TABLE 4

PDE4 inhibitors tested for their selectivity against different PDE4 conformational states or PDE4 isoforms in different cellular fractions

CompoundStudyConstructConstruct CategoryMutation/Modification/Cellular FractionIC50
nM
A-33Fox et al., 2014PDE4B1LongPKA-mimetic, ERK-ablative32
PDE4B1LongL674Q, PKA-mimetic, ERK-ablative2035
PDE4D7LongPKA-mimetic, ERK-ablative1569
PDE4D7LongQ594L, PKA-mimetic, ERK-ablative21
BPN14770Zhang et al., 2018PDE4D7Long1018
PDE4D7LongPKA-mimetic, ERK-ablative7.8
PDE4D3LongPKA-mimetic, ERK-ablative7.4
PDE4D2SupershortERK-ablative127
PDE4B1LongPKA-mimetic, ERK-ablative2013
CilomilastWallace et al., 2005PDE4A11LongCytosolic34
PDE4A11LongParticulate P234
PDE4A4LongCytosolic61
PDE4A4LongParticulate P259
PDE4A10LongCytosolic130
DenbufyllineWallace et al., 2005PDE4A11LongCytosolic250
PDE4A11LongParticulate P2310
PDE4A4LongCytosolic560
PDE4A4LongParticulate P2460
PDE4A10LongCytosolic590
PMNPQBurgin et al., 2010PDE4D7LongPKA-mimetic5
PDE4D7LongPKA-mimetic, Phe196Ala170
PDE4D7LongPKA-mimetic, Phe201Ala310
PDE4D7LongPKA-mimetic, ERK-ablative0.52
PDE4D2SupershortERK-ablative0.66
PDE4B1LongPKA-mimetic4.4
RoflumilastWallace et al., 2005PDE4A11LongCytosolic4.8
PDE4A11LongParticulate P23.9
PDE4A4LongCytosolic9.0
PDE4A4LongParticulate P22.5
PDE4A10LongCytosolic4.1
RolipramZhang et al., 2018PDE4D7Long675
PDE4D7LongPKA-mimetic, ERK-ablative32
PDE4D3LongPKA-mimetic, ERK-ablative29
PDE4D2SupershortERK-ablative142
PDE4B1LongPKA-mimetic, ERK-ablative175
Huston et al., 1996PDE4A4LongParticulate195
PDE4A4LongCytosolic1600
Wallace et al., 2005PDE4A11LongCytosolic720
PDE4A11LongParticulate P2660
PDE4A4LongCytosolic1310
PDE4A4LongParticulate P2260
PDE4A10LongCytosolic64
Rena et al., 2001PDE4A10LongParticulate P154
PDE4A10LongParticulate P252
PDE4A10LongCytosolic56
Huston et al., 1997PDE4B1LongParticulate P1100
PDE4B1LongParticulate P250
PDE4B1LongCytosolic80
PDE4B3LongParticulate P1140
PDE4B3LongParticulate P2100
PDE4B3LongCytosolic50
PDE4B2ShortParticulate P1180
PDE4B2ShortParticulate P2210
PDE4B2ShortCytosolic20
Bolger et al., 1997PDE4D1ShortParticulate P2n/a
PDE4D1ShortCytosolic50
PDE4D2SupershortParticulate P2n/a
PDE4D2SupershortCytosolic50
PDE4D3LongParticulate P2320
PDE4D3LongCytosolic140
PDE4D4LongParticulate P250
PDE4D4LongCytosolic60
PDE4D5LongParticulate P2590
PDE4D5LongCytosolic80
Ro 20-1724Wallace et al., 2005PDE4A11LongCytosolic990
PDE4A11LongParticulate P2910
PDE4A4LongCytosolic2930
PDE4A4LongParticulate P22900
PDE4A10LongCytosolic1240
RS25344Burgin et al., 2010PDE4D7LongPKA-mimetic19
PDE4D7LongPKA-mimetic, Phe196Ala4.1
PDE4D7LongPKA-mimetic, Phe201Ala6.2
PDE4D7LongPKA-mimetic, ERK-ablative0.91
PDE4D2SupershortERK-ablative0.81
PDE4B1LongPKA-mimetic9.4
Alvarez et al., 1996PDE4D3Long3.16
PDE4D3LongPKA-mimetic0.5
RS33793Alvarez et al., 1996PDE4D3Long39.8
PDE4D3LongPKA-mimetic0.2
  • n/a, not applicable.