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Assay Detail

CHEMBL1120736

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

Binding
Inhibition of SERT-mediated serotonin uptake in human JAR cells
3
Total Activities
3
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

Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).
O'Neill DJ, Adedoyin A, Alfinito PD, Bray JA, Cosmi S, Deecher DC, Fensome A, Harrison J, Leventhal L, Mann C, McComas CC, Sullivan NR, Spangler TB, Uveges AJ, Trybulski EJ, Whiteside GT, Zhang P.
J Med Chem (2010) 53 : 4511 -4521
PubMed 20462211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.35 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41 FLUOXETINE 4.0 1 8.03
CHEMBL1085831 1 5.69
CHEMBL1083083 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41 FLUOXETINE IC50 = 9.4 nM 8.03
CHEMBL1085831 IC50 = 2042.0 nM 5.69
CHEMBL1083083 IC50 = 4589.0 nM 5.34