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Assay Detail

CHEMBL2090833

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

Binding
Tight binding inhibition of human matriptase expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type S2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Suppressor of tumorigenicity 14 protein (CHEMBL3018)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent, selective inhibitors of matriptase.
Colombo E, Désilets A, Duchêne D, Chagnon F, Najmanovich R, Leduc R, Marsault E.
ACS Med Chem Lett (2012) 3 : 530 -534
PubMed 24900505 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 9.25 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2086421 1 10.96
CHEMBL2089123 1 10.06
CHEMBL2089124 1 8.85
CHEMBL2089154 1 8.34
CHEMBL2089122 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2086421 Ki = 0.011 nM 10.96
CHEMBL2089123 Ki = 0.088 nM 10.06
CHEMBL2089124 Ki = 1.4 nM 8.85
CHEMBL2089154 Ki = 4.6 nM 8.34
CHEMBL2089122 Ki = 9.5 nM 8.02