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Assay Detail

CHEMBL3389936

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

Binding
Inhibition of recombinant hepsin (unknown origin) using Boc-QAR-AMC as substrate by fluorescence assay
20
Total Activities
20
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

Serine protease hepsin (CHEMBL2079849)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.
Han Z, Harris PK, Jones DE, Chugani R, Kim T, Agarwal M, Shen W, Wildman SA, Janetka JW.
ACS Med Chem Lett (2014) 5 : 1219 -1224
PubMed 25408834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 9.10 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356591 1 9.68
CHEMBL3356597 1 9.68
CHEMBL3356589 1 9.66
CHEMBL3356594 1 9.55
CHEMBL3356595 1 9.47
CHEMBL3356590 1 9.39
CHEMBL3356606 1 9.33
CHEMBL273264 NAFAMOSTAT 3.0 1 9.28
CHEMBL3356600 1 9.26
CHEMBL3356596 1 9.24
CHEMBL3356592 1 9.24
CHEMBL3356599 1 9.22
CHEMBL3356604 1 9.21
CHEMBL3356603 1 9.17
CHEMBL3356598 1 8.92
CHEMBL3356605 1 8.92
CHEMBL3356602 1 8.85
CHEMBL3356593 1 8.68
CHEMBL3356601 1 8.07
CHEMBL191881 LEUPEPTIN 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356591 Ki = 0.21 nM 9.68
CHEMBL3356597 Ki = 0.21 nM 9.68
CHEMBL3356589 Ki = 0.22 nM 9.66
CHEMBL3356594 Ki = 0.28 nM 9.55
CHEMBL3356595 Ki = 0.34 nM 9.47
CHEMBL3356590 Ki = 0.41 nM 9.39
CHEMBL3356606 Ki = 0.47 nM 9.33
CHEMBL273264 NAFAMOSTAT Ki = 0.53 nM 9.28
CHEMBL3356600 Ki = 0.55 nM 9.26
CHEMBL3356596 Ki = 0.57 nM 9.24
CHEMBL3356592 Ki = 0.58 nM 9.24
CHEMBL3356599 Ki = 0.6 nM 9.22
CHEMBL3356604 Ki = 0.61 nM 9.21
CHEMBL3356603 Ki = 0.68 nM 9.17
CHEMBL3356598 Ki = 1.2 nM 8.92
CHEMBL3356605 Ki = 1.2 nM 8.92
CHEMBL3356602 Ki = 1.4 nM 8.85
CHEMBL3356593 Ki = 2.1 nM 8.68
CHEMBL3356601 Ki = 8.5 nM 8.07
CHEMBL191881 LEUPEPTIN Ki = 61.0 nM 7.21