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Assay Detail

CHEMBL3829339

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Binding
Inhibition of human matriptase using Boc-Gln-Ala-Arg-AMC as substrate after 20 mins by fluorimetric analysis
7
Total Activities
7
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

Evaluation of bisbenzamidines as inhibitors for matriptase-2.
Beckmann AM, Gilberg E, Gattner S, Huang TL, Vanden Eynde JJ, Mayence A, Bajorath J, Stirnberg M, Gütschow M.
Bioorg Med Chem Lett (2016) 26 : 3741 -3745
PubMed 27287367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.16 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269032 1 6.40
CHEMBL3828410 1 6.31
CHEMBL3594083 1 6.28
CHEMBL3594082 1 6.25
CHEMBL9126 1 6.14
CHEMBL365916 1 6.09
CHEMBL181480 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269032 Ki = 397.0 nM 6.40
CHEMBL3828410 Ki = 492.0 nM 6.31
CHEMBL3594083 Ki = 526.0 nM 6.28
CHEMBL3594082 Ki = 558.0 nM 6.25
CHEMBL9126 Ki = 719.0 nM 6.14
CHEMBL365916 Ki = 816.0 nM 6.09
CHEMBL181480 Ki = 2280.0 nM 5.64