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Assay Detail

CHEMBL656194

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

Binding
Inhibitory activity using recombinant human Calpain 1 with Suc-Leu-Tyr-MNA as substrate.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Nonpeptidic inhibitors of recombinant human calpain I
Chatterjee S, Senadhi S, Bozyczko-Coyne D, Siman R, Mallamo JP
Bioorg Med Chem Lett (1997) 7 : 287 -290
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.30 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 7.96
CHEMBL42716 1 7.60
CHEMBL98832 1 7.52
CHEMBL100316 1 7.30
CHEMBL439590 1 7.12
CHEMBL316721 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 11.0 nM 7.96
CHEMBL42716 IC50 = 25.0 nM 7.60
CHEMBL98832 IC50 = 30.0 nM 7.52
CHEMBL100316 IC50 = 50.0 nM 7.30
CHEMBL439590 IC50 = 75.0 nM 7.12
CHEMBL316721 IC50 = 500.0 nM 6.30