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Assay Detail

CHEMBL4038151

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

Binding
Inhibition of recombinant human N-terminal 6His-tagged matriptase catalytic domain (596 to 855 residues) expressed in Escherichia coli using fluorogenic Boc-QAR-AMC peptide as substrate after 5 mins by fluorescence based assay
3
Total Activities
3
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

Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Teufel DP, Bennett G, Harrison H, van Rietschoten K, Pavan S, Stace C, Le Floch F, Van Bergen T, Vermassen E, Barbeaux P, Hu TT, Feyen JHM, Vanhove M.
J Med Chem (2018) 61 : 2823 -2836
PubMed 29517911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 4.51 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4070056 1 4.82
CHEMBL4059991 1 4.40
CHEMBL4094403 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4070056 Ki = 15000.0 nM 4.82
CHEMBL4059991 Ki = 40000.0 nM 4.40
CHEMBL4094403 Ki = 50000.0 nM 4.30