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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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Factor Xa Serine protease panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Binding affinity to human FXa assessed as inhibition constant
Assay data:4 Active, 3 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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 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
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of factor Xa (unknown origin) assessed as inhibition constant
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Potency index, ratio of rivaroxaban IC50 to test compound IC50 for inhibition of factor Xa (unknown origin)
Assay data:2 Tested
Inhibition of factor Xa (unknown origin)
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of factor Xa (unknown origin) assessed as residual enzymatic activity at 20 nM (Rvb = 127.54%)
Assay data:4 Tested
Inhibition of human fXA by fluorescence based analysis
Inhibition of fXa (unknown origin)
Inhibition of factor Xa (unknown origin) using Boc-Ile-Glu-Gly-Arg-AMC as substrate preincubated with compound for 15 mins followed by substrate addition and measured after 15 mins by fluorescence based assay
Inhibition of factor Xa (unknown origin) using CH3OCO-dCha-Gly-Arg-pNA as substrate by fluorescence plate reader analysis
Enzymatic Activity Assay from US Patent US20230391761: "SUBSTITUTED S-ALANINATE DERIVATIVES"
Assay data:17 Active, 14 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In Vitro Testing of Human Factor Xa Assay from US Patent US11691960: "2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamide derivatives and the use thereof as medicament"
Assay data:5 Active, 5 Activity ≤ 1 µM, 13 Tested
Inhibition of Factor Xa from US Patent US11541049: "Tetrahydroisoquinoline derivatives, preparation process and use thereof"
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (Serine protease panel) EUB0000735a F10
Inhibition of heparin binding to factor 10a using chromogenic substrate incubated for 7 min by absorbance based assay
Assay data:4 Active, 3 Activity ≤ 1 µM, 5 Tested
Inhibition of coagulation factor Xa (unknown origin) using chromogenic substrate incubated for 7 min in presence of antithrombin by absorbance based assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
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