Basic Information
ID: ALA3889054
Type: Binding
Description: Time-Resolved Endpoint Proteolysis Assay: Inhibitor compounds, prepared at 3× the desired final concentration in 1×BACE assay buffer (20 mM sodium acetate pH 5.0, 10% glycerol, 0.1% Brij-35) supplemented with 7.5% DMSO are pre-incubated with an equal volume of autoBACE-2 enzyme diluted in 1×BACE assay buffer (final enzyme concentration 1 nM) in black 384-well NUNC plates for 30 minutes at 30° C. The assay is initiated by addition of an equal volume of the QSY7-EISEVNLDAEFC-Eu-amide substrate (200 nM final concentration, Km=8 μM for 4 μM for autoBACE-2) prepared in 1×BACE assay buffer supplemented with 7.5% DMSO and incubated for 90 minutes at 30° C. DMSO is present at 5% final concentration in the assay. Following laser excitation of sample wells at 320 nm, the fluorescence signal at 620 nm is collected for 400 ms following a 50 μs delay on a RUBYstar HTRF plate reader (BMG Labtechnologies).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3889054
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 456.50 | 1.57 | 1.57 |
| 392.45 | 1.37 | 1.37 |
| 374.46 | 1.23 | 1.23 |
| 438.51 | 1.43 | 1.43 |
| 475.49 | 3.04 | 3.04 |
| 493.48 | 3.18 | 3.18 |
| 459.93 | 2.82 | 2.82 |
| 450.50 | 1.66 | 1.66 |
| 425.49 | 2.16 | 2.16 |
| 469.34 | 2.44 | 2.44 |
| 398.41 | 1.98 | 1.98 |
| 437.52 | 2.03 | 2.03 |
| 455.51 | 2.17 | 2.17 |
| 454.92 | 2.31 | 2.31 |
| 443.48 | 2.30 | 2.30 |
| 380.42 | 1.84 | 1.84 |
| 441.94 | 2.68 | 2.68 |