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Assay Detail

CHEMBL4671982

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

Binding
Inhibition of TrxR in human BEL-7402/5-FU cells by colorimetric assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BEL-7402/5-FU
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thioredoxin reductase 1, cytoplasmic (CHEMBL1927)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.
Zhu P,Qian J,Xu Z,Meng C,Liu J,Shan W,Zhu W,Wang Y,Yang Y,Zhang W,Zhang Y,Ling Y
J Nat Prod (2020) 83 : 3041 -3049
PubMed 33026807 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.35 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757091 1 6.70
CHEMBL4755909 1 6.70
CHEMBL4798017 1 6.40
CHEMBL4763453 1 6.22
CHEMBL465843 PIPLARTINE 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757091 IC50 = 200.0 nM 6.70
CHEMBL4755909 IC50 = 200.0 nM 6.70
CHEMBL4798017 IC50 = 400.0 nM 6.40
CHEMBL4763453 IC50 = 600.0 nM 6.22
CHEMBL465843 PIPLARTINE IC50 = 1800.0 nM 5.75