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Assay Detail

CHEMBL4182004

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

Binding
Inhibition of SERT in rat brain synaptosomes assessed as reduction in [3H]-5-HT uptake measured after 15 mins by scintillation counting method
7
Total Activities
7
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 activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Xiao Y, Zhang QW, Li JQ.
Bioorg Med Chem Lett (2017) 27 : 5420 -5423
PubMed 29138029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.63 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2104993 VORTIOXETINE 4.0 1 8.54
CHEMBL4209430 1 7.00
CHEMBL4203932 1 6.47
CHEMBL4217086 1 6.23
CHEMBL4215605 1 6.08
CHEMBL4211687 1 6.06
CHEMBL4205570 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2104993 VORTIOXETINE IC50 = 2.9 nM 8.54
CHEMBL4209430 IC50 = 100.0 nM 7.00
CHEMBL4203932 IC50 = 340.0 nM 6.47
CHEMBL4217086 IC50 = 590.0 nM 6.23
CHEMBL4215605 IC50 = 840.0 nM 6.08
CHEMBL4211687 IC50 = 880.0 nM 6.06
CHEMBL4205570 IC50 = 950.0 nM 6.02