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Assay Detail

CHEMBL3404295

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

Binding
Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells using Boc-QLR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay
16
Total Activities
16
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
Ki 16 5.15 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273264 NAFAMOSTAT 3.0 1 7.60
CHEMBL379186 1 5.26
CHEMBL3403521 1 5.15
CHEMBL3403528 1 5.00
CHEMBL3403529 1 4.85
CHEMBL3403531 1 4.79
CHEMBL379586 1 4.77
CHEMBL356792 1 4.74
CHEMBL3403532 1 4.70
CHEMBL3402440 1 4.65
CHEMBL3402437 1 -
CHEMBL3400827 1 -
CHEMBL3403533 1 -
CHEMBL3403530 1 -
CHEMBL3402439 1 -
CHEMBL3402438 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273264 NAFAMOSTAT Ki = 25.0 nM 7.60
CHEMBL379186 Ki = 5500.0 nM 5.26
CHEMBL3403521 Ki = 7100.0 nM 5.15
CHEMBL3403528 Ki = 10100.0 nM 5.00
CHEMBL3403529 Ki = 14000.0 nM 4.85
CHEMBL3403531 Ki = 16200.0 nM 4.79
CHEMBL379586 Ki = 17000.0 nM 4.77
CHEMBL356792 Ki = 18200.0 nM 4.74
CHEMBL3403532 Ki = 20000.0 nM 4.70
CHEMBL3402440 Ki = 22200.0 nM 4.65
CHEMBL3402437 Ki > 50000.0 nM -
CHEMBL3400827 Ki > 50000.0 nM -
CHEMBL3403533 Ki > 50000.0 nM -
CHEMBL3403530 Ki > 50000.0 nM -
CHEMBL3402439 Ki > 50000.0 nM -
CHEMBL3402438 Ki > 50000.0 nM -