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α-Gal A Assay from Article 10.1021/cb500143h: "Molecular Basis of 1-Deoxygalactonojirimycin Arylthiourea Binding to Human a-Galactosidase A: Pharmacological Chaperoning Efficacy on Fabry Disease Mutants."
Assay data:7 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Non-competitive inhibition of human recombinant lysosomal alpha-GalA using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 mins followed by substrate addition and measured after 30 mins by fluorescence spectrophotometry based Lineweaver-Burk plot analysis
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Competitive inhibition of human recombinant lysosomal alpha-GalA using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 mins followed by substrate addition and measured after 30 mins by fluorescence spectrophotometry based Lineweaver-Burk plot analysis
Assay data:3 Active, 1 Activity ≤ 1 µM, 5 Tested
Inhibition of human recombinant lysosomal alpha-GalA using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 mins followed by substrate addition and measured after 30 mins by fluorescence spectrophotometric assay
Assay data:2 Active, 16 Tested
Inhibition of human recombinant lysosomal alpha-GalA at 1 mM using 4-methylumbelliferyl-alpha-D-glucopyranoside as substrate preincubated for 45 mins followed by substrate addition and measured after 30 mins by fluorescence spectrophotometric assay relative to control
Assay data:14 Tested
SummaryPubMed CitationRelated BioAssays by Target
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of recombinant human alpha-gal A assessed as residual activity at 1 mM using 4 Np-alpha-Gal as substrate by UV-visible spectrophotometric method
Assay data:2 Tested
Chaperone activity assessed as enhancement of alpha GAL-A N215S mutant enzyme activity in Fabry patient derived lymphocytes up to 50 uM pretreated for 4 days followed by compound washout cultured for 4 days and subsequent 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay
Non-competitive inhibition of recombinant human alpha GAL-A using varying levels of 4-methylumbelliferyl alpha-D-galactopyranoside substrate at pH 7 Lineweaver-burk plot analysis
Assay data:1 Active, 1 Tested
Non-competitive inhibition of recombinant human alpha GAL-A using varying levels of 4-methylumbelliferyl alpha-D-galactopyranoside substrate at pH 4.6 Lineweaver-burk plot analysis
Inhibition of recombinant human alpha GAL-A at 100 uM using p-nitrophenyl-glycopyranoside or 4-methylumbelliferyl-glycopyranoside as substrate by spectrophotometric method relative to control
Assay data:1 Tested
Chaperone activity assessed as enhancement of human alpha GAL-A R363C mutant enzyme activity expressed in COS7 cells at 10 to 100 uM at pH 4.6 pretreated for 60 hrs followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Chaperone activity assessed as enhancement of human alpha GAL-A R301Q mutant enzyme activity expressed in COS7 cells at 10 to 100 uM at pH 4.6 pretreated for 60 hrs followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Chaperone activity assessed as enhancement of human alpha GAL-A Q279E mutant enzyme activity expressed in COS7 cells at 10 to 100 uM at pH 4.6 pretreated for 60 hrs followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Chaperone activity assessed as enhancement of human alpha GAL-A P205T mutant enzyme activity expressed in COS7 cells at 10 to 100 uM at pH 4.6 pretreated for 60 hrs followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Chaperone activity assessed as enhancement of human alpha GAL-A S148N mutant enzyme activity expressed in COS7 cells at 10 to 100 uM at pH 4.6 pretreated for 60 hrs followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Potency index, ratio of compound effect to 1,4-dideoxy-1,4-imino-L-allitol effect for chaperone activity assessed as enhancement of alpha GAL-A N215S mutant enzyme activity in Fabry patient derived lymphocytes at 100 uM
Potency index, ratio of compound effect to Deoxygalactonojirimycin effect for chaperone activity assessed as enhancement of alpha GAL-A N215S mutant enzyme activity in Fabry patient derived lymphocytes at 25 uM
Chaperone activity assessed as enhancement of alpha GAL-A N215S mutant enzyme activity in Fabry patient derived lymphocytes at 25 uM at pH 4.6 pretreated for 4 days followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay relative to control
Chaperone activity assessed as enhancement of alpha GAL-A N215S mutant enzyme activity in Fabry patient derived lymphocytes up to 100 uM at pH 4.6 pretreated for 4 days followed by 4MU-alpha-galactopyranoside substrate addition in presence of N-acetylgalactosamine measured after 1 hr by fluorescence assay
Assay data:6 Active, 6 Tested
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