Assay Detail
Binding
CHEMBL670183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.41 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286991 | — | — | 1 | 9.05 |
| CHEMBL159967 | — | — | 1 | 8.74 |
| CHEMBL159320 | — | — | 1 | 8.66 |
| CHEMBL163980 | — | — | 1 | 8.48 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.43 |
| CHEMBL159319 | — | — | 1 | 8.23 |
| CHEMBL164037 | — | — | 1 | 7.87 |
| CHEMBL159608 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286991 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL159967 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL159320 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL163980 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL159319 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL164037 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL159608 | — | IC50 | = | 16.0 | nM | 7.80 |