Assay Detail
Binding
CHEMBL2215837
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Inhibition of DAT-mediated [3H]DA in rat synaptosomes by scintillation counting
8
Total Activities
8
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 | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.86 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204356 | — | — | 1 | 7.68 |
| CHEMBL2205043 | — | — | 1 | 7.43 |
| CHEMBL2205045 | — | — | 1 | 6.96 |
| CHEMBL2205054 | — | — | 1 | 6.92 |
| CHEMBL2204357 | — | — | 1 | 6.77 |
| CHEMBL2204359 | — | — | 1 | 6.60 |
| CHEMBL2204363 | — | — | 1 | 6.50 |
| CHEMBL2204360 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204356 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2205043 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2205045 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2205054 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2204357 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2204359 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2204363 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2204360 | — | IC50 | = | 890.0 | nM | 6.05 |