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Assay Detail

CHEMBL654084

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

Binding
Inhibitory activity of compound against recombinant human Calpain 1
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

Xanthene derived potent nonpeptidic inhibitors of recombinant human calpain I
Chatterjee S, Iqbal M, Kauer JC, Mallamo JP, Senadhi S, Mallya S, Bozyczko-Coyne D, Siman R
Bioorg Med Chem Lett (1996) 6 : 1619 -1622
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.17 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 7.77
CHEMBL42716 1 7.60
CHEMBL42617 1 7.30
CHEMBL41337 1 6.89
CHEMBL41336 1 6.86
CHEMBL296285 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 17.0 nM 7.77
CHEMBL42716 IC50 = 25.0 nM 7.60
CHEMBL42617 IC50 = 50.0 nM 7.30
CHEMBL41337 IC50 = 130.0 nM 6.89
CHEMBL41336 IC50 = 138.0 nM 6.86
CHEMBL296285 IC50 = 240.0 nM 6.62