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Binding affinity to recombinant hexahistidine tagged human MT-SP1 (596 to 855 residues) expressed in Escherichia coli BL21 gold (DE3) cells using Boc-Leu-Arg-Arg-AMC as substrate by ITC analysis
Assay data:5 Active, 2 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant hexahistidine tagged human MT-SP1 (596 to 855 residues) expressed in Escherichia coli BL21 gold (DE3) cells using Boc-Leu-Arg-Arg-AMC as substrate measured every 30 secs for 10 mins by fluorescence based assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of human matriptase using Mes-D-Pro-Arg-AMC.2TFA as substrate incubated for 10 mins by fluorescence based assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Binding affinity to recombinant hexahistidine tagged human MT-SP1 (596 to 855 residues) expressed in Escherichia coli BL21 gold (DE3) cells assessed as free energy change by ITC analysis
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant hexahistidine tagged human MT-SP1 (596 to 855 residues) expressed in Escherichia coli BL21 gold (DE3) cells assessed as change in enthalpy by ITC analysis
Binding affinity to recombinant hexahistidine tagged human MT-SP1 (596 to 855 residues) expressed in Escherichia coli BL21 gold (DE3) cells assessed as change in entropy by ITC analysis
Inhibition of recombinant human Matriptase 1 ST14 catalytic domain using Boc-Gln-Ala-Arg-AMC as substrate at 3.85 to 385 nM preincubated for 30 mins followed by substrate addition and measured for 40 mins by microplate reader method
Assay data:4 Tested
Inhibition of recombinant human matriptase using Boc-QAR-MCA as substrate
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Binding affinity to N-terminal MRGS(His)6GSDDDDK-tagged Matriptase (unknown origin) expressed in Escherichia coli assessed as inhibition constant using Mes-DArg-Pro-Arg-AMC as substrate
Assay data:23 Active, 3 Activity ≤ 1 nM, 23 Activity ≤ 1 µM, 23 Tested
Inhibition of recombinant human N-terminal met-His6-tagged matriptase catalytic domain (Gly596 to Val855 residues) expressed in Escherichia coli mediated pro-HGF activation preincubated for 30 mins followed by pro-HGF addition and measured after 1 hr by immunoblotting analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of recombinant human N-terminal met-His6-tagged matriptase catalytic domain (Gly596 to Val855 residues) expressed in Escherichia coli using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorescence based assay
Assay data:18 Active, 2 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 18 Tested
Inhibition Enzymatic Assay from US Patent US9365853: "Matriptase inhibitors and uses thereof against orthomyxoviridae infections"
Assay data:7 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition Assay from US Patent US8569313: "Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors"
Assay data:46 Active, 4 Activity ≤ 1 nM, 46 Activity ≤ 1 µM, 47 Tested
Determination of Inhibition Constants from Article 10.1021/jm051272l: "Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase."
Assay data:54 Active, 54 Activity ≤ 1 µM, 54 Tested
Enzyme Inhibition Assay from Article 10.1021/jm0704898: "Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1."
Assay data:9 Active, 8 Activity ≤ 1 µM, 14 Tested
Inhibition of matriptase (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human matriptase preincubated for 15 mins followed by chromogenic substrate addition
Assay data:3 Tested
Inhibition of recombinant human N-terminal Met and 6-His-tagged matriptase (G596 to V855 residues) expressed in Escherichia coli using Boc-QAR-AMC as substrate incubated for 40 mins by FLINT assay
Assay data:9 Active, 1 Activity ≤ 1 µM, 15 Tested
Inhibition of recombinant human N-terminal met-His6-tagged matriptase catalytic domain (Gly596 to Val855 residues) expressed in Escherichia coli using Boc-QAR-AMC as substrate after 40 mins by fluorescence intensity assay
Assay data:1 Tested
Assay data:19 Active, 10 Activity ≤ 1 µM, 20 Tested
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