Assay Detail
Binding
CHEMBL674263
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]GBR-12935 from dopamine transporter (DAT) in rat brain membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and ligand binding of nortropane derivatives: N-substituted 2beta-carbomethoxy-3beta-(4'-iodophenyl)nortropane and N-(3-iodoprop-(2E)-enyl)-2beta-carbomethoxy-3beta-(3',4'-disubstituted phenyl)nortropane. New high-affinity and selective compounds for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.30 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611178 | — | — | 1 | 7.85 |
| CHEMBL611426 | — | — | 1 | 7.82 |
| CHEMBL2113648 | — | — | 1 | 7.77 |
| CHEMBL311347 | — | — | 1 | 7.57 |
| CHEMBL2113650 | — | — | 1 | 7.54 |
| CHEMBL611424 | — | — | 1 | 7.52 |
| CHEMBL611180 | — | — | 1 | 7.52 |
| CHEMBL2113649 | — | — | 1 | 7.38 |
| CHEMBL611181 | — | — | 1 | 7.03 |
| CHEMBL611177 | — | — | 1 | 6.95 |
| CHEMBL611179 | — | — | 1 | 6.30 |
| CHEMBL611427 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611178 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL611426 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2113648 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL311347 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2113650 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL611424 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL611180 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2113649 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL611181 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL611177 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL611179 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL611427 | — | Ki | = | 500.0 | nM | 6.30 |