Basic Information
ID: ALA3708026
Type: Binding
Description: Immunofluorescence Resonance Energy Transfer (FRET) Assay: The FRET assay was performed essentially as described in Gruninger-Leitch et al., Journal of Biological Chemistry (2002) 277(7) 4687-93 (Substrate and inhibitor profile of BACE (beta-secretase) and comparison with other mammalian aspartic proteases). In summary, a peptide is designed that is cleaved by the protease. The peptide is labelled with dabcyl at the N terminus and Lucifer Yellow at the C-terminus, such that for an intact peptide the Lucifer Yellow fluorescence is quenched by the dabcyl. When the peptide is cut by BACE2, the quenching is removed and a fluorescent signal is generated. The assay was performed as described in Grueninger et al. 2002 at pH 4.5 using a substrate concentration of 5 μM. A FRET peptide based on the TMEM27 sequence was devised. dabcyl-QTLEFLKIPS-LucY (SEQ ID NO: 1). BACE2 had a high activity against this sequence, which is unrelated to the known APP-based substrates. Conversely, BACE1 had insignificant activity against this peptide.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3708026
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 406.86 | 3.91 | 3.91 |
| 419.81 | 3.62 | 3.62 |
| 325.36 | 1.97 | 1.97 |
| 339.39 | 2.36 | 2.36 |
| 339.39 | 2.36 | 2.36 |
| 437.80 | 3.92 | 3.92 |
| 451.83 | 4.31 | 4.31 |
| 424.85 | 4.21 | 4.21 |
| 424.85 | 4.21 | 4.21 |
| 374.37 | 3.68 | 3.68 |
| 443.47 | 4.21 | 4.21 |
| 443.47 | 4.21 | 4.21 |
| 452.91 | 4.99 | 4.99 |
| 454.88 | 4.44 | 4.44 |
| 457.50 | 4.60 | 4.60 |
| 453.89 | 5.04 | 5.04 |
| 381.40 | 3.32 | 3.32 |
| 395.40 | 4.72 | 4.72 |
| 461.46 | 4.35 | 4.35 |
| 412.84 | 4.63 | 4.63 |
| 396.39 | 4.12 | 4.12 |
| 378.40 | 3.98 | 3.98 |
| 408.42 | 3.99 | 3.99 |
| 446.40 | 5.00 | 5.00 |
| 476.42 | 4.92 | 4.92 |