBL433340 | — | Ki | = | 16900.0 | nM | 4.77 |
| CHEMBL86830 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL84971 | — | Ki | > | 30000.0 | nM | - |