Assay Detail
Binding
CHEMBL884449
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Binding affinity was evaluated using [3H]WIN-35428 binding to dopamine transporter (DAT) in rat caudate-putamen
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.50 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 7.24 |
| CHEMBL138438 | — | — | 1 | 7.06 |
| CHEMBL2112760 | — | — | 1 | 6.61 |
| CHEMBL336707 | — | — | 1 | 6.28 |
| CHEMBL336706 | — | — | 1 | 5.90 |
| CHEMBL140191 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 57.6 | nM | 7.24 |
| CHEMBL138438 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL2112760 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL336707 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL336706 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL140191 | — | IC50 | = | 1330.0 | nM | 5.88 |