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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
Kallikrein Serine protease panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of human KLK1 using H-DVal-Leu-Arg-AFC as substrate
Assay data:3 Active, 1 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of KLK1 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of human KLK1
SummaryPubMed CitationRelated BioAssays by Target
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
Kallikrein Inhibition Assay Utilizing a Quenched AMC Peptide Substrate from US Patent US20230295157: "3-(1H-IMIDAZOL-2-YL)-2,3,8,8A-TETRAHYDROINDOLIZIN-5(1H)-ONE DERIVATIVES USEFUL AS FACTOR XIA INHIBITORS"
Assay data:350 Active, 22 Activity ≤ 1 nM, 347 Activity ≤ 1 µM, 357 Tested
Determination of the IC50 for KLK1 from US Patent US11613527: "Enzyme inhibitors"
Assay data:109 Tested
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Biological Assay from US Patent US11584735: "Solid forms of a plasma kallikrein inhibitor and salts thereof"
Assay data:2 Tested
Inhibitory Effect on the Enzymatic Activity of KLK from US Patent US11541023: "Compounds and compositions for the treatment of neurodegenerative and inflammatory diseases"
Assay data:2 Active, 4 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (Serine protease panel) EUB0000735a KLK1
Inhibition of recombinant human kallikrein (25 to 262 residues) assessed as remaining enzyme activity using Z-VVR-AMC as substrate at 10 uM preincubated for 5 to 15 mins followed by substrate addition and measured at 5 mins interval for 2 hrs by fluorescence based envision plate reader method relative to control
Inhibition of human KLK1 preincubated for 5 mins followed by substrate addition by fluorometer analysis
Binding affinity to human tissue kallikrein-1 assessed as inhibition constant using H-D-Valyl-L-leucyl-L-arginine 7-amino-4-trifluoromethylcoumarin as substrate measured upto 120 mins by spectrofluorometric analysis
Determination of the IC50 for KLK1 from US Patent US11242333: "Inhibitors of plasma kallikrein"
Assay data:51 Active, 2 Activity ≤ 1 µM, 95 Tested
Inhibitory Activity In Vitro from US Patent US11198691: "N-((het)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors"
Assay data:92 Tested
Determination of the IC50 for KLK1 from US Patent US11180484: "Pyrazole derivatives as plasma kallikrein inhibitors"
Assay data:59 Tested
Inhibitory Activity In Vitro Assay from US Patent US11084809: "N-((HET)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors"
Inhibitory Activity Assay from US Patent US11001578: "N-((HET)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors"
Inhibitory Activity Assay from US Patent US10781181: "N-((het) arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors"
Assay data:108 Tested
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