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Proteinase 3 Serine protease panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Binding affinity to human neutrophil proteinase 3 assessed as inhibition constant using Methoxysuccinyl-L-alanyl-L-alanyl-L-prolylL-valine p-Nitroaniline as substrate measured upto 120 mins by spectrophotometric analysis
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human proteinase 3 assessed as ratio of Kinact to Ki using flurogenic substrate as elastase substrate V by fluorescence assay
Assay data:3 Tested
Inhibition of human proteinase 3 at 100 uM preincubated for 30 mins followed by FP-rhodamine addition measured after 30 mins by fluorescence assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human proteinase 3 assessed as inactivation constant using flurogenic substrate as elastase substrate V by fluorescence assay
Inhibition of human proteinase 3 using flurogenic substrate as elastase substrate V by fluorescence assay
Inhibition of proteinase 3 (unknown origin) at 10 uM relative to control
Stability of the compound in cystic fibrosis patient lung sputum assessed as proteinase 3-mediated compound hydrolysis at 40 uM incubated for 24 mins under dark by SDS-PAGE analysis
Assay data:2 Tested
Inhibition of PR3 (unknown origin) expressed in Pichia pastoris using Ac-Glu(O-Bzl)-Lys(Ac)-Hyp(Bzl)-Nva-ACC substrate by spectrofluorometry relative to control
Competitive inhibition of purified human proteinase 3 at 160 nM using MeOSuc-AAPV-MCA as substrate by fluorescence based assay
Assay data:4 Active, 4 Tested
Competitive inhibition of purified human proteinase 3 at 40 nM using MeOSuc-AAPV-MCA as substrate by fluorescence based assay
Assay data:2 Active, 2 Tested
Inhibition of purified human proteinase 3 using MeOSuc-AAPV-MCA as substrate by fluorescence based assay
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human neutrophil proteinase 3 using M4765 as substrate preincubated for 5 mins followed by substrate addition
Inhibition of human PR3 using Suc(OMe)-AAPV-MCA as substrate after 30 mins
Inhibition of human PR3 at 10000 nM using Suc(OMe)-AAPV-MCA as substrate after 30 mins relative to control
Binding affinity to PR3 in cystic fibrosis patient sputum supernatant at 50 nM after 20 mins by extravidin peroxidase based Western blot analysis
Potency index, ratio of (3S)-3-((S)-2-((S)-1-acetylpyrrolidine-2-carboxamido)-3-(4-hydroxyphenyl)propanamido)-4-(1-(bis(4-chlorophenoxy)phosphoryl)ethylamino)-4-oxobutanoic acid inactivation rate constant to compound inactivation rate constant for human PR3
Binding affinity to PR3 in cystic fibrosis patient sputum after 2 hrs by HPLC analysis
Inhibition of human PR3 assessed as first order rate constant using ABZ-VADnVADYQ-EDDnp as substrate by FRET assay
Inhibition of human PR3 assessed as inactivation rate constant at 0.01 uM using ABZ-VADnVADYQ-EDDnp as substrate by FRET assay
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