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Biological Assay from US Patent US11584735: "Solid forms of a plasma kallikrein inhibitor and salts thereof"
Assay data:2 Tested
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of factor XIIa (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human factor 12a preincubated for 5 mins followed by substrate addition by fluorometer analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of coagulation factor XIIa (unknown origin) assessed as chromogenic substrate using TH5253 as substrate at 1 mM incubated for 1 hr by spectrophotometer based microplate reader method
Inhibition of human factor 12a using H-D-Pro-Phe-Arg-p-nitroanilide as chromogenic substrate assessed as liberation of p-nitroaniline at 100 mM measured every 5 mins for 60 min by multimode plate reader analysis
Inhibition of human factor 12a using H-D-Pro-Phe-Arg-p-nitroanilide as chromogenic substrate assessed as liberation of p-nitroaniline at 2 mM measured every 5 mins for 60 min by multimode plate reader analysis
Inhibition of human factor 12a activation in citrated pooled human plasma assessed as inhibition of bradykinin release incubated for 10 mins followed by kaolin addition and measured after 15 mins by ELISA
Inhibition of human factor 12a using H-D-Pro-Phe-Arg-p-nitroanilide as chromogenic substrate assessed as liberation of p-nitroaniline in presence of BSA measured every 5 mins for 60 min by multimode plate reader analysis
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human factor 12a using H-D-Pro-Phe-Arg-p-nitroanilide as chromogenic substrate assessed as liberation of p-nitroaniline measured every 5 mins for 60 min by multimode plate reader analysis
Assay data:57 Active, 50 Activity ≤ 1 µM, 87 Tested
Binding affinity to human coagulation factor 12a assessed as inhibition constant using H-D-Cyclohexylalanyl-glycyl-arginyl p-Nitroaniline as substrate measured upto 120 mins by spectrophotometric analysis
Factor XIIa (FXIIa) Inhibitory Activity from US Patent US11312723: "Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases"
Assay data:110 Active, 84 Activity ≤ 1 µM, 182 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Determination of the % Inhibition for FXIIa from US Patent US11180484: "Pyrazole derivatives as plasma kallikrein inhibitors"
Assay data:54 Tested
Factor XIIa assay from US Patent US11014920: "Factor XIIa inhibitors"
Assay data:35 Active, 35 Activity ≤ 1 µM, 35 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Factor XIIa Assay from US Patent US10875851: "Factor XIIa inhibitors"
Assay data:174 Active, 17 Activity ≤ 1 nM, 174 Activity ≤ 1 µM, 174 Tested
Enzymatic Activity Assay from US Patent US9512065: "Polymorphs of N-[(R)-1-[(S)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride"
SummaryCompounds, ActiveRelated BioAssays by Target
Protease Inhibition Assay from Article 10.1002/cbic.201600612: "Polar Hinges as Functionalized Conformational Constraints in (Bi)cyclic Peptides."
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Enzyme Assay from US Patent US9234000: "Benzylamine derivatives as inhibitors of plasma kallikrein"
Assay data:1 Active, 26 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition Assay from US Patent US8598206: "Trypsin-like serine protease inhibitors, and their preparation and use"
Assay data:14 Active, 8 Activity ≤ 1 µM, 15 Tested
Enzyme Inhibition Assay from Article 10.1016/s1074-5521(03)00071-1: "Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition."
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
IC50 Value Determination from Article 10.1021/jm8002697: "Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors."
Assay data:6 Active, 1 Activity ≤ 1 µM, 27 Tested
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