Assay Detail
Binding
CHEMBL746899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.87 | 6.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41558 | — | — | 2 | 6.63 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.30 |
| CHEMBL288128 | — | — | 1 | 6.01 |
| CHEMBL40607 | — | — | 1 | 5.99 |
| CHEMBL39262 | — | — | 1 | 5.96 |
| CHEMBL289028 | — | — | 1 | 5.81 |
| CHEMBL39259 | — | — | 1 | 5.80 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41558 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 496.0 | nM | 6.30 |
| CHEMBL288128 | — | IC50 | = | 968.0 | nM | 6.01 |
| CHEMBL40607 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL39262 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL289028 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL39259 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL370805 | COCAINE | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL41558 | — | IC50 | = | 12700.0 | nM | 4.90 |