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Assay Detail

CHEMBL4122691

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

Binding
Inhibition of SERT (unknown origin) expressed in HEK293 cells assessed as reduction in 5-HT uptake incubated for 30 mins
6
Total Activities
6
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

Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
Liu W, Wang H, Li X, Xu Y, Zhang J, Wang W, Gong Q, Qiu X, Zhu J, Mao F, Zhang H, Li J.
Bioorg Med Chem (2018) 26 : 3117 -3125
PubMed 29729987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.68 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.40
CHEMBL549 CITALOPRAM 4.0 1 8.20
CHEMBL4126644 1 7.69
CHEMBL4128689 1 7.66
CHEMBL4126958 1 6.64
CHEMBL4129019 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE IC50 = 0.4 nM 9.40
CHEMBL549 CITALOPRAM IC50 = 6.27 nM 8.20
CHEMBL4126644 IC50 = 20.42 nM 7.69
CHEMBL4128689 IC50 = 22.1 nM 7.66
CHEMBL4126958 IC50 = 229.3 nM 6.64
CHEMBL4129019 IC50 = 314.1 nM 6.50