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Assay Detail

CHEMBL962314

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

Binding
Inhibition of serotonin uptake at human SERT expressed in JAR cells
14
Total Activities
14
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

Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Zhang P, Terefenko EA, McComas CC, Mahaney PE, Vu A, Trybulski E, Koury E, Johnston G, Bray J, Deecher D.
Bioorg Med Chem Lett (2008) 18 : 6067 -6070
PubMed 18951020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.24 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41 FLUOXETINE 4.0 1 8.03
CHEMBL641 ATOMOXETINE 4.0 1 7.32
CHEMBL514193 1 6.78
CHEMBL14370 REBOXETINE 4.0 1 6.62
CHEMBL512677 1 6.56
CHEMBL453838 1 6.49
CHEMBL511827 1 6.32
CHEMBL516965 1 5.92
CHEMBL470313 1 5.85
CHEMBL475527 1 5.72
CHEMBL471519 1 5.52
CHEMBL461323 1 5.51
CHEMBL461153 1 5.37
CHEMBL461322 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41 FLUOXETINE IC50 = 9.4 nM 8.03
CHEMBL641 ATOMOXETINE IC50 = 48.0 nM 7.32
CHEMBL514193 IC50 = 166.0 nM 6.78
CHEMBL14370 REBOXETINE IC50 = 242.0 nM 6.62
CHEMBL512677 IC50 = 273.0 nM 6.56
CHEMBL453838 IC50 = 327.0 nM 6.49
CHEMBL511827 IC50 = 483.0 nM 6.32
CHEMBL516965 IC50 = 1208.0 nM 5.92
CHEMBL470313 IC50 = 1408.0 nM 5.85
CHEMBL475527 IC50 = 1910.0 nM 5.72
CHEMBL471519 IC50 = 2995.0 nM 5.52
CHEMBL461323 IC50 = 3100.0 nM 5.51
CHEMBL461153 IC50 = 4311.0 nM 5.37
CHEMBL461322 IC50 = 4565.0 nM 5.34