Assay Detail
Binding
CHEMBL884450
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Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to Dopamine transporter in rat striatal membranes.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.59 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL552552 | — | — | 1 | 7.21 |
| CHEMBL541032 | — | — | 1 | 7.14 |
| CHEMBL541526 | — | — | 1 | 7.07 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.99 |
| CHEMBL539238 | — | — | 1 | 6.95 |
| CHEMBL416764 | — | — | 1 | 6.89 |
| CHEMBL31837 | — | — | 1 | 6.86 |
| CHEMBL31981 | — | — | 1 | 6.72 |
| CHEMBL545163 | — | — | 1 | 6.71 |
| CHEMBL545395 | — | — | 1 | 6.68 |
| CHEMBL557204 | — | — | 1 | 6.64 |
| CHEMBL31831 | — | — | 1 | 6.61 |
| CHEMBL32047 | — | — | 1 | 6.59 |
| CHEMBL543519 | — | — | 1 | 6.57 |
| CHEMBL543281 | — | — | 1 | 6.57 |
| CHEMBL557834 | — | — | 1 | 6.43 |
| CHEMBL432849 | — | — | 1 | 6.25 |
| CHEMBL543044 | — | — | 1 | 6.22 |
| CHEMBL554446 | — | — | 1 | 5.50 |
| CHEMBL1947052 | — | — | 1 | 5.29 |
| CHEMBL284394 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL552552 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL541032 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL541526 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL370805 | COCAINE | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL539238 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL416764 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL31837 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL31981 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL545163 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL545395 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL557204 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL31831 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL32047 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL543519 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL543281 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL557834 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL432849 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL543044 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL554446 | — | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL1947052 | — | IC50 | = | 5180.0 | nM | 5.29 |
| CHEMBL284394 | — | IC50 | = | 195000.0 | nM | - |