Assay Detail
Binding
CHEMBL853391
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SERT-mediated [3H]5-HT uptake in rat cerebral cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| 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 | 7.16 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378437 | — | — | 1 | 7.93 |
| CHEMBL209603 | — | — | 1 | 7.84 |
| CHEMBL209808 | — | — | 1 | 7.82 |
| CHEMBL213627 | — | — | 1 | 7.79 |
| CHEMBL211302 | — | — | 1 | 7.70 |
| CHEMBL211484 | — | — | 1 | 7.59 |
| CHEMBL211077 | — | — | 1 | 7.42 |
| CHEMBL209843 | — | — | 1 | 7.34 |
| CHEMBL209651 | — | — | 1 | 7.19 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.04 |
| CHEMBL209809 | — | — | 1 | 6.73 |
| CHEMBL379716 | — | — | 1 | 6.65 |
| CHEMBL211994 | — | — | 1 | 6.62 |
| CHEMBL377129 | — | — | 1 | 6.15 |
| CHEMBL379706 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378437 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL209603 | — | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL209808 | — | Ki | = | 15.3 | nM | 7.82 |
| CHEMBL213627 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL211302 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL211484 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL211077 | — | Ki | = | 37.7 | nM | 7.42 |
| CHEMBL209843 | — | Ki | = | 45.7 | nM | 7.34 |
| CHEMBL209651 | — | Ki | = | 64.6 | nM | 7.19 |
| CHEMBL281594 | VANOXERINE | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL209809 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL379716 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL211994 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL377129 | — | Ki | = | 707.0 | nM | 6.15 |
| CHEMBL379706 | — | Ki | = | 2540.0 | nM | 5.59 |