Assay Report Card

Basic Information

ID: ALA3888552

Type: Binding

Description: Fluorescence Resonance Energy Transfer (FRET) Assay : The recombinant human BACE1, Cathepsin D, and Cathepsin E enzymes were purchased from R&D Systems (catalog numbers are 931-AS, 1014AS and 1294AS, respectively). The enzymatic inhibition activity assays were determined using the fluorescence resonance energy transfer (FRET) assay. The assays were performed in a 384-well plate format. The recombinant human BACE-1 enzyme (R&D Systems, catalog#931-AS) was diluted to 20 ng/μL in assay buffer (100 mM sodium acetate pH 4.0), 10 point 1:3 serial dilutions of compound in DMSO were preincubated with the enzyme for 15 min at room temperature. The concentration of Cathepsin D was 20 ng/μL, and 1 ng/μL of Cathepsin E was used. CatD and CatE were activated by incubation in assay buffer (0.1 M NaOAc, 0.2 M NaCl, pH 3.5) at room temperature for 30 min. Subsequently, the rhBACE-1 substrate (R&D Systems, catalog# ES004), the Cathepsin D and Cathepsin E substrate (R&D Systems, Catalog # ES001) were added accordingly to final concentration

Organism: Homo sapiens

Activity Charts

Bioactivity

Activity Types for Assay ALA3888552

IC50

Total(53)

Compound Summary

Parent Molecular Weight	ALogP	Polar Surface Area
333.44	3.63	3.63
383.50	4.49	4.49
371.44	3.60	3.60
342.40	2.99	2.99
335.41	2.96	2.96
440.55	4.70	4.70
410.52	4.69	4.69
351.41	2.48	2.48
393.49	3.65	3.65
395.46	2.49	2.49
494.59	3.71	3.71
407.51	3.89	3.89
409.49	2.74	2.74
393.49	3.65	3.65
369.43	1.22	1.22
436.51	2.32	2.32
493.61	2.26	2.26
366.42	1.88	1.88
367.41	1.27	1.27
508.62	3.96	3.96
405.50	3.51	3.51
366.42	1.88	1.88
369.51	4.17	4.17
329.40	1.85	1.85
357.45	2.63	2.63
439.56	5.31	5.31
416.48	3.22	3.22
403.53	4.67	4.67
459.59	4.53	4.53
422.53	2.66	2.66
441.53	4.15	4.15
399.50	3.92	3.92
430.51	3.38	3.38
401.47	2.77	2.77
498.58	3.62	3.62
426.48	3.39	3.39
371.48	3.02	3.02
418.54	4.07	4.07
366.42	1.88	1.88
374.49	4.05	4.05
376.46	2.90	2.90
410.91	3.55	3.55