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Determination of Related Protease Inhibition from US Patent US20240059691: "ENZYME INHIBITORS"
Assay data:279 Active, 16 Activity ≤ 1 nM, 253 Activity ≤ 1 µM, 299 Tested
SummaryRelated BioAssays by Target
Factor Xa Serine protease panel
Assay data:1 Tested
Urokinase Serine protease panel
Thrombin Serine protease panel
Plasmin Serine protease panel
Compound was evaluated for inhibition of human F2 in an in vitro cell free assay measured by fluorescence spectroscopy
Assay data:11 Active, 8 Activity ≤ 1 µM, 927 Tested
Inhibition of thrombin (unknown origin)
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
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
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
Binding affinity to human FXa assessed as inhibition constant
Assay data:4 Active, 3 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Binding affinity to FXa (unknown origin) assessed as inhibition constant
Assay data:6 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 6 Tested
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 human FXa using methoxycarbonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide as substrate at >200 uM by chromogenic substrate hydrolysis assay
Assay data:2 Active, 2 Tested
Inhibition of human FXa using methoxycarbonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide as substrate at 500 uM by chromogenic substrate hydrolysis assay
Assay data:25 Tested
Inhibition of human thrombin at 500 uM by chromogenic substrate hydrolysis assay
Assay data:27 Tested
Inhibition of factor Xa (unknown origin) assessed as inhibition constant
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
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