Assay Detail
Binding
CHEMBL948023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]WIN-35428 from human DAT expressed in transfected cell membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The synthesis of bivalent 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)-8-heterobicyclo[3.2.1]octanes as probes for proximal binding sites on the dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.53 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42553 | — | — | 1 | 8.96 |
| CHEMBL227757 | — | — | 1 | 8.70 |
| CHEMBL390929 | — | — | 1 | 8.48 |
| CHEMBL255140 | — | — | 1 | 8.10 |
| CHEMBL399740 | — | — | 1 | 7.96 |
| CHEMBL256046 | — | — | 1 | 7.92 |
| CHEMBL257482 | — | — | 1 | 7.55 |
| CHEMBL271707 | — | — | 1 | 7.51 |
| CHEMBL270659 | — | — | 1 | 7.26 |
| CHEMBL401554 | — | — | 1 | 7.17 |
| CHEMBL403660 | — | — | 1 | 6.94 |
| CHEMBL279331 | — | — | 1 | 5.81 |
| CHEMBL407902 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42553 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL227757 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL390929 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL255140 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL399740 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL256046 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL257482 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL271707 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL270659 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL401554 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL403660 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL279331 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL407902 | — | IC50 | = | 2960.0 | nM | 5.53 |