Basic Information
ID: ALA3706288
Type: Binding
Description: Enzymatic Assay: The products are solubilized in DMSO at a concentration of 10 mM. A serial 3-fold dilution over 10 points is carried out so as to have a concentration range of from 10 uM to 0.5 nM final concentration. The TACE enzyme is an internal production (carried out according to the publication protein Eng Des Sel 2006, 19,155-161) and is added so as to have a signal equivalent to 6 times the background noise in 2 h at 37C. The reaction is carried out in 50 mM Tris buffered medium containing 4% glycerol, pH 7.4. The fluorescent substrate is MCA-Pro-Leu-Ala-Val-(Dpa)-Arg-Ser-Ser-Arg-NH2 (R&D systems, reference: ES003). The substrate is cleaved by the enzyme between the alanine and the valine, thus releasing a fluorescent peptide (excitation: 320 nm, emission: 420 nm). The substrate is used at 40 uM. The reaction is carried out in a final volume of 10 ul (4 ul inhibitor, 4 ul substrate, 2 ul enzyme) in a low volume 384-well plate (Corning reference: 3676).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3706288
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 433.53 | 1.90 | 1.90 |
| 419.50 | 1.51 | 1.51 |
| 451.52 | 2.04 | 2.04 |
| 483.59 | 3.06 | 3.06 |
| 502.42 | 3.21 | 3.21 |
| 435.50 | 0.75 | 0.75 |
| 498.61 | 2.76 | 2.76 |
| 502.42 | 3.21 | 3.21 |
| 500.58 | 1.61 | 1.61 |