Assay Detail
Binding
CHEMBL672583
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Binding affinity towards Dopamine transporter by displacement of [3H]WIN-35428 radioligand from rat brain
16
Total Activities
13
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
3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogues of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.04 | 8.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610897 | — | — | 1 | 8.95 |
| CHEMBL606997 | — | — | 1 | 8.85 |
| CHEMBL607054 | — | — | 1 | 8.79 |
| CHEMBL606996 | — | — | 1 | 8.74 |
| CHEMBL14144 | — | — | 1 | 8.70 |
| CHEMBL607051 | — | — | 1 | 8.63 |
| CHEMBL607099 | — | — | 1 | 8.48 |
| CHEMBL607052 | — | — | 1 | 8.46 |
| CHEMBL607050 | — | — | 1 | 8.39 |
| CHEMBL607053 | — | — | 1 | 8.39 |
| CHEMBL606995 | — | — | 1 | 8.22 |
| CHEMBL1790051 | — | — | 1 | 7.64 |
| CHEMBL606998 | — | — | 4 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610897 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL606997 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL607054 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL606996 | — | IC50 | = | 1.81 | nM | 8.74 |
| CHEMBL14144 | — | IC50 | = | 1.99 | nM | 8.70 |
| CHEMBL607051 | — | IC50 | = | 2.33 | nM | 8.63 |
| CHEMBL607099 | — | IC50 | = | 3.27 | nM | 8.48 |
| CHEMBL607052 | — | IC50 | = | 3.44 | nM | 8.46 |
| CHEMBL607050 | — | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL607053 | — | IC50 | = | 4.06 | nM | 8.39 |
| CHEMBL606995 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1790051 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL606998 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL606998 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL606998 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL606998 | — | IC50 | = | 1030.0 | nM | 5.99 |