Assay Detail
Binding
CHEMBL677368
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Inhibition of [3H]dopamine binding to rat striatal synaptosome dopamine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.73 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL320427 | — | — | 1 | 9.51 |
| CHEMBL106627 | — | — | 1 | 9.18 |
| CHEMBL432401 | — | — | 1 | 9.08 |
| CHEMBL107808 | — | — | 1 | 9.06 |
| CHEMBL321888 | — | — | 1 | 8.97 |
| CHEMBL28394 | — | — | 1 | 8.95 |
| CHEMBL104567 | — | — | 1 | 8.81 |
| CHEMBL420291 | — | — | 1 | 8.79 |
| CHEMBL27336 | — | — | 1 | 8.63 |
| CHEMBL281288 | — | — | 1 | 8.61 |
| CHEMBL610897 | — | — | 1 | 8.54 |
| CHEMBL322365 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL320427 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL106627 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL432401 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL107808 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL321888 | — | Ki | = | 1.08 | nM | 8.97 |
| CHEMBL28394 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL104567 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL420291 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL27336 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL281288 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL610897 | — | Ki | = | 2.85 | nM | 8.54 |
| CHEMBL322365 | — | Ki | = | 271.0 | nM | 6.57 |