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Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
Assay data:6 Active, 5 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
Assay data:4 Active, 3 Activity ≤ 1 µM, 7 Tested
Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
Assay data:4 Active, 4 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of SPP expressed in HEK293 cells at 10 uM in presence of Prl-PP peptide after 30 mins
Assay data:4 Tested
SummaryPubMed Citation
Reduction of human wild type PS1-induced amyloid beta-40 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Reduction of human PS1 L166P mutant-induced amyloid beta42 level in CHO cells overexpressing human APP751 at 50 nM after 24 hrs by liquid phase electrochemiluminescence assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of gamma secretase in human HEK293 cells assessed as amyloid beta 40 production
Fraction unbound in Sprague-Dawley rat brain at 30 mg/kg, po after 4 hrs
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Fraction unbound in Sprague-Dawley rat plasma at 30 mg/kg, po after 4 hrs
Drug uptake in Sprague-Dawley rat brain at 30 mg/kg, po after 4 hrs
Drug uptake in Sprague-Dawley rat plasma at 30 mg/kg, po after 4 hrs
Reduction of human PS1 delta exon9 mutant-induced amyloid beta-40 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control
Reduction of human PS1 delta exon9 mutant-induced amyloid beta-42 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control
Inhibition of SPP expressed in HEK293 cells in presence of Prl-PP peptide after 30 mins
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
Reduction in amyloid beta40 level in Sprague-Dawley rat plasma at 30 mg/kg, po after 4 hrs
Binding affinity to presenilin-1 in UV irradiated human HeLa cells assessed as enzyme photolabeling at 10 uM in presence of 2 uM L-685,458 by SDS-PAGE based photocross linking study
Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production
Assay data:7 Active, 7 Activity ≤ 1 µM, 9 Tested
Reduction of human wild type PS1-induced amyloid beta-42 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control
Inhibition of PS1 PSase activity in human HeLa cells assessed as accumulation of full length protein at 1 to 10 uM after 4 days by Western blot analysis
Assay data:2 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Reduction of human PS1 S290C/M292D mutant-induced amyloid beta-42 level in CHO cells overexpressing human APP751 at 30 uM after 24 hrs by liquid phase electrochemiluminescence assay relative to control
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