Assay Detail
Binding
CHEMBL674430
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Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 24 | 6.53 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314424 | — | — | 1 | 8.07 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.92 |
| CHEMBL330021 | — | — | 1 | 7.74 |
| CHEMBL313179 | — | — | 1 | 7.64 |
| CHEMBL87841 | — | — | 1 | 7.56 |
| CHEMBL315166 | — | — | 1 | 7.22 |
| CHEMBL316244 | — | — | 1 | 7.21 |
| CHEMBL433340 | — | — | 1 | 7.11 |
| CHEMBL89832 | — | — | 1 | 6.96 |
| CHEMBL86830 | — | — | 1 | 6.75 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.73 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.65 |
| CHEMBL86477 | — | — | 1 | 6.58 |
| CHEMBL84971 | — | — | 1 | 6.57 |
| CHEMBL316444 | — | — | 1 | 6.36 |
| CHEMBL314433 | — | — | 1 | 6.09 |
| CHEMBL315846 | — | — | 1 | 5.62 |
| CHEMBL73234 | CARBETAPENTANE | 4.0 | 1 | 5.51 |
| CHEMBL7549 | PRECLAMOL | 2.0 | 1 | 5.49 |
| CHEMBL86519 | — | — | 1 | 5.41 |
| CHEMBL61946 | CARAMIPHEN | 2.0 | 1 | 5.29 |
| CHEMBL305881 | — | — | 1 | 5.27 |
| CHEMBL314726 | — | — | 1 | 4.52 |
| CHEMBL89095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314424 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL281594 | VANOXERINE | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL330021 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL313179 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL87841 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL315166 | — | Ki | = | 60.8 | nM | 7.22 |
| CHEMBL316244 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL433340 | — | Ki | = | 77.1 | nM | 7.11 |
| CHEMBL89832 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL86830 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL370805 | COCAINE | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL275707 | RIMCAZOLE | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL86477 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL84971 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL316444 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL314433 | — | Ki | = | 813.0 | nM | 6.09 |
| CHEMBL315846 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL73234 | CARBETAPENTANE | Ki | = | 3090.0 | nM | 5.51 |
| CHEMBL7549 | PRECLAMOL | Ki | = | 3270.0 | nM | 5.49 |
| CHEMBL86519 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL61946 | CARAMIPHEN | Ki | = | 5180.0 | nM | 5.29 |
| CHEMBL305881 | — | Ki | = | 5340.0 | nM | 5.27 |
| CHEMBL314726 | — | Ki | = | 30300.0 | nM | 4.52 |
| CHEMBL89095 | — | Ki | = | 174000.0 | nM | - |