Assay Detail
Binding
CHEMBL677553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit reuptake of dopamine ([3H]DA) at dopamine transporter of rat striatum
26
Total Activities
26
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
Synthesis and pharmacological evaluation of (Z)-9-(heteroarylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes: thiophene analogues as potent norepinephrine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.10 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118261 | — | — | 1 | 6.89 |
| CHEMBL331425 | — | — | 1 | 6.83 |
| CHEMBL325404 | — | — | 1 | 6.75 |
| CHEMBL331639 | — | — | 1 | 6.62 |
| CHEMBL331565 | — | — | 1 | 6.57 |
| CHEMBL116431 | — | — | 1 | 6.53 |
| CHEMBL119477 | — | — | 1 | 6.43 |
| CHEMBL119137 | — | — | 1 | 6.43 |
| CHEMBL117047 | — | — | 1 | 6.39 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.37 |
| CHEMBL333912 | — | — | 1 | 6.31 |
| CHEMBL118725 | — | — | 1 | 5.97 |
| CHEMBL116369 | — | — | 1 | 5.89 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 5.84 |
| CHEMBL324031 | — | — | 1 | 5.80 |
| CHEMBL334027 | — | — | 1 | 5.78 |
| CHEMBL118853 | — | — | 1 | 5.33 |
| CHEMBL119706 | — | — | 1 | 5.29 |
| CHEMBL116374 | — | — | 1 | 5.18 |
| CHEMBL440332 | — | — | 1 | 4.85 |
| CHEMBL118500 | — | — | 1 | - |
| CHEMBL118530 | — | — | 1 | - |
| CHEMBL331321 | — | — | 1 | - |
| CHEMBL443281 | — | — | 1 | - |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | - |
| CHEMBL331780 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118261 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL331425 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL325404 | — | Ki | = | 179.0 | nM | 6.75 |
| CHEMBL331639 | — | Ki | = | 242.0 | nM | 6.62 |
| CHEMBL331565 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL116431 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL119477 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL119137 | — | Ki | = | 371.0 | nM | 6.43 |
| CHEMBL117047 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL370805 | COCAINE | Ki | = | 423.0 | nM | 6.37 |
| CHEMBL333912 | — | Ki | = | 485.0 | nM | 6.31 |
| CHEMBL118725 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL116369 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL641 | ATOMOXETINE | Ki | = | 1451.0 | nM | 5.84 |
| CHEMBL324031 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL334027 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL118853 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL119706 | — | Ki | = | 5090.0 | nM | 5.29 |
| CHEMBL116374 | — | Ki | = | 6570.0 | nM | 5.18 |
| CHEMBL440332 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL118500 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL118530 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL331321 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL443281 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL72 | DESIPRAMINE | Ki | > | 10000.0 | nM | - |
| CHEMBL331780 | — | Ki | > | 10000.0 | nM | - |