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Inhibition of recombinant His-tagged full length human PDI reductase activity assessed as inhibition of PDI/DTT-mediated cleavage of disulfide bond in insulin in the presence of DTT incubated for 40 mins by spectrophotometric analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant His-tagged full length human PDI reductase activity assessed as inhibition of PDI/DTT-mediated cleavage of disulfide bond in insulin at 100 uM incubated for 40 mins by spectrophotometric analysis
Assay data:3 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to recombinant His-tagged full length human PDI-b' x domain substrate binding pocket expressed in Escherichia coli BL21 (DE3) cells assessed as inhibition constant at 100 uM incubated for 10 mins by tryptophan fluorescence based assay
Assay data:1 Active, 4 Tested
Binding affinity to recombinant His-tagged full length human PDI-b' x domain substrate binding pocket expressed in Escherichia coli BL21 (DE3) cells assessed as decrease in fluorescence intensity at 100 uM incubated for 10 mins by tryptophan fluorescence based assay
Assay data:6 Active, 6 Tested
PDI Inhibition Assay from Article 10.1021/cb4002602: "Small molecule probe suitable for in situ profiling and inhibition of protein disulfide isomerase."
Assay data:22 Active, 1 Activity ≤ 1 µM, 24 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Reductase Activity Assay from Article 10.1021/cb100387r: "Discovery of a small molecule PDI inhibitor that inhibits reduction of HIV-1 envelope glycoprotein gp120."
Assay data:11 Active, 7 Activity ≤ 1 µM, 16 Tested
Insulin reductase assay from US Patent US10064853: "Compounds for use in methods for treating diseases or conditions mediated by protein disulfide isomerase"
Assay data:6 Active, 3 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding affinity to recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 20 uM measured after 24 hrs in presence of BSA by SDS PAGE analysis
Assay data:2 Active, 2 Tested
Inhibition of N-(4-(5,5-Difluoro-1,3,7,9-tetramethyl-5H-4(Gamma4),5(Gamma4)-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-10-yl))-N-(2-(4-((6-hydroxybenzo[d]-[1,3]dioxol-5-yl)(piperidin-1-yl)methyl)benzamido)ethyl)-benzamide binding to PDIA1 in human U-87 MG cell lysates measured after 24 hrs by PAGE analysis
Binding affinity to PDIA1 in human U-87 MG cell lysates at 5 uM measured after 24 hrs by PAGE analysis
Assay data:1 Active, 1 Tested
Binding affinity to PDIA1 in human U-87 MG cells at 5 uM measured after 24 hrs in presence of DTT by coomassie staining GFP channel based Western blot assay
Binding affinity to PDIA1 in human U-87 MG cells at 10 uM measured after 24 hrs in absence of fetal bovine serum by coomassie staining GFP channel based assay
Binding affinity to PDIA1 in human U-87 MG cells at 40 uM measured after 24 hrs in presence of fetal bovine serum by Western blot analysis
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 10 to 40 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate addition
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 1.1 to 90 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate addition in presence of glutathione
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 10 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate addition in absence of glutathione
Assay data:2 Tested
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 10 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate and N-acetyl cysteine addition
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 10 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate addition in presence of glutathione
Assay data:6 Tested
Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 10 uM using bovine insulin as substrate preincubated for 1 hr followed by substrate addition in presence of N-acetyl cysteine
Assay data:4 Tested
Displacement of ANS from recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) at 100 uM measured after 1 hr by fluorescence assay
Assay data:1 Active, 3 Tested
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