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Assay Detail

CHEMBL4822047

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 incubated for 5 to 10 mins by fluorescence based assay
1
Total Activities
1
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

Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.
Wilding B, Pasqua AE, E A Chessum N, Pierrat OA, Hahner T, Tomlin K, Shehu E, Burke R, Richards GM, Whitton B, Arwert EN, Thapaliya A, Salimraj R, van Montfort R, Skawinska A, Hayes A, Raynaud F, Chopra R, Jones K, Newton G, Cheeseman MD.
Bioorg Med Chem Lett (2021) 42 : 128050 -128050
PubMed 33887439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.96 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416733 1 7.96

Activity Data

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