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Assay Detail

CHEMBL3224718

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

Binding
Inhibition of Ca2+-dependent activation of porcine calpain-1 using SucLY-AMC as substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL4062)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates
Adams SE, Parr C, Miller DJ, Allemann RK, Hallett MB
Medchemcomm (2012) 3 : 566 -570
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.01 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3221938 1 7.70
CHEMBL3221937 1 7.30
CHEMBL3221946 1 7.16
CHEMBL3221945 1 7.05
CHEMBL3221942 1 7.05
CHEMBL3221939 1 7.05
CHEMBL3221941 1 7.00
CHEMBL3221935 1 7.00
CHEMBL3221944 1 6.96
CHEMBL3221934 1 6.85
CHEMBL3221947 1 6.66
CHEMBL3221943 1 6.52
CHEMBL3221940 1 6.52
CHEMBL3221933 1 6.52
CHEMBL3221936 1 6.03
CHEMBL3221932 1 5.82
CHEMBL366254 1 5.28
CHEMBL3221930 1 5.25
CHEMBL3221928 1 5.08
CHEMBL3221924 1 5.04
CHEMBL3221927 1 4.88
CHEMBL3221931 1 4.82
CHEMBL3221923 1 4.68
CHEMBL3221922 1 4.63
CHEMBL3221929 1 4.62
CHEMBL3221926 1 4.50
CHEMBL3221925 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3221938 IC50 = 20.0 nM 7.70
CHEMBL3221937 IC50 = 50.0 nM 7.30
CHEMBL3221946 IC50 = 70.0 nM 7.16
CHEMBL3221945 IC50 = 90.0 nM 7.05
CHEMBL3221942 IC50 = 90.0 nM 7.05
CHEMBL3221939 IC50 = 90.0 nM 7.05
CHEMBL3221941 IC50 = 100.0 nM 7.00
CHEMBL3221935 IC50 = 100.0 nM 7.00
CHEMBL3221944 IC50 = 110.0 nM 6.96
CHEMBL3221934 IC50 = 140.0 nM 6.85
CHEMBL3221947 IC50 = 220.0 nM 6.66
CHEMBL3221943 IC50 = 300.0 nM 6.52
CHEMBL3221940 IC50 = 300.0 nM 6.52
CHEMBL3221933 IC50 = 300.0 nM 6.52
CHEMBL3221936 IC50 = 930.0 nM 6.03
CHEMBL3221932 IC50 = 1500.0 nM 5.82
CHEMBL366254 IC50 = 5200.0 nM 5.28
CHEMBL3221930 IC50 = 5600.0 nM 5.25
CHEMBL3221928 IC50 = 8400.0 nM 5.08
CHEMBL3221924 IC50 = 9100.0 nM 5.04
CHEMBL3221927 IC50 = 13100.0 nM 4.88
CHEMBL3221931 IC50 = 15000.0 nM 4.82
CHEMBL3221923 IC50 = 20700.0 nM 4.68
CHEMBL3221922 IC50 = 23200.0 nM 4.63
CHEMBL3221929 IC50 = 23900.0 nM 4.62
CHEMBL3221926 IC50 = 31500.0 nM 4.50
CHEMBL3221925 IC50 = 42800.0 nM 4.37