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Assay Detail

CHEMBL1019481

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

Binding
Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting
9
Total Activities
9
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

Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
Cashman JR, Voelker T, Zhang HT, O'Donnell JM.
J Med Chem (2009) 52 : 1530 -1539
PubMed 19256502 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.59 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL450907 1 8.64
CHEMBL464422 1 8.60
CHEMBL41 FLUOXETINE 4.0 1 8.14
CHEMBL473966 1 7.74
CHEMBL505431 1 6.90
CHEMBL451500 1 6.71
CHEMBL370805 COCAINE 4.0 1 6.38
CHEMBL313041 1 -
CHEMBL463431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL450907 IC50 = 2.3 nM 8.64
CHEMBL464422 IC50 = 2.5 nM 8.60
CHEMBL41 FLUOXETINE IC50 = 7.3 nM 8.14
CHEMBL473966 IC50 = 18.4 nM 7.74
CHEMBL505431 IC50 = 127.0 nM 6.90
CHEMBL451500 IC50 = 194.0 nM 6.71
CHEMBL370805 COCAINE IC50 = 416.0 nM 6.38
CHEMBL313041 IC50 > 100000.0 nM -
CHEMBL463431 IC50 > 100000.0 nM -