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Assay Detail

CHEMBL867681

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

Binding
Inhibition of isolated human calpain1
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Expert

Target

Calpain 1 (CHEMBL2111357)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel dual inhibitors of calpain and lipid peroxidation with enhanced cellular activity.
Auvin S, Pignol B, Navet E, Troadec M, Carré D, Camara J, Bigg D, Chabrier PE.
Bioorg Med Chem Lett (2006) 16 : 1586 -1589
PubMed 16380258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.06 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203568 1 8.31
CHEMBL204883 1 8.10
CHEMBL439155 1 7.60
CHEMBL201990 1 7.42
CHEMBL383110 1 7.31
CHEMBL206235 1 7.26
CHEMBL203570 1 7.12
CHEMBL203244 1 7.07
CHEMBL204229 1 7.05
CHEMBL203632 2 6.98
CHEMBL204046 1 6.86
CHEMBL412566 1 6.82
CHEMBL206453 1 6.82
CHEMBL203448 1 6.65
CHEMBL206126 1 6.45
CHEMBL204398 1 6.26
CHEMBL206571 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203568 IC50 = 4.9 nM 8.31
CHEMBL204883 IC50 = 8.0 nM 8.10
CHEMBL439155 IC50 = 25.0 nM 7.60
CHEMBL201990 IC50 = 38.0 nM 7.42
CHEMBL383110 IC50 = 48.7 nM 7.31
CHEMBL206235 IC50 = 55.4 nM 7.26
CHEMBL203570 IC50 = 75.9 nM 7.12
CHEMBL203244 IC50 = 85.5 nM 7.07
CHEMBL204229 IC50 = 88.6 nM 7.05
CHEMBL203632 IC50 = 105.0 nM 6.98
CHEMBL203632 IC50 = 105.0 nM 6.98
CHEMBL204046 IC50 = 138.0 nM 6.86
CHEMBL412566 IC50 = 150.9 nM 6.82
CHEMBL206453 IC50 = 150.0 nM 6.82
CHEMBL203448 IC50 = 222.0 nM 6.65
CHEMBL206126 IC50 = 354.1 nM 6.45
CHEMBL204398 IC50 = 553.2 nM 6.26
CHEMBL206571 IC50 = 905.0 nM 6.04