Basic Information
ID: ALA3706219
Type: Binding
Description: IMAP FP Assay: PDE4 specifically hydrolyzes cAMP and releases the product AMP. The potency of PDE inhibition by said agents is determined in an in vitro enzymatic assay. The assay is commercially available (IMAP FP assay Molecular Devices Corp. (MDS)) and is optimized for the use of human PDE4. Fluorescently labeled cAMP is hydrolyzed by PDE4 and in a second step, binding of labeled product to a large binding partner allowed product detection by fluorescence polarization (FP) measurements.PDE4 is partially purified from undifferentiated human monocytic cells (U-937) according to Thorpy et al. 1992 (J. Pharmacol. Exp. Ther. 263: 1195). Final preparations are specific for cAMP and did not hydrolyze cGMP above the detection limit of the assay. In addition, PDE4 preparations are validated by inhibition studies with PDE4-specific and unspecific PDE inhibitors.Stock solutions of test compounds are made in DMSO and diluted in assay buffer (10 mM Tris-HCl, 10 mM MgCl2, 0.1% BSA 0.05% NaN3, pH 7.2).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3706219
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 1149.26 | ||
| 1225.27 | ||
| 1166.20 | ||
| 1067.07 | ||
| 1307.46 |