Assay Report Card

Basic Information

ID: ALA3706090

Type: Binding

Description: Inhibition Assay: Zero point five μL of the test compounds (dissolved in N,N′-dimethylsulfoxide) were incubated with 48.5 μL of the fluorescence-quenched peptide substrate solution (Biotin-XSEVNLDAEFRHDSGC-Eu: X=εe-amino-n-capronic acid,Eu=Europium cryptate) and 1 μL of recombinant human BACE-1 protein (R&D systems) for 3 h at 30° C. in the 96 well half-area plate (black color plate,Costar). The substrate peptide was synthesized by reacting with Biotin-XSEVNLDAEFRHDSGC (Peptide Institute) and Cryptate TBPCOOH mono SMP (CIS bio international). The final concentration of the substrate peptide and recombinant human BACE-1 protein were 18 nM and 7.4 nM, respectively. The enzymatic reaction was performed in sodium acetate buffer (50 mM sodium acetate (pH 5.0), 0.008% Triton X-100). After the reaction, a 50 μL of 8.0 μg/mL Streptavidin-XL665 (CIS bio international) dissolved in phosphate buffer (150 mM K2HPO4KH2PO4 (pH 7.0), 0.008% Triton X-100, 0.8 M KF) was added.

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
505.767.797.79
304.363.203.20
398.474.014.01
348.203.123.12
358.433.833.83
239.323.613.61
342.905.185.18
439.774.424.42
389.914.024.02
371.463.083.08
422.354.584.58
410.364.434.43
386.914.054.05
461.414.984.98
343.884.574.57
385.493.383.38
345.904.624.62
394.293.963.96
394.484.294.29
462.425.045.04
400.454.374.37
387.483.823.82
340.494.374.37
395.283.363.36
405.323.763.76
373.453.513.51
374.945.025.02
483.235.135.13
360.873.653.65
460.425.585.58
428.874.674.67
360.873.653.65
394.334.914.91
350.453.483.48
448.394.514.51
403.944.414.41
387.483.893.89
437.494.774.77
453.494.654.65
359.453.353.35
359.523.913.91
438.785.025.02
416.964.874.87
349.843.853.85
395.324.314.31
415.975.475.47
405.323.763.76
346.843.483.48
422.354.584.58
378.863.793.79
395.324.314.31
369.452.102.10
395.324.314.31
341.442.702.70
418.954.444.44
390.903.663.66
322.413.443.44
411.553.013.01
304.423.143.14
385.924.874.87