Assay Detail
Binding
CHEMBL853389
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Inhibition of [3H]WIN-35428 binding to rat striatum DAT
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 | 6.77 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.07 |
| CHEMBL211302 | — | — | 1 | 7.42 |
| CHEMBL209651 | — | — | 1 | 7.19 |
| CHEMBL209809 | — | — | 1 | 6.94 |
| CHEMBL209843 | — | — | 1 | 6.93 |
| CHEMBL379706 | — | — | 1 | 6.90 |
| CHEMBL213627 | — | — | 1 | 6.85 |
| CHEMBL211484 | — | — | 1 | 6.74 |
| CHEMBL211077 | — | — | 1 | 6.65 |
| CHEMBL211994 | — | — | 1 | 6.63 |
| CHEMBL209603 | — | — | 1 | 6.47 |
| CHEMBL379716 | — | — | 1 | 6.40 |
| CHEMBL378437 | — | — | 1 | 6.33 |
| CHEMBL209808 | — | — | 1 | 6.24 |
| CHEMBL377129 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 8.56 | nM | 8.07 |
| CHEMBL211302 | — | Ki | = | 38.4 | nM | 7.42 |
| CHEMBL209651 | — | Ki | = | 64.6 | nM | 7.19 |
| CHEMBL209809 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL209843 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL379706 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL213627 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL211484 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL211077 | — | Ki | = | 226.0 | nM | 6.65 |
| CHEMBL211994 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL209603 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL379716 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL378437 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL209808 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL377129 | — | Ki | = | 1500.0 | nM | 5.82 |