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Assay Detail

CHEMBL3404294

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Binding
Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor activator (CHEMBL3351190)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.
Franco FM, Jones DE, Harris PK, Han Z, Wildman SA, Jarvis CM, Janetka JW.
Bioorg Med Chem (2015) 23 : 2328 -2343
PubMed 25882520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.85 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273264 NAFAMOSTAT 3.0 1 6.82
CHEMBL3403524 1 6.52
CHEMBL3403525 1 6.22
CHEMBL550687 1 6.09
CHEMBL1195245 1 5.96
CHEMBL3403523 1 5.52
CHEMBL3403522 1 5.17
CHEMBL590799 CAMOSTAT 3.0 1 4.50
CHEMBL579653 1 -
CHEMBL535214 1 -
CHEMBL3403527 1 -
CHEMBL3403526 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273264 NAFAMOSTAT IC50 = 150.0 nM 6.82
CHEMBL3403524 IC50 = 300.0 nM 6.52
CHEMBL3403525 IC50 = 600.0 nM 6.22
CHEMBL550687 IC50 = 820.0 nM 6.09
CHEMBL1195245 IC50 = 1100.0 nM 5.96
CHEMBL3403523 IC50 = 3000.0 nM 5.52
CHEMBL3403522 IC50 = 6800.0 nM 5.17
CHEMBL590799 CAMOSTAT IC50 = 32000.0 nM 4.50
CHEMBL579653 IC50 > 50000.0 nM -
CHEMBL535214 IC50 > 50000.0 nM -
CHEMBL3403527 IC50 > 50000.0 nM -
CHEMBL3403526 IC50 > 50000.0 nM -