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Found 7 Enz. Inhib. hit(s) with Target = 'Beta-secretase 1' and Ligand = 'BDBM143218'
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataKi:  0.949nMpH: 5.01Assay Description:The protocol that was used to determine the recited values isdescribed as follows.BACE1 HTRF FRET AssayReagentsNa+-Acetate pH 5.01% Brij-35GlycerolDi...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataKi:  0.949nM ΔG°:  -52.4kJ/molepH: 5.0 T: 2°CAssay Description:A homogeneous time-resolved FRET assay was used to determine IC50 values for inhibitors of the soluble human BACE1 catalytic domain. This assay monit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataKi:  949nMpH: 5.0Assay Description:This assay monitored the increase of 620 nm fluorescence that resulted from BACE1 cleavage of an APPswedish APPswe mutant peptide FRET substrate (QSY...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataIC50: <0.540nMAssay Description:Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of human BACE1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataIC50: <2.20nMAssay Description:Inhibition of human BACE1 using biotin-GLTNIKTEEISEISYEVEFR-C[Oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM143218(US8940748, 34 | US9029362, 34 | US9687494, 34)
Affinity DataIC50:  6.40nMAssay Description:Displacement of [3H]-PF-6475886 from recombinant human full length FL-tagged BACE1 expressed in HEK293 cell membranes after 30 mins by parallel scint...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed