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Assay Detail

CHEMBL4399088

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

Binding
Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using insulin as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by fluorescence based assay
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

Insulin-degrading enzyme (CHEMBL1293287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.
Leroux F, Bosc D, Beghyn T, Hermant P, Warenghem S, Landry V, Pottiez V, Guillaume V, Charton J, Herledan A, Urata S, Liang W, Sheng L, Tang WJ, Deprez B, Deprez-Poulain R.
Eur J Med Chem (2019) 179 : 557 -566
PubMed 31276900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.55 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51085 EBSELEN 3.0 1 7.85
CHEMBL4241044 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51085 EBSELEN IC50 = 14.0 nM 7.85
CHEMBL4241044 IC50 = 56.0 nM 7.25