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Assay Detail

CHEMBL1011738

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.
Cashman JR, Voelker T, Johnson R, Janowsky A.
Bioorg Med Chem (2009) 17 : 337 -343
PubMed 19014888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.32 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41 FLUOXETINE 4.0 1 8.15
CHEMBL446084 1 7.89
CHEMBL454507 1 7.38
CHEMBL465123 SEPROXETINE 2.0 1 7.34
CHEMBL499461 1 6.76
CHEMBL370805 COCAINE 4.0 1 6.38
CHEMBL313041 1 -
CHEMBL480988 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41 FLUOXETINE IC50 = 7.0 nM 8.15
CHEMBL446084 IC50 = 13.0 nM 7.89
CHEMBL454507 IC50 = 42.0 nM 7.38
CHEMBL465123 SEPROXETINE IC50 = 46.0 nM 7.34
CHEMBL499461 IC50 = 173.0 nM 6.76
CHEMBL370805 COCAINE IC50 = 416.0 nM 6.38
CHEMBL313041 IC50 > 100000.0 nM -
CHEMBL480988 IC50 > 100000.0 nM -