Assay Detail
Binding
CHEMBL670181
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Binding affinity was evaluated by measuring the inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat brain tissue
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.31 | 7.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL39262 | — | — | 1 | 7.71 |
| CHEMBL40607 | — | — | 2 | 7.67 |
| CHEMBL78048 | — | — | 1 | 7.06 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL39262 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL40607 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL40607 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL78048 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL370805 | COCAINE | IC50 | = | 266.0 | nM | 6.58 |