Assay Detail
Functional
CHEMBL829628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat brain dopamine transporter as accumulation of [3H]DA
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 |
|---|---|---|---|
| Ki | 15 | 6.57 | 7.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.97 |
| CHEMBL2113053 | — | — | 1 | 7.00 |
| CHEMBL2112056 | — | — | 1 | 6.96 |
| CHEMBL211484 | — | — | 1 | 6.94 |
| CHEMBL2112061 | — | — | 1 | 6.90 |
| CHEMBL2112057 | — | — | 1 | 6.79 |
| CHEMBL2112058 | — | — | 1 | 6.60 |
| CHEMBL2113044 | — | — | 1 | 6.50 |
| CHEMBL2113047 | — | — | 1 | 6.49 |
| CHEMBL2113048 | — | — | 1 | 6.35 |
| CHEMBL2113050 | — | — | 1 | 6.28 |
| CHEMBL2113052 | — | — | 1 | 6.21 |
| CHEMBL2112060 | — | — | 1 | 6.14 |
| CHEMBL2113049 | — | — | 1 | 5.71 |
| CHEMBL2112059 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL2113053 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2112056 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL211484 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL2112061 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL2112057 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL2112058 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL2113044 | — | Ki | = | 317.0 | nM | 6.50 |
| CHEMBL2113047 | — | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL2113048 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL2113050 | — | Ki | = | 528.0 | nM | 6.28 |
| CHEMBL2113052 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL2112060 | — | Ki | = | 716.0 | nM | 6.14 |
| CHEMBL2113049 | — | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL2112059 | — | Ki | = | 1980.0 | nM | 5.70 |