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Assay Detail

CHEMBL4254543

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

Binding
Inhibition of [3H]serotonin reuptake in rat brain synaptosomes SERT after 15 mins by TopCount scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular synaptosomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Zhou AN, Xiao Y, Zhang QW, Li JQ.
Eur J Med Chem (2018) 144 : 701 -715
PubMed 29291438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.10 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2104993 VORTIOXETINE 4.0 1 8.54
CHEMBL4286174 1 8.12
CHEMBL4288120 1 8.03
CHEMBL4277476 1 8.00
CHEMBL4289783 1 7.60
CHEMBL4289605 1 7.51
CHEMBL4278933 1 7.38
CHEMBL4294077 1 7.02
CHEMBL4291322 1 6.96
CHEMBL4279099 1 6.92
CHEMBL4285796 1 6.82
CHEMBL4277854 1 6.80
CHEMBL4283479 1 6.72
CHEMBL4279592 1 6.68
CHEMBL4288753 1 6.23
CHEMBL4278094 1 5.77
CHEMBL4294729 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2104993 VORTIOXETINE IC50 = 2.9 nM 8.54
CHEMBL4286174 IC50 = 7.6 nM 8.12
CHEMBL4288120 IC50 = 9.4 nM 8.03
CHEMBL4277476 IC50 = 10.0 nM 8.00
CHEMBL4289783 IC50 = 25.0 nM 7.60
CHEMBL4289605 IC50 = 31.0 nM 7.51
CHEMBL4278933 IC50 = 42.0 nM 7.38
CHEMBL4294077 IC50 = 96.0 nM 7.02
CHEMBL4291322 IC50 = 110.0 nM 6.96
CHEMBL4279099 IC50 = 120.0 nM 6.92
CHEMBL4285796 IC50 = 150.0 nM 6.82
CHEMBL4277854 IC50 = 160.0 nM 6.80
CHEMBL4283479 IC50 = 190.0 nM 6.72
CHEMBL4279592 IC50 = 210.0 nM 6.68
CHEMBL4288753 IC50 = 590.0 nM 6.23
CHEMBL4278094 IC50 = 1700.0 nM 5.77
CHEMBL4294729 IC50 = 2900.0 nM 5.54