Assay Detail
Binding
CHEMBL675906
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Inhibitory activity determined for [3H]DA (Dopamine transporter) uptake by striated synaptosomes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| 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 | 16 | 8.00 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607061 | — | — | 1 | 8.92 |
| CHEMBL607063 | — | — | 1 | 8.85 |
| CHEMBL607112 | — | — | 1 | 8.67 |
| CHEMBL607114 | — | — | 1 | 8.51 |
| CHEMBL421777 | — | — | 1 | 8.35 |
| CHEMBL146195 | — | — | 1 | 8.30 |
| CHEMBL312037 | — | — | 1 | 8.13 |
| CHEMBL607113 | — | — | 1 | 8.13 |
| CHEMBL145888 | — | — | 1 | 7.96 |
| CHEMBL439629 | — | — | 1 | 7.90 |
| CHEMBL148419 | — | — | 1 | 7.89 |
| CHEMBL147787 | — | — | 1 | 7.88 |
| CHEMBL607062 | — | — | 1 | 7.51 |
| CHEMBL345026 | — | — | 1 | 7.49 |
| CHEMBL607111 | — | — | 1 | 7.24 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607061 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL607063 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL607112 | — | IC50 | = | 2.16 | nM | 8.67 |
| CHEMBL607114 | — | IC50 | = | 3.09 | nM | 8.51 |
| CHEMBL421777 | — | IC50 | = | 4.48 | nM | 8.35 |
| CHEMBL146195 | — | IC50 | = | 4.95 | nM | 8.30 |
| CHEMBL312037 | — | IC50 | = | 7.47 | nM | 8.13 |
| CHEMBL607113 | — | IC50 | = | 7.46 | nM | 8.13 |
| CHEMBL145888 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL439629 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL148419 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL147787 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL607062 | — | IC50 | = | 31.1 | nM | 7.51 |
| CHEMBL345026 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL607111 | — | IC50 | = | 57.9 | nM | 7.24 |
| CHEMBL370805 | COCAINE | IC50 | = | 459.0 | nM | 6.34 |