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Assay Detail

CHEMBL3829451

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

Binding
Inhibition of recombinant human ERAP2 using R-AMC as substrate measured for 15 to 30 mins by microplate fluorescence reader method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endoplasmic reticulum aminopeptidase 2 (CHEMBL5043)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective inhibitors of human aminopeptidases ERAP1 and ERAP2 by screening libraries of phosphorus-containing amino acid and dipeptide analogues.
Węglarz-Tomczak E, Vassiliou S, Mucha A.
Bioorg Med Chem Lett (2016) 26 : 4122 -4126
PubMed 27390066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.11 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416733 1 7.96
CHEMBL3827468 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416733 IC50 = 11.0 nM 7.96
CHEMBL3827468 IC50 = 550.0 nM 6.26