PDE Assays

Cell-Based PDE Assays

SB Drug Discovery offers an extensive panel of assays optimized for measuring selective PDE activity within the cell. The assay platforms utilized include direct measurement of cyclic nucleotide levels (cAMP and cGMP) by enzyme immunoassay and CRE-luciferase reporter assays.

Our cell-based PDE assays have been optimized and verified using standard reference inhibitors and give a robust read-out of PDE inhibition. Assays have been optimized in 96-well and 384-well formats and can be used to generate single-point inhibition or IC50 data.

In addition to our human PDE cell based assays, SB also offers several animal variants as well as cell lines over-expressing PDE4 isoforms such as PDE4B, PDE4C and PDE4D, allowing screening of isoform-selective inhibitors.


PDE2 cell-based assay

PDE2 cell based assay

Figure 1: Effect of BAY-60-7550 on PDE2A3 transfected cells. Cells were stimulated with forskolin in the presence of increasing concentrations of compound. cAMP levels were determined using a cAMP assay.

PDE3 cell-based assay

PDE3 cell based assay

Figure 2: Effects of PDE3 inhibitor Cilostamide on PDE3A transfected cells. Cells were treated with increasing concentrations of PDE inhibitor and stimulated by the addition of isoproterenol.

 

PDE4 cell-based assay

PDE4 cell based assay

Figure 3: Effects of PDE4 inhibitor Rolipram on PDE4B2 transfected cells. Cells were stimulated with forskolin in the presence of increasing concentrations of compound. cAMP levels were determined using a cAMP assay. 

 

PDE5 cell-based assay

PDE5 cell based assay

Figure 4: Effect of Sildenafil on human PDE5A transfected cells. Cells were incubated with increasing concentrations of compound. Cells were stimulated by incubation with SNP and cGMP levels determined using cGMP ELISA. 

 

PDE7 cell-based assay

PDE7 cell based assay

Figure 5: Effect of YM-39059 on human PDE7B transfected cells. Cells were treated with increasing concentrations of PDE inhibitor and stimulated by the addition of isoproterenol before utilizing a luminescence assay.

 

PDE8 cell-based assay

PDE8 cell based assay

Figure 6: Effects of PDE8 inhibitor on PDE8A transfected cells. Cells were stimulated with forskolin in the presence of increasing concentrations of compound. cAMP levels were determined using cAMP assay.

 

PDE10 cell-based assay

PDE10 cell based assay

Figure 7: Effect of Papaverine on PDE10A transfected cells. Cells were stimulated with forskolin in the presence of increasing concentrations of compound. cAMP levels were determined using cAMP assay.


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