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Inhibitory Activity against Enzyme hFXIa (Human Factor XIa) from US Patent US12018027: "Macrocyclic derivatives acting as XIa factor inhibitor"
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
SummaryRelated BioAssays by Target
Measurement of FXIa Inhibition from US Patent US20240174633: "CRYSTALLINE FORMS OF (4S)-24-CHLORO-4-ETHYL-73-FLUORO-35-METHOXY-32,5-DIOXO-14-(TRIFLUORO-METHYL)-32H-6-AZA-3(4,1)-PYRIDINA-1(1)-[1,2,3]TRIAZOLA-2(1,2),7(1)-DIBENZENAHEPTAPHANE-74-CARBOXAMIDE"
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
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
Trypsin Serine protease panel
Thrombin Serine protease panel
Kallikrein 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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of thrombin (unknown origin)
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant human trypsin assessed as increase in fluorescence using H2-OPT as substrate at 1 uM by SDS-PAGE based gel fluorescence scanning analysis
Assay data:3 Tested
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 human Trypsin using Z-Phe-Arg-AMC as substrate incubated for 30 mins by FRET assay
Binding affinity to human FXIa assessed as induction of higher order oligomers formation at 100 uM by analytical ultracentrifugation study analysis
Binding affinity to covalently inhibited human FXIa-PMSF assessed as induction of higher order oligomers formation at 100 uM by native PAGE analysis
Binding affinity to human FXIa assessed as induction of higher order oligomers formation at 100 uM by native PAGE analysis
Binding affinity to active site dansylated human DEGR-FXIa assessed as change in fluorescence intensity by fluorescence based analysis
Assay data:2 Tested
Binding affinity to active site dansylated human DEGR-FXIa assessed as maximal change in fluorescence intensity by fluorescence based analysis
Allosteric co-operative binding affinity to active site dansylated human DEGR-FXIa assessed as sigmoidal interaction by measuring change in fluorescence intensity by fluorescence based analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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