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Assay Detail

CHEMBL1021957

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

Binding
Inhibition of human erythrocytes mu-calpain by fluorometric assay using pep2 as substrate
23
Total Activities
23
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

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

Publication

Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
Kang DH, Jun KY, Lee JP, Pak CS, Na Y, Kwon Y.
J Med Chem (2009) 52 : 3093 -3097
PubMed 19419206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.54 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 6.70
CHEMBL470707 1 5.77
CHEMBL521771 1 5.62
CHEMBL523822 1 5.51
CHEMBL471915 1 5.50
CHEMBL491348 1 5.50
CHEMBL521636 1 5.13
CHEMBL492175 1 5.09
CHEMBL513042 1 5.00
CHEMBL489728 1 -
CHEMBL489727 1 -
CHEMBL492089 1 -
CHEMBL489535 1 -
CHEMBL491899 1 -
CHEMBL492180 1 -
CHEMBL491898 1 -
CHEMBL489530 1 -
CHEMBL491964 1 -
CHEMBL471916 1 -
CHEMBL512192 1 -
CHEMBL490503 1 -
CHEMBL523140 1 -
CHEMBL491513 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 199.0 nM 6.70
CHEMBL470707 IC50 = 1690.0 nM 5.77
CHEMBL521771 IC50 = 2390.0 nM 5.62
CHEMBL523822 IC50 = 3060.0 nM 5.51
CHEMBL471915 IC50 = 3170.0 nM 5.50
CHEMBL491348 IC50 = 3160.0 nM 5.50
CHEMBL521636 IC50 = 7430.0 nM 5.13
CHEMBL492175 IC50 = 8080.0 nM 5.09
CHEMBL513042 IC50 = 9940.0 nM 5.00
CHEMBL489728 IC50 - -
CHEMBL489727 IC50 - -
CHEMBL492089 IC50 - -
CHEMBL489535 IC50 - -
CHEMBL491899 IC50 - -
CHEMBL492180 IC50 - -
CHEMBL491898 IC50 - -
CHEMBL489530 IC50 - -
CHEMBL491964 IC50 - -
CHEMBL471916 IC50 - -
CHEMBL512192 IC50 - -
CHEMBL490503 IC50 - -
CHEMBL523140 IC50 - -
CHEMBL491513 IC50 - -