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Assay Detail

CHEMBL1115566

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

Binding
Inhibition of human SERT expressed in human JAR cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type JAR
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
Sabatucci JP, Mahaney PE, Leiter J, Johnston G, Burroughs K, Cosmi S, Zhang Y, Ho D, Deecher DC, Trybulski E.
Bioorg Med Chem Lett (2010) 20 : 2809 -2812
PubMed 20378347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.04 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1175 DULOXETINE 4.0 1 8.52
CHEMBL41 FLUOXETINE 4.0 1 8.03
CHEMBL637 VENLAFAXINE 4.0 1 7.57
CHEMBL1096495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1175 DULOXETINE IC50 = 3.0 nM 8.52
CHEMBL41 FLUOXETINE IC50 = 9.4 nM 8.03
CHEMBL637 VENLAFAXINE IC50 = 27.0 nM 7.57
CHEMBL1096495 IC50 > 2000.0 nM -