TABLE 3

PDE4 inhibitors tested for their selectivity against different PDE4 isoforms or construct lengths of the same PDE4 subtype

CompoundStudyConstructConstruct CategoryTruncation/ModificationIC50
nM
CDP840Perry et al., 1998PDE4B2Short1.9
PDE4B3Long3.8
PDE4D2Supershort2.9
PDE4D3Long2.6
ChlorbipramZhang et al., 2013PDE4B2Short99,300
PDE4B5Supershort8320
CilomilastWunder et al., 2013PDE4D3cat dom20.5
PDE4D3Long10.1
DenbufyllineOwens et al., 1997aPDE4A4Long295
PDE4A4cat domUCR1-UCR2 deleted550
D159153Wunder et al., 2013PDE4D3cat dom20,500
PDE4D3Long68.3
D159404Wunder et al., 2013PDE4D3cat dom20,000
PDE4D3Long380
EtazolateWunder et al., 2013PDE4D3cat dom143
PDE4D3Long240
GEBR-32aRicciarelli et al., 2017PDE4D1Short4970
PDE4D2Supershort2890
PDE4D3Long2420
PDE4D5Long3180
PDE4D7Long1140
Prosdocimi et al., 2018PDE4Dcat domcat dom, no C-term2300
PDE4D3LongPKA-mimetic, ERK-ablative1000
(S)-(+)-GEBR-32aCavalloro et al., 2020PDE4Dcat domcat dom, no C-term19,500
PDE4D3LongPKA-mimetic, ERK-ablative2100
(R)-(-)-GEBR-32aCavalloro et al., 2020PDE4Dcat domcat dom, no C-term31,800
PDE4D3LongPKA-mimetic, ERK-ablative15,500
GEBR-7bProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term1600
PDE4D3LongPKA-mimetic, ERK-ablative1100
GEBR-20bProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term800
PDE4D3LongPKA-mimetic, ERK-ablative600
GEBR-4aProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term7000
PDE4D3LongPKA-mimetic, ERK-ablative2100
GEBR-11bProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term900
PDE4D3LongPKA-mimetic, ERK-ablative400
GEBR-26gProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term17,000
PDE4D3LongPKA-mimetic, ERK-ablative3500
GEBR-54Prosdocimi et al., 2018PDE4Dcat domcat dom, no C-term20,000
PDE4D3LongPKA-mimetic, ERK-ablative4600
GEBR-18bProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term16,000
PDE4D3LongPKA-mimetic, ERK-ablative4800
GEBR-18aProsdocimi et al., 2018PDE4Dcat domcat dom, no C-term23,000
PDE4D3LongPKA-mimetic, ERK-ablative5000
LirimilastWunder et al., 2013PDE4D3cat dom3725
PDE4D3Long54.3
OglemilastWunder et al., 2013PDE4D3cat dom0.5
PDE4D3Long1.1
PiclamilastWunder et al., 2013PDE4D3cat dom0.064
PDE4D3Long0.12
PMNPQWunder et al., 2013PDE4D3cat dom115
PDE4D3Long0.43
RoflumilastWunder et al., 2013PDE4D3cat dom0.039
PDE4D3Long0.076
Roflumilast N-oxideWunder et al., 2013PDE4D3cat dom0.079
PDE4D3Long0.26
RolipramBruno et al., 2009PDE4D1Short910
PDE4D2Supershort1170
PDE4D3Long550
Wunder et al., 2013PDE4D3cat dom510
PDE4D3Long72.8
Zhang et al., 2013PDE4D4Long470
PDE4D5Long190
Wang et al., 2003PDE4D6Supershort57
PDE4D7Long42
R-rolipramPerry et al., 1998PDE4B2Short60.5
PDE4B3Long69
PDE4D2Supershort26.9
PDE4D3Long84.3
Ro20-1724Owens et al., 1997aPDE4A4Long1450
PDE4A4cat domUCR1-UCR2 deleted4154
YM976Wunder et al., 2013PDE4D3cat dom0.34
PDE4D3Long0.73
ZardaverineWunder et al., 2013PDE4D3cat dom163
PDE4D3Long65.3
4aBruno et al., 2009PDE4D1Short7090
PDE4D2Supershort9180
PDE4D3Long2860
4eLiang et al., 2020PDE4B2Shortcat dom10
PDE4B1Long8
PDE4D2Supershortcat dom17
PDE4D7Long9
  • cat dom, catalytic domain; C-term, C terminus.