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Assay Detail

CHEMBL4433103

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

Binding
Inhibition of [3H]-5-hydroxytryptamine reuptake in human SERT expressed in HEK293 cells by liquid scintillation counting method
16
Total Activities
16
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

Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.
Paudel S, Acharya S, Yoon G, Kim KM, Cheon SH.
Bioorg Med Chem (2016) 24 : 5546 -5555
PubMed 27647372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201066 VENLAFAXINE HYDROCHLORIDE 4.0 1 6.70
CHEMBL4449806 1 -
CHEMBL4557158 1 -
CHEMBL4438467 1 -
CHEMBL4554733 1 -
CHEMBL4452169 1 -
CHEMBL4469505 1 -
CHEMBL4435098 1 -
CHEMBL4579759 1 -
CHEMBL4452761 1 -
CHEMBL4456619 1 -
CHEMBL4539630 1 -
CHEMBL4472139 1 -
CHEMBL4455798 1 -
CHEMBL4441014 1 -
CHEMBL4530231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201066 VENLAFAXINE HYDROCHLORIDE IC50 = 200.0 nM 6.70
CHEMBL4449806 IC50 > 10000.0 nM -
CHEMBL4557158 IC50 > 10000.0 nM -
CHEMBL4438467 IC50 > 10000.0 nM -
CHEMBL4554733 IC50 > 10000.0 nM -
CHEMBL4452169 IC50 > 10000.0 nM -
CHEMBL4469505 IC50 > 10000.0 nM -
CHEMBL4435098 IC50 > 10000.0 nM -
CHEMBL4579759 IC50 > 10000.0 nM -
CHEMBL4452761 IC50 > 10000.0 nM -
CHEMBL4456619 IC50 > 10000.0 nM -
CHEMBL4539630 IC50 > 10000.0 nM -
CHEMBL4472139 IC50 > 10000.0 nM -
CHEMBL4455798 IC50 > 10000.0 nM -
CHEMBL4441014 IC50 > 10000.0 nM -
CHEMBL4530231 IC50 > 10000.0 nM -