Assay Detail
Functional
CHEMBL830117
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat brain Dopamine transporter uptake as [3H]DA accumulation
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.44 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.85 |
| CHEMBL2113053 | — | — | 1 | 6.87 |
| CHEMBL2112056 | — | — | 1 | 6.83 |
| CHEMBL211484 | — | — | 1 | 6.81 |
| CHEMBL2112061 | — | — | 1 | 6.77 |
| CHEMBL2112057 | — | — | 1 | 6.66 |
| CHEMBL2112058 | — | — | 1 | 6.47 |
| CHEMBL2113044 | — | — | 1 | 6.37 |
| CHEMBL2113047 | — | — | 1 | 6.36 |
| CHEMBL2113048 | — | — | 1 | 6.22 |
| CHEMBL2113050 | — | — | 1 | 6.15 |
| CHEMBL2113052 | — | — | 1 | 6.08 |
| CHEMBL2112060 | — | — | 1 | 6.02 |
| CHEMBL2113049 | — | — | 1 | 5.58 |
| CHEMBL2112059 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2113053 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2112056 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL211484 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL2112061 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL2112057 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL2112058 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL2113044 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL2113047 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2113048 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2113050 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2113052 | — | IC50 | = | 822.0 | nM | 6.08 |
| CHEMBL2112060 | — | IC50 | = | 962.0 | nM | 6.02 |
| CHEMBL2113049 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL2112059 | — | IC50 | = | 2670.0 | nM | 5.57 |