Assay Detail
Binding
CHEMBL675223
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Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.53 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.64 |
| CHEMBL2112787 | — | — | 1 | 7.44 |
| CHEMBL2112788 | — | — | 1 | 6.96 |
| CHEMBL275707 | RIMCAZOLE | 2.0 | 1 | 6.85 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.69 |
| CHEMBL2112760 | — | — | 1 | 6.33 |
| CHEMBL2112783 | — | — | 1 | 6.19 |
| CHEMBL2112784 | — | — | 1 | 5.97 |
| CHEMBL324896 | — | — | 1 | 5.74 |
| CHEMBL110726 | — | — | 1 | 5.56 |
| CHEMBL2112790 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2112787 | — | IC50 | = | 36.6 | nM | 7.44 |
| CHEMBL2112788 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL275707 | RIMCAZOLE | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL370805 | COCAINE | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL2112760 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL2112783 | — | IC50 | = | 639.0 | nM | 6.19 |
| CHEMBL2112784 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL324896 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL110726 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL2112790 | — | IC50 | = | 3670.0 | nM | 5.43 |