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Assay Detail

CHEMBL4718401

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

Binding
Competitive inhibition of human erythrocytes mu-calpain using varying level of Pep2 as substrate by Lineweaver-Burk plot analysis
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Calpain-1 catalytic subunit (CHEMBL3891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
Jeon KH,Lee E,Jun KY,Eom JE,Kwak SY,Na Y,Kwon Y
Eur J Med Chem (2016) 121 : 433 -444
PubMed 27318120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.98 5.24
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756611 2 5.24
CHEMBL4740912 2 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756611 Ki = 5730.0 nM 5.24
CHEMBL4740912 Ki = 19260.0 nM 4.71
CHEMBL4756611 Inhibition - % -
CHEMBL4740912 Inhibition - % -