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Assay Detail

CHEMBL1007397

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

Binding
Blockade of cathepsin G processing in human U937 cells by densitometry
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cathepsin G (CHEMBL4071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD.
J Biol Chem (2007) 282 : 20836 -20846
PubMed 17535802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.44 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL515494 1 7.05
CHEMBL516292 1 6.82
CHEMBL63440 ALOXISTATIN 2.0 1 5.96
CHEMBL1162477 1 5.92
CHEMBL478737 1 -
CHEMBL1162478 1 -
CHEMBL400387 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL515494 IC50 = 90.0 nM 7.05
CHEMBL516292 IC50 = 150.0 nM 6.82
CHEMBL63440 ALOXISTATIN IC50 = 1100.0 nM 5.96
CHEMBL1162477 IC50 = 1200.0 nM 5.92
CHEMBL478737 IC50 > 50000.0 nM -
CHEMBL1162478 IC50 - -
CHEMBL400387 IC50 > 50000.0 nM -