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Assay Detail

CHEMBL3404296

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

Binding
Inhibition of matripase (unknown origin) using Boc-QAR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Suppressor of tumorigenicity 14 protein (CHEMBL3018)
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 17 6.22 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273264 NAFAMOSTAT 3.0 1 10.70
CHEMBL379586 1 8.37
CHEMBL379186 1 6.92
CHEMBL3403528 1 6.52
CHEMBL3403532 1 6.32
CHEMBL3402439 1 6.21
CHEMBL3402440 1 6.12
CHEMBL3403530 1 5.92
CHEMBL3402437 1 5.82
CHEMBL356792 1 5.75
CHEMBL3403533 1 5.60
CHEMBL3403529 1 5.58
CHEMBL198362 RIVAROXABAN 4.0 1 5.47
CHEMBL3403531 1 5.34
CHEMBL3402438 1 5.17
CHEMBL3403521 1 5.14
CHEMBL3400827 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273264 NAFAMOSTAT Ki = 0.02 nM 10.70
CHEMBL379586 Ki = 4.3 nM 8.37
CHEMBL379186 Ki = 120.0 nM 6.92
CHEMBL3403528 Ki = 300.0 nM 6.52
CHEMBL3403532 Ki = 480.0 nM 6.32
CHEMBL3402439 Ki = 620.0 nM 6.21
CHEMBL3402440 Ki = 760.0 nM 6.12
CHEMBL3403530 Ki = 1200.0 nM 5.92
CHEMBL3402437 Ki = 1500.0 nM 5.82
CHEMBL356792 Ki = 1800.0 nM 5.75
CHEMBL3403533 Ki = 2500.0 nM 5.60
CHEMBL3403529 Ki = 2600.0 nM 5.58
CHEMBL198362 RIVAROXABAN Ki = 3350.0 nM 5.47
CHEMBL3403531 Ki = 4600.0 nM 5.34
CHEMBL3402438 Ki = 6700.0 nM 5.17
CHEMBL3403521 Ki = 7180.0 nM 5.14
CHEMBL3400827 Ki = 14900.0 nM 4.83