Assay Detail
Binding
CHEMBL853390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DAT-mediated [3H]DA uptake in rat striatum
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further structural exploration of trisubstituted asymmetric pyran derivatives (2S,4R,5R)-2-benzhydryl-5-benzylamino-tetrahydropyran-4-ol and their corresponding disubstituted (3S,6S) pyran derivatives: a proposed pharmacophore model for high-affinity interaction with the dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.05 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.97 |
| CHEMBL211302 | — | — | 1 | 7.46 |
| CHEMBL209843 | — | — | 1 | 7.36 |
| CHEMBL209651 | — | — | 1 | 7.22 |
| CHEMBL213627 | — | — | 1 | 7.21 |
| CHEMBL209809 | — | — | 1 | 7.17 |
| CHEMBL211077 | — | — | 1 | 7.07 |
| CHEMBL379706 | — | — | 1 | 7.04 |
| CHEMBL211484 | — | — | 1 | 6.94 |
| CHEMBL209808 | — | — | 1 | 6.92 |
| CHEMBL378437 | — | — | 1 | 6.85 |
| CHEMBL211994 | — | — | 1 | 6.76 |
| CHEMBL379716 | — | — | 1 | 6.74 |
| CHEMBL209603 | — | — | 1 | 6.67 |
| CHEMBL377129 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL211302 | — | Ki | = | 34.6 | nM | 7.46 |
| CHEMBL209843 | — | Ki | = | 43.9 | nM | 7.36 |
| CHEMBL209651 | — | Ki | = | 59.9 | nM | 7.22 |
| CHEMBL213627 | — | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL209809 | — | Ki | = | 67.4 | nM | 7.17 |
| CHEMBL211077 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL379706 | — | Ki | = | 91.5 | nM | 7.04 |
| CHEMBL211484 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL209808 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL378437 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL211994 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL379716 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL209603 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL377129 | — | Ki | = | 446.0 | nM | 6.35 |