Assay Detail
Binding
CHEMBL670104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester [3H]7a binding to Dopamine transporter of rat striatal membranes
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.52 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.99 |
| CHEMBL32525 | — | — | 1 | 6.52 |
| CHEMBL33039 | — | — | 1 | 6.17 |
| CHEMBL287389 | — | — | 2 | 5.54 |
| CHEMBL288315 | — | — | 1 | 5.47 |
| CHEMBL3349044 | — | — | 2 | 5.30 |
| CHEMBL1947052 | — | — | 2 | 5.29 |
| CHEMBL32987 | — | — | 1 | 5.04 |
| CHEMBL436152 | — | — | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL32525 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL33039 | — | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL287389 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL287389 | — | IC50 | = | 2940.0 | nM | 5.53 |
| CHEMBL288315 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL3349044 | — | IC50 | = | 4950.0 | nM | 5.30 |
| CHEMBL1947052 | — | IC50 | = | 5180.0 | nM | 5.29 |
| CHEMBL32987 | — | IC50 | = | 9030.0 | nM | 5.04 |
| CHEMBL436152 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3349044 | — | IC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL1947052 | — | IC50 | = | 21200.0 | nM | 4.67 |