Assay Detail
Binding
CHEMBL676558
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Inhibitory activity on dopamine transporters of rat striated membranes using [3H]- mazindol.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.64 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607061 | — | — | 1 | 8.53 |
| CHEMBL607063 | — | — | 1 | 8.46 |
| CHEMBL607114 | — | — | 1 | 8.30 |
| CHEMBL421777 | — | — | 1 | 8.26 |
| CHEMBL607112 | — | — | 1 | 8.00 |
| CHEMBL146195 | — | — | 1 | 7.94 |
| CHEMBL148419 | — | — | 1 | 7.74 |
| CHEMBL145888 | — | — | 1 | 7.67 |
| CHEMBL607113 | — | — | 1 | 7.64 |
| CHEMBL439629 | — | — | 1 | 7.58 |
| CHEMBL147787 | — | — | 1 | 7.43 |
| CHEMBL607062 | — | — | 1 | 7.01 |
| CHEMBL345026 | — | — | 1 | 6.85 |
| CHEMBL607111 | — | — | 1 | 6.79 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607061 | — | IC50 | = | 2.97 | nM | 8.53 |
| CHEMBL607063 | — | IC50 | = | 3.43 | nM | 8.46 |
| CHEMBL607114 | — | IC50 | = | 4.98 | nM | 8.30 |
| CHEMBL421777 | — | IC50 | = | 5.55 | nM | 8.26 |
| CHEMBL607112 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL146195 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL148419 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL145888 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL607113 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL439629 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL147787 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL607062 | — | IC50 | = | 96.5 | nM | 7.01 |
| CHEMBL345026 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL607111 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL370805 | COCAINE | IC50 | = | 400.0 | nM | 6.40 |