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Assay Detail

CHEMBL973384

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

Binding
Inhibition of human erythrocytes mu-calpain by spectrofluorimeter
13
Total Activities
13
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

Design and synthesis of calpain inhibitory 6-pyridone 2-carboxamide derivatives.
Lee KY, Lee KS, Jin C, Lee YS.
Eur J Med Chem (2009) 44 : 1331 -1334
PubMed 18396356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.88 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 7.16
CHEMBL492083 1 5.55
CHEMBL492081 1 5.21
CHEMBL491919 1 5.21
CHEMBL491918 1 5.13
CHEMBL491749 1 4.66
CHEMBL492082 1 4.47
CHEMBL522312 1 4.45
CHEMBL489722 1 4.40
CHEMBL490564 1 4.19
CHEMBL524152 1 4.07
CHEMBL489721 1 4.04
CHEMBL489723 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 70.0 nM 7.16
CHEMBL492083 IC50 = 2810.0 nM 5.55
CHEMBL492081 IC50 = 6190.0 nM 5.21
CHEMBL491919 IC50 = 6190.0 nM 5.21
CHEMBL491918 IC50 = 7410.0 nM 5.13
CHEMBL491749 IC50 = 22130.0 nM 4.66
CHEMBL492082 IC50 = 34010.0 nM 4.47
CHEMBL522312 IC50 = 35260.0 nM 4.45
CHEMBL489722 IC50 = 40170.0 nM 4.40
CHEMBL490564 IC50 = 64610.0 nM 4.19
CHEMBL524152 IC50 = 84750.0 nM 4.07
CHEMBL489721 IC50 = 91420.0 nM 4.04
CHEMBL489723 IC50 > 100000.0 nM -