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Assay Detail

CHEMBL1676765

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

Binding
Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay
17
Total Activities
17
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

Synthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1-propenes as a new class of anticancer agents.
McNamara YM, Cloonan SM, Knox AJ, Keating JJ, Butler SG, Peters GH, Meegan MJ, Williams DC.
Bioorg Med Chem (2011) 19 : 1328 -1348
PubMed 21227702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.00 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL549 CITALOPRAM 4.0 1 7.72
CHEMBL6467 4-METHYLTHIOAMPHETAMINE 1 6.70
CHEMBL6731 TENAMFETAMINE 2.0 1 6.05
CHEMBL43048 MIDOMAFETAMINE 3.0 1 5.96
CHEMBL1672015 1 5.80
CHEMBL1672023 1 5.72
CHEMBL1165303 1 5.66
CHEMBL1164191 1 5.60
CHEMBL1165775 1 4.80
CHEMBL1672014 1 -
CHEMBL1672016 1 -
CHEMBL1672018 1 -
CHEMBL1672019 1 -
CHEMBL1165387 1 -
CHEMBL1672021 1 -
CHEMBL1672022 1 -
CHEMBL1671870 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL549 CITALOPRAM IC50 = 19.0 nM 7.72
CHEMBL6467 4-METHYLTHIOAMPHETAMINE IC50 = 200.0 nM 6.70
CHEMBL6731 TENAMFETAMINE IC50 = 900.0 nM 6.05
CHEMBL43048 MIDOMAFETAMINE IC50 = 1100.0 nM 5.96
CHEMBL1672015 IC50 = 1600.0 nM 5.80
CHEMBL1672023 IC50 = 1900.0 nM 5.72
CHEMBL1165303 IC50 = 2200.0 nM 5.66
CHEMBL1164191 IC50 = 2500.0 nM 5.60
CHEMBL1165775 IC50 = 15700.0 nM 4.80
CHEMBL1672014 IC50 - -
CHEMBL1672016 IC50 - -
CHEMBL1672018 IC50 - -
CHEMBL1672019 IC50 - -
CHEMBL1165387 IC50 - -
CHEMBL1672021 IC50 - -
CHEMBL1672022 IC50 - -
CHEMBL1671870 IC50 - -