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. Author manuscript; available in PMC: 2010 May 14.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Jan 23;19(13):3686–3692. doi: 10.1016/j.bmcl.2009.01.057

Table 2.

PDE isoform selectivity data for 1, 5, 10 and 18.

PDE
isof orm*
1
I C50 /% inh.
5
I C50 /% inh.
10
I C50 /% inh.
18
I C50 /% inh.
graphic file with name nihms-191949-t0007.jpg PDE1A inactive inactive 36% 32%
PDE1B inactive inactive 52% 56%
PDE1C inactive 26% 49% 74%
PDE2A inactive 41% 68% 54%
PDE3A inactive 1.7 μM 56% 54%
PDE3B inactive 720 nM 4.6 μM 2.3 μM
PDE4A1A 102 nM 12.9 nM 0.26 nM 0.6 nM
PDE4B1 901 nM 48.2 nM 2.3 nM 4.1 nM
PDE4B2 534 nM 37.2 nM 1.6 nM 2.9 nM
PDE4C1 40% 452 nM 46 nM 106 nM
PDE4D2 403 nM 49.2 nM 1.9 nM 2.1 nM
PDE5A1 inactive 60% 58% 51%
PDE7A inactive 73% 48% 59%
PDE7B inactive 33% 43% 35%
PDE8A1 inactive 57% inactive inactive
PDE9A2 inactive inactive inactive inactive
PDE10A1 inactive 823 nM 632 nM 388 nM
PDE11A4 inactive inactive inactive inactive
*

data generated by BPS Biosciences (CA) [http://www.bpsbioscience.com]and represents either the IC50 value or the % inhibition at 10 μM of compound.