Assay Detail
Binding
CHEMBL831100
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Inhibition of rat brain Serotonin transporter uptake as [3H]5-HT accumulation
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| 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 | 6.08 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113050 | — | — | 1 | 7.62 |
| CHEMBL2113053 | — | — | 1 | 7.59 |
| CHEMBL211484 | — | — | 1 | 7.54 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.99 |
| CHEMBL2112061 | — | — | 1 | 6.17 |
| CHEMBL2112056 | — | — | 1 | 6.13 |
| CHEMBL2113048 | — | — | 1 | 6.06 |
| CHEMBL2113052 | — | — | 1 | 5.97 |
| CHEMBL2112057 | — | — | 1 | 5.53 |
| CHEMBL2113044 | — | — | 1 | 5.45 |
| CHEMBL2112059 | — | — | 1 | 5.42 |
| CHEMBL2112060 | — | — | 1 | 5.36 |
| CHEMBL2113047 | — | — | 1 | 5.25 |
| CHEMBL2112058 | — | — | 1 | 5.21 |
| CHEMBL2113049 | — | — | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113050 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2113053 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL211484 | — | IC50 | = | 28.9 | nM | 7.54 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 101.4 | nM | 6.99 |
| CHEMBL2112061 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL2112056 | — | IC50 | = | 745.0 | nM | 6.13 |
| CHEMBL2113048 | — | IC50 | = | 862.0 | nM | 6.06 |
| CHEMBL2113052 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL2112057 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL2113044 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL2112059 | — | IC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL2112060 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL2113047 | — | IC50 | = | 5560.0 | nM | 5.25 |
| CHEMBL2112058 | — | IC50 | = | 6120.0 | nM | 5.21 |
| CHEMBL2113049 | — | IC50 | = | 10600.0 | nM | 4.97 |