Phosphodiesterase enzyme selectivity assays

DP Dipak R. Patel
SU Shweta Urva
SH Stephen Ho
CB Cody J. Buckman
YM Yanfei Ma
JL Jean Lim
SS Sean E. Sissons
MZ Mary S. Zuniga
DP Diane Philips
KC Karen Cox
DD Daniel J. Dairaghi
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All 3′, 5′ cyclic nucleotide phosphodiesterase enzyme activities were measured with a radiometric enzyme assay based on scintillation proximity assay detection system or a filtration binding format. Compounds tested were diluted in pure DMSO using 10‐point concentration response curves. Selectivity against PDE3A (catalytic domain), PDE4 (A, B, C, and D), PDE7B, and PDE8A were measured using [3H]‐cAMP, whereas selectivity against PDE2A, PDE5A, PDE6AB, PDE9A, PDE10A, and PDE11A were measured using [3H]‐cGMP, as described. 5

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