Assay Detail
Binding
CHEMBL676690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested for the ability to displace [3H]WIN-35 428 binding to dopamine transporter (DAT) in rat striatal tissue
15
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.61 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48892 | — | — | 2 | 7.62 |
| CHEMBL301094 | — | — | 2 | 7.32 |
| CHEMBL297102 | — | — | 1 | 7.15 |
| CHEMBL296907 | — | — | 1 | 7.07 |
| CHEMBL51993 | — | — | 2 | 6.91 |
| CHEMBL49736 | — | — | 1 | 6.72 |
| CHEMBL52392 | — | — | 1 | 6.27 |
| CHEMBL51130 | — | — | 1 | 5.64 |
| CHEMBL299838 | — | — | 1 | 5.04 |
| CHEMBL50901 | — | — | 1 | 4.38 |
| CHEMBL48222 | — | — | 1 | - |
| CHEMBL49933 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48892 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL48892 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL301094 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL301094 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL297102 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL296907 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL51993 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL51993 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL49736 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL52392 | — | Ki | = | 533.0 | nM | 6.27 |
| CHEMBL51130 | — | Ki | = | 2280.0 | nM | 5.64 |
| CHEMBL299838 | — | Ki | = | 9180.0 | nM | 5.04 |
| CHEMBL50901 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL48222 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL49933 | — | Ki | > | 1000.0 | nM | - |