Page last updated: 2024-09-20

rolipram

Description

(-)-rolipram : The (R)-enantiomer of rolipram. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID448055
CHEMBL ID430893
CHEBI ID40133
SCHEMBL ID576805
MeSH IDM0067312
PubMed CID5092
CHEMBL ID63
CHEBI ID104872
SCHEMBL ID27930
MeSH IDM0067312

Synonyms (238)

Synonym
bdbm50042058
HMS3267P19
BRD-K75516118-001-01-7
NCGC00016899-01
cas-61413-54-5
NCGC00024862-01
tocris-0905
tocris-1350
tocris-1349
NCGC00015898-01
lopac-r-6520
NCGC00024862-02
NCGC00024862-03
r-rolipram
(r)-4-(3-cyclopentyloxy-4-methoxy-phenyl)-pyrrolidin-2-one
(-)-rolipram
1Q9M
(r)-(-)-rolipram
DB04149
1RO6
(4r)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one
(r)-rolipram
2-pyrrolidinone, 4-(3-(cyclopentyloxy)-4-methoxyphenyl)-, (r)-
c16h21no3
NCGC00015898-02
(4r)-4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one
chebi:40133 ,
CHEMBL430893 ,
85416-75-7
dpx51kup08 ,
unii-dpx51kup08
rolipram, (-)-
NCGC00016899-02
NCGC00016899-05
NCGC00016899-04
NCGC00016899-03
NCGC00015898-10
(r)-4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
1XMY
AKOS015891287
rolipram, (r)-
2-pyrrolidinone, 4-(3-(cyclopentyloxy)-4-methoxyphenyl)-, (4r)-
(4r)-4-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinone
SCHEMBL576805
CCG-208064
HY-16900A
CS-3246
3G4K
AC-22384
SR-01000597573-1
sr-01000597573
2-pyrrolidinone, 4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, (4r)-
mfcd03093860
(4r)-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
4r)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one
HB2898
HMS3676I06
Q27094987
R0182
(r)-(-)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one
AS-31755
BCP14111
HMS3412I06
AE-641/11320426
A863588
DTXSID101318033
(r)-rolipram;(-)-rolipram
4-(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone
rolipram [usan:inn]
einecs 262-771-1
2-pyrrolidinone, 4-(3-(cyclopentyloxy)-4-methoxyphenyl)-
brn 1588548
MLS001146912
HMS3267A05
HMS3393N15
BRD-A34255068-001-04-8
rolipramum [latin]
smr000058510
zk-62711
me-3167
adeo
EU-0101072
rolipram, solid, >=98% (hplc)
BPBIO1_000912
BSPBIO_000828
BIO2_000556
BIO2_000076
rolipram ,
4-[4-methoxy-3-(cyclopentyloxy)phenyl]-2-pyrrolidinone
zk 62711
61413-54-5
4-[3-(cyclopentoxy)-4-methoxy-phenyl]pyrrolidin-2-one
PRESTWICK2_000924
PRESTWICK3_000924
IDI1_033826
2-pyrrolidinone, 4-[3-(cyclopentyloxy)-4-methoxyphenyl]- (9ci)
sb 95952
4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
(+/-)-rolipram
UPCMLD-DP110:001
AB00513966
MLS000759531
MLS000758273
UPCMLD-DP110
4-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinone
DB01954
D01783
rolipram (jan/usan/inn)
LOPAC0_001072
UPCMLD-DP110:002
NCGC00089796-07
NCGC00089796-04
NCGC00089796-06
MLS000069691 ,
KBIO2_002644
KBIO3_000152
KBIO2_000076
KBIO2_005212
KBIOGR_000076
KBIO3_000151
KBIOSS_000076
PRESTWICK1_000924
SPBIO_003007
PRESTWICK0_000924
(4r)-4-[3-(cyclopentyloxy)-4 methoxyphenyl)pyrrolidin-2-one
BSPBIO_001356
NCGC00089796-05
NCGC00089796-08
NCGC00089796-02
[3h]-rolipram
4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one
[3h]rolipram
gtpl5313
4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one
chembl63 ,
(r,s)-rolipram
bdbm14361
4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one
NCGC00015898-04
rolipramum
CHEBI:104872 ,
HMS1989D18
R 6520
HMS2051N15
HMS2090J16
NCGC00015898-12
sb-95952
zk 62 711
nsc-760125
zk-62771
HMS1361D18
HMS1791D18
HMS1570J10
HMS2097J10
HMS3263G06
nsc760125
MLS001424084
pharmakon1600-01505683
tox21_110672
dtxcid1024124
dtxsid3044124 ,
CCG-205149
AKOS015959793
HMS2232F06
CCG-100965
NCGC00015898-08
NCGC00015898-03
NCGC00015898-09
NCGC00015898-06
NCGC00015898-07
NCGC00015898-05
NCGC00015898-11
nsc 760125
k676nl63n7 ,
unii-k676nl63n7
LP01072
BRD-A34255068-001-26-1
4-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinon
S1430
rolipram [who-dd]
rolipram [mart.]
rolipram [jan]
4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidone
85416-74-6
rolipram [mi]
rolipram [inn]
rolipram [usan]
gtpl5260
HMS3369J08
(plusmn)-rolipram
CS-1754
HY-16900
MLS006010272
NC00215
SCHEMBL27930
NCGC00015898-15
tox21_110672_1
KS-1400
AB00384360-17
NCGC00261757-01
tox21_501072
4-(3-cyclopentyloxy-4-methoxy-phenyl)-pyrrolidin-2-one
4-[3-cyclopentyloxy-4-methoxyphenyl]-2-pyrrolidinone
4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidinone
4-(3-cyclopentyloxy-4-methoxyphenyl)-pyrrolidin-2-one
4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
AC-32927
HMS3402D18
R0110
OPERA_ID_1749
AB00384360_19
2-pyrrolidinone, 4-[3-(cyclopentyloxy)-4-methoxyphenyl]-
HMS3655J21
HMS3654P06
SR-01000000162-5
SR-01000000162-4
SR-01000000162-12
SR-01000000162-9
SR-01000000162-3
sr-01000000162
SBI-0051042.P002
HMS3714J10
SW196583-4
FT-0738515
BCP21910
Q410285
HB2896
rolipram - cas 61413-54-5
HMS3675F08
BCP23388
(+)-rolipram; (s)-rolipram
HMS3411F08
SB12922
SDCCGSBI-0051042.P003
NCGC00015898-31
(r,s)-rolipram;sb 95952;zk 62711
r-(-)-rolipram
A847969

Research Excerpts

Overview

ExcerptReference
"Rolipram is a selective phosphodiesterase-4 (PDE4) inhibitor. "( Huang, Y; Qi, C; Wang, Q; Zheng, Y, 2023)
"Rolipram is a selective phosphodiesterase 4 (PDE4) inhibitor that exerts a variety of effects, including anti-inflammatory, immunosuppressive, and anti-tumor effects. "( Liang, Y; Liu, Q; Wang, Z; Zhang, L; Zhang, N, 2018)
"Rolipram is a multifaceted antiinflammatory and antithrombotic compound that protects from ischemic neurodegeneration in clinically meaningful settings."( Brede, M; Göb, E; Heydenreich, N; Kleinschnitz, C; Kraft, P; Meuth, SG; Schwarz, T, 2013)
"Rolipram is a selective phosphodiesterase 4 inhibitor, which increases intracellular cyclic AMP in nerve and immune cells."( Abdi, S; Kim, HK; Kwon, JY; Yoo, C, 2015)
"Rolipram is a selective inhibitor of phosphodiesterase-4 (PDE4), and positron emission tomography (PET) using [(11)C]rolipram can monitor the in vivo activity of this enzyme that is part of the cAMP second messenger cascade. "( Abe, K; Fujita, M; Hong, J; Innis, RB; Inoue, O; Itoh, T; Pike, VW, 2010)
"Rolipram is a specific type IV phosphodiesterase inhibitor that suppresses the activity of immune cells and the production of pro-inflammatory cytokines. "( Hatakeyama, N; Horikawa, Y; Jin, M; Komatsu, K; Konishi, N; Matsuhashi, T; Odashima, M; Ohba, R; Otaka, M; Oyake, J; Sato, T; Wada, I; Watanabe, S, 2005)
"Rolipram is a selective PDE4 inhibitor which exists in two enantiomeric forms, R(-) and S(+)."( Bender, D; Brown, J; Cunningham, VJ; Dommett, D; Gee, AD; Gunn, RN; Jakobsen, S; Knibb, ST; Martarello, L; Matthews, JC; Parker, CA, 2005)
"Rolipram is a potent inhibitor HIV-1 replication and therefore deserves further investigation as a potential therapeutic agent in the treatment of HIV-1-infected patients."( Angel, JB; Dinarello, CA; Endres, S; Greten, TF; Saget, BM; Skolnik, PR; Walsh, SP, 1995)
"Rolipram is a selective inhibitor of Type IV phosphodiesterase isozymes (PDE IV) which is often used as a baseline comparator for compounds in this class. "( Geiger, LE; Larson, JL; Pino, MV; Simeone, CR, 1996)
"Rolipram is a type IV phosphodiesterase inhibitor that suppresses inflammation and TNF-alpha production. "( Feldmann, M; Maini, RN; Malfait, AM; Marinova-Mutafchieva, L; Mason, LJ; Mauri, C; Ross, SE; Williams, RO, 1997)
"Rolipram is a clinically effective antidepressant with cyclic AMP-selective phosphodiesterase (cyclic-AMP PDE) inhibiting action. "( Araki, T; Chen, T; Itoyama, Y; Kato, H; Kogure, K, 1998)
"Rolipram is a type IV phosphodiesterase inhibitor endowed with powerful immunomodulatory properties. "( Beltrami, B; Di Marco, R; Di Mauro, M; Magro, G; Meroni, PL; Nicoletti, F; Xiang, M; Zaccone, P, 1999)
"Rolipram is a specific cAMP phosphodiesterase type 4 (PDE4) inhibitor in the brain, which induces an increase in the intracellular levels of cAMP. "( Fernández, AG; Palacios, JM; Silvestre, JS, 1999)
"Rolipram is a selective inhibitor of phosphodiesterases (PDE) IV, especially of the subtype PDE IVB. "( Mix, E; Winblad, B; Zhu, J, 2001)
"Rolipram is a racemic drug that increases brain cAMP availability by inhibiting phosphodiesterase. "( Smith, DF, 1990)
"Rolipram is a clinically effective antidepressant with selective cAMP phosphodiesterase (PDE) inhibiting properties. "( Baumgarten, HG; Brüning, G; Kaulen, P; Sarter, M; Schneider, HH, 1989)
"Rolipram is an antidepressant with a novel mechanism of action: enhanced noradrenaline (first messenger) synthesis and release, and inhibition of cAMP (second messenger) breakdown. "( Meya, U; Murray, GH; Ross, CE; Rowland, M; Toon, S, 1988)
"Rolipram is a potent phosphodiesterase inhibitor, active in classical pharmacological tests used in the screening of antidepressants (AD). "( Dresse, A; Giesbers, I; Scuvée-Moreau, J, 1987)

Effects

ExcerptReference
"Rolipram has a good anti-fibrosis effect after inhibiting the activity of PDE4."( Chen, Y; Fan, J; Guo, Q; Meng, D; Song, G; Wu, L; Xu, G; Xu, L; Xu, P, 2021)
"Rolipram has a pharmacologic profile similar to that of the atypical antipsychotics and has low extrapyramidal symptom liability. "( Chapin, DS; Martin, AN; McCarthy, SA; Siuciak, JA, 2007)
"Rolipram has a phenyl-pyrrolidinone structure, unrelated to the methylxanthines, and acts as a specific inhibitor of the type IV phosphodiesterase."( Endres, S; Semmler, J; Wachtel, H, 1993)
"Rolipram has a good anti-fibrosis effect after inhibiting the activity of PDE4."( Chen, Y; Fan, J; Guo, Q; Meng, D; Song, G; Wu, L; Xu, G; Xu, L; Xu, P, 2021)
"Rolipram has been shown to play a neuroprotective role in some central nervous system (CNS) diseases."( Dong, XL; Wang, YH; Xu, J; Zhang, N, 2021)
"Rolipram has been shown to relief inflammation and BBB damage in a variety of neurological disorders."( Brede, M; Göb, E; Heydenreich, N; Kleinschnitz, C; Kraft, P; Meuth, SG; Schwarz, T, 2013)
"Rolipram has antipsychotic properties."( Manahan-Vaughan, D; Wiescholleck, V, 2012)
"Rolipram has a pharmacologic profile similar to that of the atypical antipsychotics and has low extrapyramidal symptom liability. "( Chapin, DS; Martin, AN; McCarthy, SA; Siuciak, JA, 2007)
"Rolipram has high (PDE4(H)) and low (PDE4(L)) affinities for phosphodiesterase (PDE)-4, respectively. "( Chan, AL; Chen, CM; Chien, HC; Huang, HL; Ko, WC; Lin, CN, 2008)
"Rolipram has extensively been studied in humans for the treatment of depression, but has not yet been marketed."( Fontana, A; Lichtenfels, R; Löschmann, PA; Meyermann, R; Northoff, GH; Riethmüller, A; Sommer, N; Steinbach, JP; Steinbrecher, A; Weller, M, 1995)
"Rolipram has a phenyl-pyrrolidinone structure, unrelated to the methylxanthines, and acts as a specific inhibitor of the type IV phosphodiesterase."( Endres, S; Semmler, J; Wachtel, H, 1993)

Actions

ExcerptReference
"Rolipram caused an increase in the frequency of Ca(2+) sparks and the spontaneous transient BK currents (TBKCs), hyperpolarized the cell membrane potential (MP), and decreased the intracellular Ca(2+) levels."( Cheng, Q; Li, N; Petkov, GV; Xin, W, 2014)
"Rolipram could suppress the inflammatory signals and could be a potential therapeutic strategy against LPS-induced inflammation to protect the salivary gland cells."( Hong, JH; Lee, DU; Shin, DM, 2016)
"Rolipram induces an increase in pERK expression in these interneurons."( Anzilotti, S; Bernardi, G; Colucci D'Amato, L; Dato, C; Fusco, FR; Giampà, C; Laurenti, D; Leuti, A; Melone, MA; Perrone, L, 2012)
"Rolipram promotes the maturation of OPCs, facilitates remyelination, and increases ERK phosphorylation. "( Liu, B; Liu, Y; Sun, X; Xiao, Z; Zhang, L, 2012)
"Rolipram reduced the increase of F-actin content of polymorphonuclear leukocytes and the increase of transit time of 100 micro L of blood sample through a microchannel. "( Hiramatsu, Y; Homma, S; Onizuka, M; Sakakibara, Y; Sato, S; Sato, Y, 2003)
"Rolipram reduced the increase in CD11b expression and the decrease in L-selectin expression of monocytes in response to simulated extracorporeal circulation."( Endo, S; Hiramatsu, Y; Homma, S; Sato, M; Sato, S; Sato, Y; Sohara, Y, 2005)
"Rolipram did not inhibit 5-lipoxygenase activity but did inhibit human monocyte production of leukotriene B4 (LTB4, IC50 3.5 microM)."( Breton, J; Griswold, DE; Marshall, PJ; Torphy, TJ; Webb, EF; White, JR, 1993)
"Rolipram failed to increase perfusate cAMP alone but dramatically increased perfusate cAMP above ISO alone."( Barnard, JW; Prasad, VR; Seibert, AF; Smart, DA; Strada, SJ; Taylor, AE; Thompson, WJ, 1994)
"Rolipram appears to inhibit the expansion and effector function of uveitogenic T cells, raising the possibility that it may be useful for treatment of established disease. "( Caspi, RR; Chan, CC; Rizzo, LV; Silver, PB; Strassmann, G; Wiggert, B; Xu, H, 1999)
"Rolipram may increase intra-cellular levels of cAMP by selectively inhibiting Type IV phosphodiesterases, enzymes that catalyze cAMP breakdown."( Ciraulo, DA; Foye, M; Knapp, CM; Kornetsky, C; Lee, K, 2001)
"Rolipram reduced the increase of F-actin and CD11b but did not change the decrease of L-selectin."( Ishikawa, S; Onizuka, M; Sakakibara, Y; Sato, S; Sato, Y; Yamamoto, T, 2002)

Treatment

ExcerptReference
"Rolipram pretreatments in vivo prevented cocaine-induced reductions in GABAergic inhibition but did not further increase cocaine-induced potentiation of excitation, leading to the restoration of a balance between excitation and inhibition and normalization of the E/I ratio."( Li, Y; Liu, QS; Liu, X; Vickstrom, C; Zhong, P, 2017)
"Rolipram treatment remarkably promoted the expression of Sirtuin 1 (SIRT1) while inhibited NF-κB activation."( Chen, G; Chen, T; Fan, L; He, P; Jin, J; Li, J; Peng, Y; Ruan, W; Xu, H, 2018)
"Rolipram-treated MSCs (Roli-MSCs) had significantly increased expression of the neuroprogenitor proteins Nestin, Musashi, GFAP, and Sox-2."( Cho, GW; Joe, IS, 2016)
"Rolipram treatment significantly attenuated STZ induced and age related memory deficits, biochemical and histopathological alterations."( Kumar, A; Singh, N, 2017)
"Rolipram treatment significantly increased the number of motoneurons that regenerated axons across the repair site at 1 and 2 weeks, and increased the number of sensory neurons that regenerated axons across the repair site at 2 weeks."( Brushart, T; Furey, M; Gordon, T; Ladak, A; Tyreman, N; Udina, E, 2010)
"Rolipram-treated A172 or U87MG cell survival was lower in the presence of forskolin, adenylate cyclase activator, than that in its absence."( Kim, HM; Lee, GH; Lee, JW; Lee, MS; Moon, EY, 2012)
"Rolipram/forskolin treatment also induced Bad to accumulate in CLL heavy-membrane fractions, consistent with Bad translocation to mitochondria."( Lerner, A; Moon, EY, 2003)
"Rolipram treatment did not affect KC expression and the recruitment of neutrophils in the lung tissue."( Barsante, MM; Nicoli, JR; Pinho, V; Soares, AC; Souza, DG; Teixeira, M; Vieira, AT, 2003)
"Rolipram pretreatment shifted the thapsigargin-induced fluid leak site from extra-alveolar to alveolar vessels in the intact pulmonary circulation."( Alvarez, D; Chen, H; Cioffi, DL; Cioffi, EA; Creighton, JR; Goodman, SR; King, J; Sayner, SL; Stevens, T; Townsley, M; Wu, S, 2005)
"Rolipram and tofisopam treatments induced higher BV/TV than placebo (+23.8% and +18.3% respectively)."( Beaupied, H; Benhamou, CL; Bernard, P; Bizot, JC; Bonnet, N; Courteix, D; Trovero, F, 2007)
"Rolipram treatment increases levels of transcripts derived from the 1A3 promoter to a greater extent than the 1B promoter."( Chaves, J; Lerner, A; Makkinje, A; Meyers, JA; Taverna, J, 2007)
"Rolipram treatment restored cAMP to sham levels and significantly reduced cortical contusion volume and improved neuronal cell survival in the parietal cortex and CA3 region of the hippocampus."( Alonso, OF; Atkins, CM; Bramlett, HM; Dietrich, WD; Oliva, AA; Pearse, DD, 2007)
"Rolipram-treated and control animals equally developed circulating antibodies to myelin basic protein."( Davis, RL; Faulds, D; Genain, CP; Hauser, SL; Hedgpeth, J; Li, Y; Nguyen, MH; Roberts, T; Uccelli, A, 1995)
"Rolipram pretreatment was protective against LPS-induced mortality and also resulted in reduced plasma TNF alpha concentrations."( Esser, KM; Turner, CR; Wheeldon, EB, 1993)
"Rolipram treatment of animals with manifest arthritis inhibited further arthritis development and also tended to diminish its severity at a phase of disease where non-treated control animals showed a rapidly progressing disease development."( Klareskog, L; Larsson, E; Lorentzen, J; Müssener, A; Nyman, U, 1997)
"Rolipram treatment significantly elevated intracellular cyclic AMP (adenosine 3',5'-cyclic monophosphate) in clonal T cells (P < .01 for Th1 or Th2 clones); these elevations were consistently greater in the Th2 clones (P < .05)."( Essayan, DM; Huang, SK; Kagey-Sobotka, A; Lichtenstein, LM, 1997)
"Rolipram treatment from days -1 to 7 after immunization (afferent phase) was not protective, but severity of EAU was reduced to 50% by treatment from days 8 to 16 after immunization or when EAU was induced by adoptive transfer (efferent phase). "( Caspi, RR; Chan, CC; Rizzo, LV; Silver, PB; Strassmann, G; Wiggert, B; Xu, H, 1999)
"In rolipram-treated animals, the epithelium was completely disturbed until Day 14. "( Funk, RH; Kasper, M; Ploetze, K; Roth-Eichhorn, S; Schade, I; Schueler, S; Wunderlich, J, 2001)
"Rolipram pretreatment, markedly inhibited these parameters by 100, 95 and 95% respectively."( Alvarez, A; Cerdá, M; Cortijo, J; Issekutz, AC; Lobb, RR; Morcillo, EJ; Piqueras, L; Sanz, MJ, 2002)
"Pretreatment with rolipram (0.1 or 0.2 mg/kg) significantly increased entries and time spent in the open arms of the elevated plus maze test in rats with repeated ethanol abstinence. "( Fei, N; Gong, MF; Liang, JH; Pan, JC; Wen, RT; Xu, JP; Xu, Y; Zhang, HT; Zhou, YM, 2017)
"Treatment with rolipram increased the AMPK phosphorylation and SIRT6 levels in the liver and kidney while reducing NF-κB acetylation."( Liang, Y; Liu, Q; Wang, Z; Zhang, L; Zhang, N, 2018)
"Pre-treatment with rolipram enhanced Akt phosphorylation and associated cytoprotection in CSE-treated cells, which could be reversed by the PI3K inhibitor LY294002 partly."( Jeong, SH; Kyung, SY; Lee, SP; Park, JW; Ryter, SW, 2013)
"Treatment with rolipram increased expression of CREB and pCREB, reduced the inflammatory reaction (decreased TNF-α levels and increased IL-10 levels), and prevented cognitive impairment in these diabetic animals."( He, T; Li, W; Miao, Y; Wang, B; Zhong, Y; Zhu, Y, 2015)
"Treatment with rolipram blocked LPS-induced Ca(2+) increase and ROS production."( Hong, JH; Lee, DU; Shin, DM, 2016)
"Pretreatment with rolipram significantly reduced the increase in bladder wet weight and MPO activity, and ameliorated histological inflammatory changes caused by CYP."( Kawakami, S; Kihara, K; Masuda, H; Matsuoka, Y; Sakura, M; Yokoyama, M, 2009)
"Pre-treatment with rolipram, motapizone or PGE2 only reached about 20% of inhibition but was not affected by oxidative stress."( Almudéver, P; Cortijo, J; Lluch, J; Milara, J; Morcillo, EJ; Navarro, A, 2011)
"Co-treatment with rolipram and forskolin also enhanced CREB phosphorylation on serine 133 that was inhibited by H-89, PKA inhibitor and cAMP-responsive guanine nucleotide exchange factor 1(Epac1), a Rap GDP exchange factor-mediated Rap1 activity in A172 cells."( Kim, HM; Lee, GH; Lee, JW; Lee, MS; Moon, EY, 2012)
"Pretreatment with rolipram decreased the duration of ventricular tachycardia without any change in the incidences of dysrhythmias or the mortality rate. "( Aleixandre, F; Carceles, MD; Fuente, T; Laorden, ML; López-Vidal, J, 2003)
"Treatment with rolipram (3-30 mg kg-1) was associated with earlier lethality and significant inhibition of the TNF-alpha production."( Barsante, MM; Nicoli, JR; Pinho, V; Soares, AC; Souza, DG; Teixeira, M; Vieira, AT, 2003)
"Pretreatment with rolipram significantly attenuated the intramuscular distribution of 14C-DG, producing a relatively homogeneous distribution of radioactivity."( Gee, A; Hosoi, R; Inoue, O; Nishimura, T; Shukuri, M; Terai, M, 2005)
"Pretreatment with rolipram significantly reduced LR, eosinophils infiltration, and histamine release into the bronchoalveolar space during the early asthmatic reaction."( Chazan, R; Glapiński, J; Grubek-Jaworska, H; Hoser, G; Nejman-Gryz, P, 2006)
"Treatment with rolipram was followed by inhibition of the early phase of AIA associated with downregulation of both OVA-specific splenocyte proliferation and decreases of IFN-gamma released from the spleen cells but no decreases of the amount of IL-10, or levels of anti-OVA IgG, IgG2a, and IgG1."( Alam, AH; Hossain, MA; Li, X; Takano, H; Taneda, S; Yamaki, K; Yanagisawa, R; Yoshino, S, 2007)
"Mice treated with Rolipram (10 mg/kg after training showed elevated cyclic AMP but not cyclic GMP in frontal cortex, thalamus, and hypothalamus."( Bonnet, KA; Judge, ME; Quartermain, D; Randt, CT, 1982)
"Pretreatment with rolipram (30 mumol/kg) and Org 20421 (30 mumol/kg) abolished the eosinophilia and neutrophilia evoked by ovalbumin."( Barnes, PJ; Chung, KF; Elwood, W; Giembycz, MA; Sun, J, 1995)
"Pretreatment with rolipram (10 mg kg-1, i.p.) prevented airway hyperreactivity to histamine which develops 24 h after exposure of conscious guinea-pigs to aerosol PAF (500 micrograms ml-1) or antigen (5 mg ml-1)."( Cortijo, J; Martí-Cabrera, M; Morcillo, EJ; Ortiz, JL; Vallés, JM, 1996)
"Treatment with rolipram, but not theophylline, prevented the increase in responsiveness to inhaled histamine 24 h after antigen challenge."( Blake, SM; Gozzard, N; Herd, CM; Higgs, GA; Holbrook, M; Hughes, B; Page, CP, 1996)
"Pretreatment with rolipram also attenuated increases in serum tumor necrosis factor alpha (TNFalpha) levels induced by LPS and zymosan treatment, measured after 2.5 h."( Hellewell, PG; Miotla, JM; Teixeira, MM, 1998)
"Treatment with rolipram (10 microM) and forskolin (5 microM) for 25 min decreased Lp to 37% of control."( Adamson, RH; Curry, FE; Fry, GN; Liu, B; Rubin, LL, 1998)
"Treatment with rolipram, and to a lesser extent pentoxifylline, significantly reduced the severity of the colonic histopathology and MPO levels."( Diaz-Granados, N; Howe, K; Lu, J; McKay, DM, 2000)
"Pretreatment with rolipram abrogated oedema formation and significantly inhibited hyperalgesia."( Cunha, FQ; Francischi, JN; Poole, S; Tafuri, WL; Teixeira, MM; Yokoro, CM, 2000)
"Pre-treatment with rolipram prevented the decline in cardiac index in animals that received LPS."( Dutta, P; Ryan, DE; Tabrizchi, R, 2001)
"Treatment with rolipram when started at 6 h after QA injection resulted in neuronal damage amounting to 60%; the result after starting at 24 h was not different from solvent (91%)."( Block, F; Nolden-Koch, M; Schmidt, W; Schwarz, M, 2001)
"6. Treatment with rolipram and RP 73401 dose-dependently inhibited eosinophil adhesion and migration in vitro."( Alves, AC; Barreto, EO; Cordeiro, RS; Jose, PJ; Lagente, V; Martins, MA; Pires, AL; Serra, MF; Silva, JP; Silva, PM; Teixeira, MM, 2001)
"Treatment with rolipram reduced the escape latency."( Nagakura, A; Niimura, M; Takeo, S, 2002)

Roles (2)

RoleDescription
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
EC 3.1.4.* (phosphoric diester hydrolase) inhibitorAn EC 3.1.* (ester hydrolase) inhibitor that interferes with the action of a phosphoric diester hydrolase (EC 3.1.4.*).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
rolipramA member of the lclass of pyrrolidin-2-ones that is pyrrolidin-2-one bearing a 3-(cyclopentyloxy)-4-methoxyphenyl substituent at the 4-position. It is a type IV-specific phosphodiesterase (PDE4) inhibitor.
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

rolipram is involved in 1 pathway(s), involving a total of 0 unique proteins and 13 unique compounds

PathwayProteinsCompounds
Phosphodiesterases in neuronal function013

Protein Targets (102)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency14.21910.012610.691788.5700AID887
TDP1 proteinHomo sapiens (human)Potency16.78890.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency3.54810.180013.557439.8107AID1468
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
EWS/FLI fusion proteinHomo sapiens (human)Potency3.59920.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency63.09570.016525.307841.3999AID602332
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency7.75430.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency22.74960.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
lamin isoform A-delta10Homo sapiens (human)Potency0.00200.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
CREB-binding proteinHomo sapiens (human)Potency0.03910.02822.360012.5893AID907; AID916
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency22.74961.000012.224831.6228AID885
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency2.41080.003245.467312,589.2998AID2517
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
Chain A, CruzipainTrypanosoma cruziPotency21.45090.002014.677939.8107AID1476; AID1478
glp-1 receptor, partialHomo sapiens (human)Potency0.20040.01846.806014.1254AID624148; AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency4.25960.100020.879379.4328AID488772; AID588453
USP1 protein, partialHomo sapiens (human)Potency70.79460.031637.5844354.8130AID743255
GLI family zinc finger 3Homo sapiens (human)Potency0.06010.000714.592883.7951AID1259369; AID1259392
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency27.54040.01237.983543.2770AID1645841
estrogen nuclear receptor alphaHomo sapiens (human)Potency6.44180.000229.305416,493.5996AID743069
arylsulfatase AHomo sapiens (human)Potency0.02391.069113.955137.9330AID720538
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
Bloom syndrome protein isoform 1Homo sapiens (human)Potency1.00000.540617.639296.1227AID2364; AID2528
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.98110.039816.784239.8107AID1454
flap endonuclease 1Homo sapiens (human)Potency8.43680.133725.412989.1251AID588795
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency35.48130.010323.856763.0957AID2662
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency11.22020.050127.073689.1251AID588590
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency19.95260.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency19.95261.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, cAMP-specific phosphodiesterase PDE4D2Homo sapiens (human)IC50 (µMol)0.33000.33000.44000.5500AID977608
Chain A, cAMP-specific phosphodiesterase PDE4D2Homo sapiens (human)IC50 (µMol)0.33000.33000.44000.5500AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.28800.00090.07390.2880AID977608
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)0.93030.00001.068010.0000AID157302; AID157779; AID158447; AID158466; AID159936; AID275702; AID695680
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.36660.00001.104010.0000AID1060996; AID157302; AID158447; AID158466; AID159936; AID1625374; AID1625375; AID275701; AID448555; AID647425; AID735056
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)1.09800.00001.465110.0000AID157302; AID158447; AID158466; AID159936; AID275703
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.44220.00001.146310.0000AID157302; AID158447; AID158466; AID159936; AID1625379; AID275704
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)3.16230.00002.072410.0000AID157297
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)3.16230.00031.990110.0000AID157297
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.50000.00040.16800.9772AID1060996
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)116.85440.00001.77679.2000AID159057; AID159067; AID1797296; AID1799753; AID241176; AID260821
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki200.00001.00001.90002.8000AID159075
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)IC50 (µMol)127.66690.00001.85239.2000AID1797296; AID1799753; AID260828
Retina-specific copper amine oxidaseHomo sapiens (human)IC50 (µMol)0.00030.00030.00520.0100AID159969
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)115.02170.00001.18439.6140AID157937; AID157952; AID158099; AID158112; AID158584; AID1797296; AID1799753; AID260827
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki200.00000.00071.07978.5000AID158118
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)IC50 (µMol)16.00000.00801.16175.6000AID260830
3',5'-cyclic-AMP phosphodiesterase Sus scrofa (pig)IC50 (µMol)3.63000.00103.40026.4000AID158405
ReninHomo sapiens (human)IC50 (µMol)3.50000.00000.77968.2000AID160134
Tumor necrosis factorHomo sapiens (human)IC50 (µMol)4.23330.20000.67911.3000AID1372328; AID1372331; AID215076
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50 (µMol)1,355.00000.40002.23759.9000AID158756; AID46326
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)IC50 (µMol)0.72870.00032.723210.0000AID158402; AID158405; AID159952; AID159964; AID159969; AID160103; AID160105; AID195536; AID219415; AID45804; AID45806
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)Ki0.01100.01101.01233.0000AID160121
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)IC50 (µMol)0.72870.00032.723210.0000AID158402; AID158405; AID159952; AID159964; AID159969; AID160103; AID160105; AID195536; AID219415; AID45804; AID45806
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)Ki0.01100.01101.01233.0000AID160121
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)IC50 (µMol)0.84470.00032.663810.0000AID157915; AID158402; AID158405; AID159952; AID159964; AID159969; AID160103; AID160105; AID195536; AID219415; AID45804; AID45806
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)Ki0.01100.01101.01233.0000AID160121
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)10.00000.00021.557410.0000AID241176
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.05890.00031.465610.0000AID1799063
Adenosine receptor A1Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00020.552110.0000AID31403
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)1.19420.00001.068010.0000AID1254336; AID1335402; AID1404140; AID155682; AID157744; AID157775; AID158402; AID158457; AID158463; AID158465; AID158469; AID159517; AID159628; AID159632; AID159634; AID159635; AID159636; AID159640; AID159645; AID159654; AID159656; AID159777; AID159778; AID159783; AID159787; AID159793; AID159796; AID159935; AID160128; AID160129; AID160134; AID160135; AID1703915; AID219165; AID225258; AID260823; AID314437; AID349551; AID349562; AID363083; AID363084; AID363085; AID363086; AID363087; AID363094; AID440693; AID517457; AID662984; AID695680; AID704168; AID759595
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki1.79150.00041.43528.7600AID157304; AID157758; AID157760; AID159650; AID159663; AID159806; AID159810; AID1797212; AID1799063; AID225259; AID238295; AID239332
Adenosine receptor A2bRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00240.68169.0000AID33406
Adenosine receptor A2aRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00120.48289.0000AID33406
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)0.09500.00030.81978.4900AID759595
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)1.50000.00010.729810.0000AID1311212
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)1.50000.00030.38877.0000AID1311212
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC50 (µMol)100.00000.00000.54509.1000AID1480235
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)IC50 (µMol)0.72870.00032.723210.0000AID158402; AID158405; AID159952; AID159964; AID159969; AID160103; AID160105; AID195536; AID219415; AID45804; AID45806
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)Ki0.01100.01101.01233.0000AID160121
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC50 (µMol)112.50000.23002.510510.0000AID158884; AID158890; AID158909; AID314434
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)Ki200.00009.50009.750010.0000AID158913
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)IC50 (µMol)1,355.00000.40002.23759.9000AID158756; AID46326
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50 (µMol)149.35920.00002.14179.2000AID158884; AID158890; AID158909; AID1797296
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)Ki200.00009.50009.750010.0000AID158913
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BRattus norvegicus (Norway rat)IC50 (µMol)100.00000.10000.20000.3000AID179556
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)17.00120.00001.104010.0000AID1160998; AID1166735; AID1247790; AID1254336; AID1254337; AID1311212; AID1335403; AID1374977; AID1381681; AID1404136; AID1404141; AID1420132; AID1420139; AID1421678; AID1427214; AID1464265; AID1512227; AID1512233; AID155682; AID157744; AID157785; AID158457; AID158463; AID158465; AID1593011; AID159517; AID1596202; AID159628; AID159632; AID159634; AID159635; AID159636; AID159640; AID159645; AID159654; AID159656; AID159777; AID159778; AID159783; AID159787; AID159793; AID159796; AID159935; AID160128; AID160129; AID160134; AID160135; AID1625373; AID1625374; AID1667995; AID1703916; AID1707985; AID1724978; AID1727166; AID1743663; AID1743666; AID1783024; AID1797296; AID1884344; AID219165; AID225256; AID225258; AID260824; AID314438; AID318118; AID318127; AID349551; AID349562; AID363083; AID363084; AID363085; AID363086; AID363087; AID363088; AID363089; AID363090; AID363091; AID363092; AID363093; AID363094; AID425684; AID425685; AID440693; AID517456; AID662984; AID704167; AID731227; AID733565; AID736493
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki1.25770.00041.16418.7600AID157304; AID157758; AID157760; AID159650; AID159663; AID159806; AID159810; AID159939; AID159940; AID1797212; AID1799063; AID225259; AID238295; AID239333
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)2.78120.00001.465110.0000AID1254336; AID1335404; AID1404142; AID155682; AID157744; AID157917; AID157918; AID158457; AID158463; AID158465; AID159517; AID159628; AID159632; AID159634; AID159635; AID159636; AID159640; AID159645; AID159654; AID159656; AID159777; AID159778; AID159783; AID159787; AID159793; AID159796; AID159935; AID160128; AID160129; AID160134; AID160135; AID1703917; AID1773140; AID1773141; AID219165; AID225258; AID260825; AID349551; AID349562; AID363083; AID363084; AID363085; AID363086; AID363087; AID363094; AID440693; AID662984; AID704166
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki0.22640.00040.12471.0000AID157304; AID157758; AID157760; AID159650; AID159663; AID159806; AID159810; AID225259; AID238295
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)15.88510.00001.146310.0000AID1129294; AID1160999; AID1166733; AID1177596; AID1177597; AID1187760; AID1254336; AID1254338; AID1261704; AID1335405; AID1351564; AID1374976; AID1404143; AID1420133; AID1420140; AID1427215; AID1464266; AID1512234; AID1543153; AID1543154; AID155682; AID157744; AID157921; AID157922; AID158457; AID158463; AID158465; AID1591866; AID159517; AID1596204; AID159628; AID159632; AID159634; AID159635; AID159636; AID159640; AID159645; AID159654; AID159656; AID159777; AID159778; AID159783; AID159787; AID159793; AID159796; AID1598959; AID159935; AID160128; AID160129; AID160134; AID160135; AID1605515; AID1623076; AID1625378; AID1625379; AID1703918; AID1724979; AID1727184; AID1743664; AID1773990; AID1797296; AID1799753; AID1884574; AID219165; AID225258; AID260822; AID260824; AID260826; AID260838; AID260839; AID260840; AID260841; AID314439; AID349551; AID349562; AID363083; AID363084; AID363085; AID363086; AID363087; AID363094; AID363095; AID363096; AID363097; AID363098; AID363099; AID363100; AID363101; AID363102; AID389793; AID425687; AID440693; AID440695; AID440702; AID440708; AID440709; AID440710; AID462320; AID517458; AID662984; AID704164
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki1.44180.00041.52938.7600AID157304; AID157758; AID157760; AID159650; AID159663; AID159806; AID159810; AID1797212; AID1799063; AID225259; AID238295; AID239334; AID239335; AID239336; AID395330; AID440708; AID440709; AID440710
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)145.18350.00002.072410.0000AID155664; AID155672; AID159213; AID159214; AID159219; AID159222; AID159227; AID159342; AID1797296; AID241177; AID260822
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)Ki200.00000.00500.33811.4000AID159490
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)IC50 (µMol)200.00000.09001.63104.6900AID1381682; AID1421679
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC50 (µMol)133.33330.23001.98149.0000AID158884; AID158890; AID158909
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)Ki200.00009.50009.750010.0000AID158913
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)122.00000.00031.990110.0000AID155664; AID155672; AID159213; AID159214; AID159219; AID159222; AID159227; AID159342; AID1799753; AID241177; AID260822
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)Ki200.00000.00500.32091.4000AID159490
cGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)IC50 (µMol)88.66670.00331.624010.0000AID157930; AID219317; AID662985
Endothelin-1 receptorSus scrofa (pig)Ki0.00450.00450.00450.0045AID159650
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CRattus norvegicus (Norway rat)IC50 (µMol)100.00000.10000.20000.3000AID179556
Protein cereblonHomo sapiens (human)IC50 (µMol)202.00000.28601.70663.0000AID1685005
Protein cereblonHomo sapiens (human)Ki102.00001.49006.580010.0000AID1685005
Phosphodiesterase Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.10000.20000.3000AID179556
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)IC50 (µMol)141.60640.00001.97009.2000AID1797296; AID260832
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)IC50 (µMol)154.16700.00002.05139.2000AID1797296
Phosphodiesterase Sus scrofa (pig)IC50 (µMol)100.00000.62000.73150.8430AID155675
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC50 (µMol)141.60640.00001.49049.2000AID1797296; AID260831
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)EC50 (µMol)0.48000.01701.21593.4000AID695683
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)EC50 (µMol)0.50000.01701.21593.4000AID695683
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)EC50 (µMol)0.66000.22000.66001.1000AID260834; AID650863
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)EC50 (µMol)1.10001.10001.10001.1000AID260834
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)Log IC500.00570.00570.00570.0057AID157916
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Log IC500.00590.00590.00590.0059AID157781
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Log IC500.00640.00640.00640.0064AID157924
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)Log IC500.00400.00400.00400.0040AID159498
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)Log IC500.00400.00400.00400.0040AID159498
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (330)

Processvia Protein(s)Taxonomy
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
sensory perception of smellcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of protein kinase A signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
neutrophil homeostasiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
neutrophil chemotaxiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
leukocyte migrationcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to lipopolysaccharidecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-5 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of heart contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
establishment of endothelial barriercAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesioncGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cellular response to insulin stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesion mediated by integrincGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of lipid catabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
oocyte maturationcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
lipid metabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
response to xenobiotic stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of meiotic nuclear divisioncGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of apoptotic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
steroid hormone mediated signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of oocyte developmentcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of ribonuclease activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to cGMPcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
apoptotic signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IICREB-binding proteinHomo sapiens (human)
response to hypoxiaCREB-binding proteinHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayCREB-binding proteinHomo sapiens (human)
chromatin remodelingCREB-binding proteinHomo sapiens (human)
regulation of DNA-templated transcriptionCREB-binding proteinHomo sapiens (human)
protein acetylationCREB-binding proteinHomo sapiens (human)
signal transductionCREB-binding proteinHomo sapiens (human)
canonical NF-kappaB signal transductionCREB-binding proteinHomo sapiens (human)
regulation of smoothened signaling pathwayCREB-binding proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase ICREB-binding proteinHomo sapiens (human)
N-terminal peptidyl-lysine acetylationCREB-binding proteinHomo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathwayCREB-binding proteinHomo sapiens (human)
protein destabilizationCREB-binding proteinHomo sapiens (human)
cellular response to nutrient levelsCREB-binding proteinHomo sapiens (human)
cellular response to UVCREB-binding proteinHomo sapiens (human)
homeostatic processCREB-binding proteinHomo sapiens (human)
embryonic digit morphogenesisCREB-binding proteinHomo sapiens (human)
positive regulation of DNA-templated transcriptionCREB-binding proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IICREB-binding proteinHomo sapiens (human)
rhythmic processCREB-binding proteinHomo sapiens (human)
protein-containing complex assemblyCREB-binding proteinHomo sapiens (human)
regulation of cellular response to heatCREB-binding proteinHomo sapiens (human)
positive regulation of protein localization to nucleusCREB-binding proteinHomo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationCREB-binding proteinHomo sapiens (human)
heart valve developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
ventricular septum developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
aorta developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of inflammatory responsecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
establishment of endothelial barriercGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to mechanical stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cAMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cGMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to 2,3,7,8-tetrachlorodibenzodioxinecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of gene expressioncGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of mitochondrion organizationcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
regulation of DNA-templated transcriptionHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cellular response to epidermal growth factor stimulusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
catecholamine metabolic processRetina-specific copper amine oxidaseHomo sapiens (human)
xenobiotic metabolic processRetina-specific copper amine oxidaseHomo sapiens (human)
visual perceptionRetina-specific copper amine oxidaseHomo sapiens (human)
amine metabolic processRetina-specific copper amine oxidaseHomo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
signal transductionHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP metabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP catabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of long-term synaptic potentiationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
negative regulation of neural precursor cell proliferationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
behavioral fear responseHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
visual learningHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
operant conditioningHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
neuromuscular process controlling balanceHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
negative regulation of steroid hormone biosynthetic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
kidney developmentReninHomo sapiens (human)
mesonephros developmentReninHomo sapiens (human)
angiotensin maturationReninHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionReninHomo sapiens (human)
proteolysisReninHomo sapiens (human)
regulation of blood pressureReninHomo sapiens (human)
male gonad developmentReninHomo sapiens (human)
hormone-mediated signaling pathwayReninHomo sapiens (human)
response to lipopolysaccharideReninHomo sapiens (human)
response to immobilization stressReninHomo sapiens (human)
drinking behaviorReninHomo sapiens (human)
regulation of MAPK cascadeReninHomo sapiens (human)
cell maturationReninHomo sapiens (human)
amyloid-beta metabolic processReninHomo sapiens (human)
response to cAMPReninHomo sapiens (human)
response to cGMPReninHomo sapiens (human)
cellular response to xenobiotic stimulusReninHomo sapiens (human)
juxtaglomerular apparatus developmentReninHomo sapiens (human)
positive regulation of gene expressionTumor necrosis factorHomo sapiens (human)
negative regulation of gene expressionTumor necrosis factorHomo sapiens (human)
positive regulation of MAP kinase activityTumor necrosis factorHomo sapiens (human)
positive regulation of MAPK cascadeTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-33 productionTumor necrosis factorHomo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseTumor necrosis factorHomo sapiens (human)
negative regulation of miRNA transcriptionTumor necrosis factorHomo sapiens (human)
positive regulation of miRNA transcriptionTumor necrosis factorHomo sapiens (human)
negative regulation of signaling receptor activityTumor necrosis factorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IITumor necrosis factorHomo sapiens (human)
positive regulation of gene expressionTumor necrosis factorHomo sapiens (human)
negative regulation of gene expressionTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-8 productionTumor necrosis factorHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processTumor necrosis factorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IITumor necrosis factorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityTumor necrosis factorHomo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascadeTumor necrosis factorHomo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseTumor necrosis factorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionTumor necrosis factorHomo sapiens (human)
positive regulation of synoviocyte proliferationTumor necrosis factorHomo sapiens (human)
positive regulation of I-kappaB phosphorylationTumor necrosis factorHomo sapiens (human)
negative regulation of apoptotic signaling pathwayTumor necrosis factorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IITumor necrosis factorHomo sapiens (human)
response to hypoxiaTumor necrosis factorHomo sapiens (human)
microglial cell activationTumor necrosis factorHomo sapiens (human)
positive regulation of cytokine productionTumor necrosis factorHomo sapiens (human)
positive regulation of protein phosphorylationTumor necrosis factorHomo sapiens (human)
negative regulation of endothelial cell proliferationTumor necrosis factorHomo sapiens (human)
negative regulation of L-glutamate import across plasma membraneTumor necrosis factorHomo sapiens (human)
macrophage activation involved in immune responseTumor necrosis factorHomo sapiens (human)
chronic inflammatory response to antigenic stimulusTumor necrosis factorHomo sapiens (human)
leukocyte migration involved in inflammatory responseTumor necrosis factorHomo sapiens (human)
regulation of immunoglobulin productionTumor necrosis factorHomo sapiens (human)
negative regulation of cytokine production involved in immune responseTumor necrosis factorHomo sapiens (human)
positive regulation of chronic inflammatory response to antigenic stimulusTumor necrosis factorHomo sapiens (human)
positive regulation of humoral immune response mediated by circulating immunoglobulinTumor necrosis factorHomo sapiens (human)
skeletal muscle contractionTumor necrosis factorHomo sapiens (human)
negative regulation of systemic arterial blood pressureTumor necrosis factorHomo sapiens (human)
glucose metabolic processTumor necrosis factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTumor necrosis factorHomo sapiens (human)
inflammatory responseTumor necrosis factorHomo sapiens (human)
humoral immune responseTumor necrosis factorHomo sapiens (human)
JNK cascadeTumor necrosis factorHomo sapiens (human)
circadian rhythmTumor necrosis factorHomo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsTumor necrosis factorHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageTumor necrosis factorHomo sapiens (human)
response to xenobiotic stimulusTumor necrosis factorHomo sapiens (human)
response to virusTumor necrosis factorHomo sapiens (human)
response to salt stressTumor necrosis factorHomo sapiens (human)
response to fructoseTumor necrosis factorHomo sapiens (human)
negative regulation of heart rateTumor necrosis factorHomo sapiens (human)
vascular endothelial growth factor productionTumor necrosis factorHomo sapiens (human)
positive regulation of gene expressionTumor necrosis factorHomo sapiens (human)
negative regulation of gene expressionTumor necrosis factorHomo sapiens (human)
negative regulation of lipid storageTumor necrosis factorHomo sapiens (human)
response to activityTumor necrosis factorHomo sapiens (human)
regulation of metabolic processTumor necrosis factorHomo sapiens (human)
calcium-mediated signalingTumor necrosis factorHomo sapiens (human)
extracellular matrix organizationTumor necrosis factorHomo sapiens (human)
osteoclast differentiationTumor necrosis factorHomo sapiens (human)
sequestering of triglycerideTumor necrosis factorHomo sapiens (human)
cortical actin cytoskeleton organizationTumor necrosis factorHomo sapiens (human)
positive regulation of protein-containing complex assemblyTumor necrosis factorHomo sapiens (human)
positive regulation of fever generationTumor necrosis factorHomo sapiens (human)
negative regulation of myelinationTumor necrosis factorHomo sapiens (human)
response to nutrient levelsTumor necrosis factorHomo sapiens (human)
negative regulation of interleukin-6 productionTumor necrosis factorHomo sapiens (human)
positive regulation of chemokine productionTumor necrosis factorHomo sapiens (human)
positive regulation of fractalkine productionTumor necrosis factorHomo sapiens (human)
positive regulation of type II interferon productionTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-1 beta productionTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-18 productionTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-6 productionTumor necrosis factorHomo sapiens (human)
positive regulation of interleukin-8 productionTumor necrosis factorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationTumor necrosis factorHomo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTumor necrosis factorHomo sapiens (human)
positive regulation of heterotypic cell-cell adhesionTumor necrosis factorHomo sapiens (human)
toll-like receptor 3 signaling pathwayTumor necrosis factorHomo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityTumor necrosis factorHomo sapiens (human)
response to isolation stressTumor necrosis factorHomo sapiens (human)
response to macrophage colony-stimulating factorTumor necrosis factorHomo sapiens (human)
vasodilationTumor necrosis factorHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTumor necrosis factorHomo sapiens (human)
positive regulation of apoptotic processTumor necrosis factorHomo sapiens (human)
positive regulation of programmed cell deathTumor necrosis factorHomo sapiens (human)
regulation of canonical NF-kappaB signal transductionTumor necrosis factorHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTumor necrosis factorHomo sapiens (human)
negative regulation of protein-containing complex disassemblyTumor necrosis factorHomo sapiens (human)
positive regulation of protein-containing complex disassemblyTumor necrosis factorHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processTumor necrosis factorHomo sapiens (human)
positive regulation of MAP kinase activityTumor necrosis factorHomo sapiens (human)
positive regulation of MAPK cascadeTumor necrosis factorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionTumor necrosis factorHomo sapiens (human)
positive regulation of JUN kinase activityTumor necrosis factorHomo sapiens (human)
positive regulation of neuron apoptotic processTumor necrosis factorHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationTumor necrosis factorHomo sapiens (human)
negative regulation of viral genome replicationTumor necrosis factorHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processTumor necrosis factorHomo sapiens (human)
response to ethanolTumor necrosis factorHomo sapiens (human)
regulation of fat cell differentiationTumor necrosis factorHomo sapiens (human)
negative regulation of fat cell differentiationTumor necrosis factorHomo sapiens (human)
negative regulation of myoblast differentiationTumor necrosis factorHomo sapiens (human)
negative regulation of osteoblast differentiationTumor necrosis factorHomo sapiens (human)
positive regulation of osteoclast differentiationTumor necrosis factorHomo sapiens (human)
positive regulation of protein catabolic processTumor necrosis factorHomo sapiens (human)
positive regulation of action potentialTumor necrosis factorHomo sapiens (human)
positive regulation of cell adhesionTumor necrosis factorHomo sapiens (human)
positive regulation of mitotic nuclear divisionTumor necrosis factorHomo sapiens (human)
negative regulation of DNA-templated transcriptionTumor necrosis factorHomo sapiens (human)
positive regulation of DNA-templated transcriptionTumor necrosis factorHomo sapiens (human)
negative regulation of mitotic cell cycleTumor necrosis factorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IITumor necrosis factorHomo sapiens (human)
positive regulation of translational initiation by ironTumor necrosis factorHomo sapiens (human)
negative regulation of glucose importTumor necrosis factorHomo sapiens (human)
positive regulation of JNK cascadeTumor necrosis factorHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTumor necrosis factorHomo sapiens (human)
astrocyte activationTumor necrosis factorHomo sapiens (human)
embryonic digestive tract developmentTumor necrosis factorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationTumor necrosis factorHomo sapiens (human)
positive regulation of inflammatory responseTumor necrosis factorHomo sapiens (human)
negative regulation of neurogenesisTumor necrosis factorHomo sapiens (human)
regulation of insulin secretionTumor necrosis factorHomo sapiens (human)
positive regulation of synaptic transmissionTumor necrosis factorHomo sapiens (human)
regulation of synapse organizationTumor necrosis factorHomo sapiens (human)
defense response to Gram-positive bacteriumTumor necrosis factorHomo sapiens (human)
cognitionTumor necrosis factorHomo sapiens (human)
leukocyte tethering or rollingTumor necrosis factorHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTumor necrosis factorHomo sapiens (human)
negative regulation of lipid catabolic processTumor necrosis factorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisTumor necrosis factorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityTumor necrosis factorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityTumor necrosis factorHomo sapiens (human)
positive regulation of protein transportTumor necrosis factorHomo sapiens (human)
response to glucocorticoidTumor necrosis factorHomo sapiens (human)
positive regulation of hair follicle developmentTumor necrosis factorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTumor necrosis factorHomo sapiens (human)
regulation of synaptic transmission, glutamatergicTumor necrosis factorHomo sapiens (human)
positive regulation of glial cell proliferationTumor necrosis factorHomo sapiens (human)
positive regulation of vitamin D biosynthetic processTumor necrosis factorHomo sapiens (human)
positive regulation of calcidiol 1-monooxygenase activityTumor necrosis factorHomo sapiens (human)
epithelial cell proliferation involved in salivary gland morphogenesisTumor necrosis factorHomo sapiens (human)
regulation of branching involved in salivary gland morphogenesisTumor necrosis factorHomo sapiens (human)
negative regulation of vascular wound healingTumor necrosis factorHomo sapiens (human)
negative regulation of branching involved in lung morphogenesisTumor necrosis factorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeTumor necrosis factorHomo sapiens (human)
cellular response to lipopolysaccharideTumor necrosis factorHomo sapiens (human)
cellular response to amino acid stimulusTumor necrosis factorHomo sapiens (human)
cellular response to retinoic acidTumor necrosis factorHomo sapiens (human)
cellular response to nicotineTumor necrosis factorHomo sapiens (human)
cellular response to type II interferonTumor necrosis factorHomo sapiens (human)
cellular response to ionizing radiationTumor necrosis factorHomo sapiens (human)
positive regulation of mononuclear cell migrationTumor necrosis factorHomo sapiens (human)
positive regulation of podosome assemblyTumor necrosis factorHomo sapiens (human)
endothelial cell apoptotic processTumor necrosis factorHomo sapiens (human)
protein localization to plasma membraneTumor necrosis factorHomo sapiens (human)
negative regulation of oxidative phosphorylationTumor necrosis factorHomo sapiens (human)
inflammatory response to woundingTumor necrosis factorHomo sapiens (human)
extrinsic apoptotic signaling pathwayTumor necrosis factorHomo sapiens (human)
cellular response to toxic substanceTumor necrosis factorHomo sapiens (human)
liver regenerationTumor necrosis factorHomo sapiens (human)
necroptotic signaling pathwayTumor necrosis factorHomo sapiens (human)
negative regulation of bile acid secretionTumor necrosis factorHomo sapiens (human)
antiviral innate immune responseTumor necrosis factorHomo sapiens (human)
response to Gram-negative bacteriumTumor necrosis factorHomo sapiens (human)
positive regulation of neuroinflammatory responseTumor necrosis factorHomo sapiens (human)
negative regulation of amyloid-beta clearanceTumor necrosis factorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionTumor necrosis factorHomo sapiens (human)
positive regulation of amyloid-beta formationTumor necrosis factorHomo sapiens (human)
response to L-glutamateTumor necrosis factorHomo sapiens (human)
positive regulation of neutrophil activationTumor necrosis factorHomo sapiens (human)
positive regulation of protein localization to plasma membraneTumor necrosis factorHomo sapiens (human)
regulation of establishment of endothelial barrierTumor necrosis factorHomo sapiens (human)
negative regulation of bicellular tight junction assemblyTumor necrosis factorHomo sapiens (human)
cellular response to amyloid-betaTumor necrosis factorHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTumor necrosis factorHomo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellTumor necrosis factorHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellTumor necrosis factorHomo sapiens (human)
regulation of membrane lipid metabolic processTumor necrosis factorHomo sapiens (human)
response to 3,3',5-triiodo-L-thyronineTumor necrosis factorHomo sapiens (human)
response to gold nanoparticleTumor necrosis factorHomo sapiens (human)
positive regulation of protein localization to cell surfaceTumor necrosis factorHomo sapiens (human)
positive regulation of blood microparticle formationTumor necrosis factorHomo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 2 productionTumor necrosis factorHomo sapiens (human)
positive regulation of hepatocyte proliferationTumor necrosis factorHomo sapiens (human)
regulation of endothelial cell apoptotic processTumor necrosis factorHomo sapiens (human)
regulation of reactive oxygen species metabolic processTumor necrosis factorHomo sapiens (human)
positive regulation of DNA biosynthetic processTumor necrosis factorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandTumor necrosis factorHomo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayTumor necrosis factorHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
sensory perception of smellcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of protein kinase A signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
response to toxic substanceBifunctional epoxide hydrolase 2Homo sapiens (human)
positive regulation of gene expressionBifunctional epoxide hydrolase 2Homo sapiens (human)
dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
cholesterol homeostasisBifunctional epoxide hydrolase 2Homo sapiens (human)
stilbene catabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
phospholipid dephosphorylationBifunctional epoxide hydrolase 2Homo sapiens (human)
regulation of cholesterol metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide metabolic processBifunctional epoxide hydrolase 2Homo sapiens (human)
regulation of smooth muscle cell apoptotic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cGMP catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
regulation of smooth muscle cell proliferationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
response to amphetamineCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
locomotory behaviorCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
visual learningCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
monocyte differentiationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
dopamine catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
serotonin metabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
neutrophil homeostasiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
neutrophil chemotaxiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
leukocyte migrationcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to lipopolysaccharidecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-5 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of heart contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
establishment of endothelial barriercAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesioncGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cellular response to insulin stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesion mediated by integrincGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of lipid catabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
oocyte maturationcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
lipid metabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
response to xenobiotic stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of meiotic nuclear divisioncGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of apoptotic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
steroid hormone mediated signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of oocyte developmentcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of ribonuclease activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to cGMPcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
apoptotic signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
protein ubiquitinationProtein cereblonHomo sapiens (human)
positive regulation of Wnt signaling pathwayProtein cereblonHomo sapiens (human)
negative regulation of protein-containing complex assemblyProtein cereblonHomo sapiens (human)
positive regulation of protein-containing complex assemblyProtein cereblonHomo sapiens (human)
negative regulation of monoatomic ion transmembrane transportProtein cereblonHomo sapiens (human)
locomotory exploration behaviorProtein cereblonHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processProtein cereblonHomo sapiens (human)
signal transductionDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
negative regulation of cGMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
negative regulation of cAMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cAMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
chemical synaptic transmissioncAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cAMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
negative regulation of cGMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (83)

Processvia Protein(s)Taxonomy
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
enzyme bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
signaling receptor regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
beta-2 adrenergic receptor bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
ATPase bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
scaffold protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
heterocyclic compound bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein kinase B bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nuclear estrogen receptor activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
estrogen bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
transcription coactivator bindingCREB-binding proteinHomo sapiens (human)
p53 bindingCREB-binding proteinHomo sapiens (human)
chromatin bindingCREB-binding proteinHomo sapiens (human)
damaged DNA bindingCREB-binding proteinHomo sapiens (human)
transcription coactivator activityCREB-binding proteinHomo sapiens (human)
transcription corepressor activityCREB-binding proteinHomo sapiens (human)
histone acetyltransferase activityCREB-binding proteinHomo sapiens (human)
protein bindingCREB-binding proteinHomo sapiens (human)
zinc ion bindingCREB-binding proteinHomo sapiens (human)
acetyltransferase activityCREB-binding proteinHomo sapiens (human)
peptide N-acetyltransferase activityCREB-binding proteinHomo sapiens (human)
MRF bindingCREB-binding proteinHomo sapiens (human)
histone H3K18 acetyltransferase activityCREB-binding proteinHomo sapiens (human)
histone H3K27 acetyltransferase activityCREB-binding proteinHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCREB-binding proteinHomo sapiens (human)
peptide-lysine-N-acetyltransferase activityCREB-binding proteinHomo sapiens (human)
peptide lactyltransferase activityCREB-binding proteinHomo sapiens (human)
DNA-binding transcription factor bindingCREB-binding proteinHomo sapiens (human)
chromatin DNA bindingCREB-binding proteinHomo sapiens (human)
magnesium ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
zinc ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
TPR domain bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
phosphate ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein homodimerization activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
kinase bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
protein kinase activator activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
protein bindingRetina-specific copper amine oxidaseHomo sapiens (human)
primary amine oxidase activityRetina-specific copper amine oxidaseHomo sapiens (human)
electron transfer activityRetina-specific copper amine oxidaseHomo sapiens (human)
quinone bindingRetina-specific copper amine oxidaseHomo sapiens (human)
aliphatic amine oxidase activityRetina-specific copper amine oxidaseHomo sapiens (human)
copper ion bindingRetina-specific copper amine oxidaseHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
protein bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
metal ion bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
aspartic-type endopeptidase activityReninHomo sapiens (human)
signaling receptor bindingReninHomo sapiens (human)
insulin-like growth factor receptor bindingReninHomo sapiens (human)
protein bindingReninHomo sapiens (human)
peptidase activityReninHomo sapiens (human)
transcription cis-regulatory region bindingTumor necrosis factorHomo sapiens (human)
protease bindingTumor necrosis factorHomo sapiens (human)
cytokine activityTumor necrosis factorHomo sapiens (human)
tumor necrosis factor receptor bindingTumor necrosis factorHomo sapiens (human)
protein bindingTumor necrosis factorHomo sapiens (human)
death receptor agonist activityTumor necrosis factorHomo sapiens (human)
identical protein bindingTumor necrosis factorHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
magnesium ion bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
epoxide hydrolase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
toxic substance bindingBifunctional epoxide hydrolase 2Homo sapiens (human)
phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
10-hydroxy-9-(phosphonooxy)octadecanoate phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lipid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
protein homodimerization activityBifunctional epoxide hydrolase 2Homo sapiens (human)
lysophosphatidic acid phosphatase activityBifunctional epoxide hydrolase 2Homo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
enzyme bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
signaling receptor regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
beta-2 adrenergic receptor bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
ATPase bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
scaffold protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
heterocyclic compound bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein kinase B bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nuclear estrogen receptor activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
estrogen bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
protein bindingProtein cereblonHomo sapiens (human)
transmembrane transporter bindingProtein cereblonHomo sapiens (human)
metal ion bindingProtein cereblonHomo sapiens (human)
cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cGMP bindingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
metal ion bindingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
metal ion bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (56)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
ruffle membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
synaptic vesiclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
postsynaptic densitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
Z disccAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
dendritic spinecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
excitatory synapsecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
extracellular spacecAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
ciliumcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
apical plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
endoplasmic reticulumcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
Golgi apparatuscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
guanyl-nucleotide exchange factor complexcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytoplasmCREB-binding proteinHomo sapiens (human)
nucleusCREB-binding proteinHomo sapiens (human)
nucleoplasmCREB-binding proteinHomo sapiens (human)
cytoplasmCREB-binding proteinHomo sapiens (human)
cytosolCREB-binding proteinHomo sapiens (human)
nuclear bodyCREB-binding proteinHomo sapiens (human)
chromatinCREB-binding proteinHomo sapiens (human)
histone acetyltransferase complexCREB-binding proteinHomo sapiens (human)
transcription regulator complexCREB-binding proteinHomo sapiens (human)
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
endoplasmic reticulumcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
Golgi apparatuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
presynaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
synaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial matrixcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
extracellular exosomeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
nucleusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cytoplasmRetina-specific copper amine oxidaseHomo sapiens (human)
plasma membraneRetina-specific copper amine oxidaseHomo sapiens (human)
plasma membraneRetina-specific copper amine oxidaseHomo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
endoplasmic reticulumHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
Golgi apparatusHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cytosolHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
plasma membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
ruffle membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
sarcolemmaHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perikaryonHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cellular_componentHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
nucleusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
extracellular regionReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
plasma membraneReninHomo sapiens (human)
apical part of cellReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
extracellular spaceTumor necrosis factorHomo sapiens (human)
phagocytic cupTumor necrosis factorHomo sapiens (human)
extracellular regionTumor necrosis factorHomo sapiens (human)
extracellular spaceTumor necrosis factorHomo sapiens (human)
plasma membraneTumor necrosis factorHomo sapiens (human)
external side of plasma membraneTumor necrosis factorHomo sapiens (human)
cell surfaceTumor necrosis factorHomo sapiens (human)
neuronal cell bodyTumor necrosis factorHomo sapiens (human)
membrane raftTumor necrosis factorHomo sapiens (human)
recycling endosomeTumor necrosis factorHomo sapiens (human)
cell surfaceTumor necrosis factorHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
nucleoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
ruffle membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomal matrixBifunctional epoxide hydrolase 2Homo sapiens (human)
cytosolBifunctional epoxide hydrolase 2Homo sapiens (human)
extracellular exosomeBifunctional epoxide hydrolase 2Homo sapiens (human)
peroxisomeBifunctional epoxide hydrolase 2Homo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
synaptic vesiclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
postsynaptic densitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
Z disccAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
dendritic spinecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
excitatory synapsecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
extracellular spacecAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
ciliumcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
apical plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
endoplasmic reticulumcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
Golgi apparatuscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
guanyl-nucleotide exchange factor complexcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
nucleusHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
cytosolHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
lysosomeCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nucleusProtein cereblonHomo sapiens (human)
cytoplasmProtein cereblonHomo sapiens (human)
cytosolProtein cereblonHomo sapiens (human)
membraneProtein cereblonHomo sapiens (human)
perinuclear region of cytoplasmProtein cereblonHomo sapiens (human)
Cul4A-RING E3 ubiquitin ligase complexProtein cereblonHomo sapiens (human)
cellular_componentDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cytosolDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
synapsecAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cytosolcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (809)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID157779PDE4A activity assessed using human recombinant purified GST-PDE4A2481999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Substituted furans as inhibitors of the PDE4 enzyme.
AID448555Inhibition of human recombinant PDE4B by scintillation proximity assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
AID1598194Selectivity ratio of IC50 for recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells to IC50 for recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infected Sf9 insect cells2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.
AID1060996Inhibition of human recombinant PDE4B2 assessed as inhibition of cAMP hydrolysis by colorimetric assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.
AID76664Antigen-induced bronchoconstriction in guinea pigs after peroral administration 1 hour pre-treatment1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID695680Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID210151Inhibition of LPS-stimulated tumor necrosis factor-alpha release by human whole blood2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID158447Inhibition of partially-purified PDE 4 from human monocytes1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.
AID1370513Antiviral activity against Zika virus infected in human A549 cells preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID158468Competition of [3H]rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosol1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID267646Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1370515Cytotoxicity against human A549 cells assessed as cell viability at 1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID1625379Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cells2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID130614Inhibition of lipopolysaccharide (LPS)-induced TNF alpha generation in mouse1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID167443Stimulation of acid secretion from rabbit parietal glands1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID1598192Selectivity ratio of IC50 for recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) expressed in baculovirus infected Sf9 insect cells to IC50 for recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infecte2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.
AID275702Inhibition of human recombinant PDE4A2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
AID695683Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID157297Inhibitory activity of the against phosphodiesterase 3 (PDE3); No significant inhibitory activity at pIC502001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID159936Inhibitory concentration against phosphodiesterase 4 (PDE4) in cytosol of human neutrophils2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID156050Inhibition of N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated production of reactive oxygen species (ROS) in human PMNL by 35% of control2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID275704Inhibition of human recombinant PDE4D2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
AID1370516Cytotoxicity against human A549 cells assessed as cell viability at 10 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID90823Inhibition of lipopolysaccharide (LPS)-induced TNF alpha release by human monocytes1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID267645Antiviral activity against wild type HIV1 virus2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1370514Cytotoxicity against human A549 cells assessed as cell viability at 0.1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID210611The value for hypothermia against antigen provocation (po)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID647425Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
AID131562Reversal of reserpine-induced hypothermia in the mouse on peroral administration1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID76663Antigen-induced bronchoconstriction in guinea pigs after iv administration 10 min pre-treatment1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID233957Ratio of ROS IC35/PDE4 IC50 was determined2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID219081Emetic effect in ferret model, threshold value1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Substituted furans as inhibitors of the PDE4 enzyme.
AID1625374Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID59636Emetic effect in dogs1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID1625375Inhibition of human N-terminal His6-tagged C-terminal FLAG-tagged PDE4B2 expressed in baculovirus infected sf9 cells using cAMP as substrate by microplate reader analysis2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID157302Inhibition of phosphodiesterase 4 (PDE4) in human neutrophils2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID735056Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30 mins by colorimetric assay method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
AID275701Inhibition of human recombinant PDE4B2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
AID1370517Cytotoxicity against human A549 cells assessed as cell viability at 100 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID158466Inhibition activity against human monocyte derived PDE4 catalytic activity (LPDE4)1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID133069Percent inhibition of arachidonic acid induced mouse ear edema after 1 hr pretreatment with 30 uM/kg peroral dose2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
AID275703Inhibition of human recombinant PDE4C2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
AID235540Value is the ratio between HPDE4 and LPDE41998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2010Nature biotechnology, Jan, Volume: 28, Issue:1
Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety.
AID1811Experimentally measured binding affinity data derived from PDB2003Structure (London, England : 1993), Jul, Volume: 11, Issue:7
Three-dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2003Structure (London, England : 1993), Jul, Volume: 11, Issue:7
Three-dimensional structures of PDE4D in complex with roliprams and implication on inhibitor selectivity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID159966Inhibition of rolipram binding to rat brain2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID159072Inhibitory concentration against phosphodiesterase 2 from rat kidney2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID1464267Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins before LPS stimulation for 18 hrs by TR-FRET assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID159806Inhibition of rolipram binding to Phosphodiesterase 42002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
AID260839Inhibition of C5a mediated human eosinophil chemotaxis2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1598203Induction of emesis in ICR mouse assessed as reduction in ketamine/xylazine-induced duration of anesthesia at 0.1 mg/kg, ip pretreated for 15 mins followed by ketamine/xylazine addition2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.
AID1480237Solubility in sodium phosphate buffer at pH 7.42018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
AID1725049Inhibition of Pam3Cys-induced TNFalpha production in C57BL/6 mouse bone marrow derived Macrophage at 1 to 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Synthesis and SAR Studies of 1
AID260825Inhibition of PDE4C2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID160109Inhibition of phosphodiesterase 4 from rat liver at 0.1 uM2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID160128Inhibition of Rolipram binding to PDE4 at 1 uM1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.
AID612628Antiinflammatory activity in mouse neutrophils assessed as inhibition of LPS-stimulated TNFalpha cytokine expression at 100 ug/ml after 3 hrs by flow cytometeric analysis2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Psilostachyin, acetylated pseudoguaianolides and their analogues: preparation and evaluation of their anti-inflammatory potential.
AID632290Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness.
AID159656Inhibition of human Phosphodiesterase 42001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
AID1311212Inhibition of PDE4B derived from human monocytes using [3H]-cAMP as substrate after 30 mins2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors.
AID1480239Inhibition of PDE4 (unknown origin) expressed in HEK293 cells co-expressing PM-AKAR3 assessed as increase in cAMP levels by FRET assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
AID77063Reduced histamine-induced bronchoconstriction in anesthetized guinea pig at 1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID363088Inhibition of human PDE4B1 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID160134Inhibition of phosphodiesterase 41998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.
AID1365249Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production at 10 uM pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents.
AID759595Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
AID159645Inhibitory potency against guinea pig ventricular phosphodiesterase 42000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID425689Inhibition of PDE7A2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1370517Cytotoxicity against human A549 cells assessed as cell viability at 100 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID425687Inhibition of PDE4D22009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID314436Inhibition of PDE3A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID1591866Inhibition of recombinant human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli BL21 codonplus cells using [3H]cAMP as substrate preincubated for 15 mins followed by substrate addition by liquid scintillation counting method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.
AID1543153Inhibition of human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli strain BL21 using [3H]cAMP as substrate after 15 mins by liquid scintillation counter analysis
AID222150Inhibition of fMLP-induced oxidative burst in human eosinophils2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID1372328Inhibition of LPS-induced TNF-alpha production in human PBMC preincubated for 30 mins followed by LPS addition measured after 5 hrs by ELISA2018Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-α production.
AID239334Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4DE (PDE4DE) in baculovirus expression system2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID1512230Antiinflammatory activity against LPS-induced sepsis Swiss albino mouse model assessed as downregulation of IL6 production in serum at 10 mg/kg, po administered once at 1.5 hrs before LPS challenge and measured after 90 mins2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID440693Inhibition of PDE4 from human U937 cells2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID314439Inhibition of PDE4D2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID1598959Inhibition of PDE4D (unknown origin) using cAMP as substrate2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
AID395508Antidepressant activity in ICR mouse assessed as decrease in immobility duration at 0.5 mg/kg, ip once a day for 8 days by forced swimming test2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
AID157760Inhibition of Phosphodiesterase 41997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
AID1153963Inhibition of LPS-induced TNF-alpha production in human PBMC2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Synthesis and structure-activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-α.
AID1512233Inhibition of PDE4B in human U937 cells using [3H] cAMP as substrate incubated for 30 mins2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID1374975Inhibition of PDE4 in human PBMC assessed as reduction in LPS-stimulated TNFalpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID215247Inhibition of tumor necrosis factor alpha (TNF-alpha) release in murine endotoxemia model after peroral administration1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
AID349562Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID43768In vivo inhibition of antigen induced eosinophil recruitment in Brown-Norvway Rats at 10 mg/kg peroral dose2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID318123Antiviral activity against HIV2 ROD in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID159506Inhibition of bovine arterial Phosphodiesterase 41996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Studies of cardiotonic agents. 8. Synthesis and biological activities of optically active 6-(4-(benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl-3(2H)- pyridazinone (KF15232).
AID159342Inhibitory concentration against phosphodiesterase 3 from human platelet2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID1667995Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay2020Bioorganic & medicinal chemistry letters, 05-15, Volume: 30, Issue:10
Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation.
AID1703918Inhibition of PDE4D (unknown origin)2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID219415Inhibition of [3H]rolipram binding to Wistar rat brain membranes2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID225258Inhibition of phosphodiesterase type IV (PDE4) activity1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Orally active indole N-oxide PDE4 inhibitors.
AID1335399Inhibition of human PDE2A using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID77059Reduced histamine-induced bronchoconstriction in anesthetized guinea pig at 0.1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID159213Inhibitory activity against cGMP inhibited Phosphodiesterase 3, isolated from guinea pig ventricular tissue1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
AID133091Inhibition of reserpine-induced hypothermia in mice by peroral dose1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID1177597Inhibition of human PDE4D22014Journal of natural products, Aug-22, Volume: 77, Issue:8
Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi.
AID1157542Toxicity in Marshall ferret assessed as vomiting at 1 mg/kg, po after 2 hrs2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID260831Inhibition of PDE102006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1187756Inhibition of PDE4D3 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID159932Relative inhibition of rolipram binding and Phosphodiesterase 4 activity2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
AID158402Inhibition of recombinant human PDE4A expressed in Sf9 cells2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
AID1593011Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.
AID1420141Selectivity index, ratio of IC50 for human U937 cells-derived PDE4D to IC50 for human U937 cells-derived PDE4B2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID1254339Selectivity ratio of IC50 for human full-length PDE4B1 to IC50 for human full-length PDE4D72015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
AID1707985Inhibition of recombinant human PDE4B using 5'-cGMP as substrate measured after 90 mins by colorimetric assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.
AID1884344Inhibition of PDE4B (unknown origin) using [3H]cAMP as substrate incubated for 1 hr by PDElight HTS cAMP phosphodiesterase assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis.
AID389793Inhibition of full length human PDE4D2 expressed in Escherichia coli BL21 by liquid scintillation counting2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.
AID1872570Inhibition of PDE4 (unknown origin)2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID157781Inhibition of phosphodiesterase (PDE) 4A1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID158909Inhibition of phosphodiesterase 1 at 20 uM1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1166735Inhibition of human recombinant PDE4B2 assessed after 60 mins by IMAP fluorescence polarization assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID1512234Inhibition of PDE4D in human U937 cells using [3H]cAMP as substrate incubated for 30 mins2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID159635Inhibition of guinea pig PDE IV1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1160999Inhibition of human recombinant PDE4D2 activity assessed as residual cAMP concentration by HTRF assay2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Novel Roflumilast analogs as soft PDE4 inhibitors.
AID71925In vitro inotropic effect, 20% increase in the force of contraction of isolated ferret papillary muscle strips (Not reached at 100 uM)1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase.
AID159783Inhibition of human Phosphodiesterase 42002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
AID1625378Inhibition of human His-tagged PDE4D catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID241177Inhibition of Phosphodiesterase 32005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID241180Inhibition of Phosphodiesterase 72005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID1773135Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID349559Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID440712Selectivity ratio of Ki for human PDE4D2 to Ki for human PDE4D32009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID1727186Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum alanine aminotransferase level at 50 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID131172In vivo inhibition of LPS induced tumor necrosis factor (TNF-alpha) in mice1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Orally active indole N-oxide PDE4 inhibitors.
AID215591Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Thalidomide analogs and PDE4 inhibition.
AID260833Selectivity for PDE4D2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID241178Inhibition of Phosphodiesterase 42005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID219317Inhibitory activity against phosphodiesterase was determined in vitro using bovine aorta, at 1 uM cGMP for cGMP-PDE.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
AID425690Inhibition of PDE7B2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID318118Inhibition of PDE4B2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Rhodanine derivatives as novel inhibitors of PDE4.
AID1157532Inhibition of Hartley guinea pig PDE4 assessed as hydrolization of cAMP by measuring [3H]cAMP at 100 nM by radioisotope method2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID1353616Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta production at 10 uM after 24 hrs by ELISA relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation.
AID1703891Vasorelaxant activity in OVA-sensitized guinea pig-derived trachea assessed as decrease in CCh-induced tracheal tonic contraction in absence of functional epithelium treated with compound after contraction stabilised2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1773165Induction of apoptosis in human A549 cells assessed as increase in late apoptotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.955%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID759554Toxicity in iv dosed ferret assessed as first emetic dose by measuring occurrence of vomiting episode after 6 hrs2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
AID632939Inhibition of PDE in rat UMR106 cells co-expressing CRE-luc assessed as PTH-induced cAMP accumulation by luciferase reporter gene assay2011Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2.
AID157917Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase 4C1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID230413Ratio of PDEIV IC50 to IC50 [3H]rolipram high affinity binding.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
AID1335403Inhibition of full length human PDE4B1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID425677Inhibition of PDE1A2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1311213Anti-inflammatory activity in human PBMC assessed as suppression of LPS-induced TNF-alpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors.
AID159632Inhibition of guinea pig macrophage Phosphodiesterase 41998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.
AID1743666Inhibition of PDE4B in human PBMC assessed as reduction in LPS-induced TNFalpha release preincubated for 30 mins followed by LPS stimulation and measured after 18 hrs by TR-FRET assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID1872571Displacement of [3H]-Rolipram from full-length recombinant human PDE4 expressed in yeast membrane by liquid scintillation counting method2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID239336Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D5 (PDE4D5) in baculovirus expression system2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID363086Inhibition of human PDE4A10 in cytosolic fraction of inflammatory cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1464280Inhibition of LPS-induced TNFalpha production in Swiss Albino mouse model of sepsis at 10 mg/kg, po pre-treated 30 mins before LPS challenge and measured 90 mins post LPS injection by ELISA method relative to untreated control2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID1157545Toxicity in po dosed Marshall ferret assessed as vomiting2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID1231629Inhibition of human recombinant PDE4A4 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
AID1773177Induction of apoptosis in human U-251 cells assessed as increase in late apoptotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.311%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID157763Relative inhibition of phosphodiesterase 4 activity and rolipram binding to PDE42002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID612629Antiinflammatory activity in mouse neutrophils assessed as inhibition of LPS-stimulated IL1-beta expression after 4-5 hrs by ELISA relative to control2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Psilostachyin, acetylated pseudoguaianolides and their analogues: preparation and evaluation of their anti-inflammatory potential.
AID1623117Neuroprotection in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as reduction in ratio of apoptotic neuron in CA3 hippocampus region at 4 mg/kg/day, ig administered for 26 consecutive days by hematoxylin and2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID704139Antiinflammatory activity in A/J mouse assessed as inhibition of mononuclear cell accumulation in bronchoalveolar space at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID260834cAMP elevation in U937 cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID314444Inhibition of PDE10A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID232484Selectivity ratio indicated as IC50 value in inhibiting PDE4B or PDE4A compared to PDE4D2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID1261704Inhibition of human PDE4D using 3H-cAMP as substrate after 15 mins by liquid scintillation counting analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
AID704166Inhibition of human recombinant PDE4C2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID158459Binding affinity against PDE4 was determined using [3H]- rolipram in guinea pig brain membrane binding assay1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
AID704168Inhibition of human recombinant PDE4A2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID1365250Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents.
AID473491Antiinflammatory activity in mouse assessed as inhibition of phorbol ester-induced ear edema at 1 mg/ear2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
AID157770Inhibition of phosphodiesterase (PDE) 4C1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID612630Antiinflammatory activity in mouse neutrophils assessed as inhibition of LPS-stimulated IL-6 expression at 100 ug/ml after 4-5 hrs by ELISA relative to control2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Psilostachyin, acetylated pseudoguaianolides and their analogues: preparation and evaluation of their anti-inflammatory potential.
AID440709Inhibition of human recombinant PDE4D2 expressed in baculovirus system by radiometric assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID155672Inhibition of Phosphodiesterase 3 from human platelets2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID1685005Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay2021ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.
AID425697Inhibition of beta2 adrenergic receptor expressed in HEK293 cells co-transfected with PKA fragments Reg-F[1] and cat-F[2]-fused renilla luciferase assessed as effect on receptor regulated PKA activation at 100 uM after 30 mins by protein-fragment compleme2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID318124Cytotoxicity against human CEM-SS cells2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID92723Evaluated in vitro for its inhibitory activity on LPS-induced TNF-Alpha release in human whole blood.1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID1231631Inhibition of human recombinant PDE4C2 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
AID704146Antiinflammatory activity in A/J mouse lung assessed as inhibition of LPS-induced IL6 production at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID1773143Cell cycle arrest in human A549 cells assessed as G2/M phase at 500 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 6.08%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1335406Inhibition of human PDE5A using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID314435Inhibition of PDE1B2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID1404137Inhibition of recombinant full length human N-terminal GST-tagged PDE4A1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID210148In vitro inhibition of TNF-alpha-release from human whole blood2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID314441Inhibition of PDE7A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID115571Percentage inhibition of serum TNF-alpha in lipopolysaccharide injected mice at 3 mg/kg peroral dose1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID195716Displacement of [3H]rolipram from rat brain membranes1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
AID158884Inhibition of Phosphodiesterase 1 from guinea pig cardiac ventricle1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1773134Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID363083Inhibition of human PDE4A12008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID766608Bronchodilatory activity in ovalbumin-treated guinea pig at 10 mg/kg, po administered 1 hr prior to ovalbumin challenge relative to vehicle-treated control2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors.
AID704138Antiinflammatory activity in A/J mouse assessed as inhibition of eosinophils accumulation in bronchoalveolar space at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID74179Inhibition of antigen-induced bronchoconstriction in anesthetized guinea pig at 0.1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1404138Inhibition of recombinant human N-terminal GST-tagged PDE3B (592-end residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID662984Inhibition of human neutrophil PDE42012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of chalcones as potent and selective PDE5A1 inhibitors.
AID1365248Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents.
AID126634Percent cytokine TNF inhibition in monkeys at 10 mg/kg oral dose1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID158756Inhibitory concentration against phosphodiesterase 1 from bovine, calmodulin2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID1157535Toxicity in Marshall ferret assessed as vomiting at 30 mg/kg, po after 2 hrs2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID260830Inhibition of PDE92006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1731331Displacement of [3H]SR141716A from human CB1R receptor expressed in rat Chem-1 cells at 10 uM incubated for 60 mins by scintillation counting method relative to control2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1353614Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production at 10 uM after 24 hrs by ELISA relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation.
AID159075Inhibition of Phosphodiesterase 21997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
AID159227Inhibition of Phosphodiesterase 3 from guinea pig cardiac ventricle1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1773178Induction of apoptosis in human U-251 cells assessed as increase in necrotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.301%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID158899Inhibition of phosphodiesterase 1 (PDE1) from porcine adrenal tissue2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
AID158309Inhibition of low Km cyclic AMP phosphodiesterase PDE III of rabbit renal cortex1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
AID157744Inhibition of phosphodiesterase 42003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
AID1727189Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum aspartate aminotransferase level at 10 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID222460Inhibition of TNF alpha synthesis in human monocytes2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
AID1129294Inhibition of human PDE4D2 catalytic domain (86 to 413aa) expressed in Escherichia coli strain BL21 after 15 mins by liquid scintillation counting in presence of [3H]-cAMP2014Journal of natural products, Apr-25, Volume: 77, Issue:4
Prenylated coumarins: natural phosphodiesterase-4 inhibitors from Toddalia asiatica.
AID1254332Selectivity ratio of IC50 for PDE4B (unknown origin) to IC50 for PDE4D (unknown origin)2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
AID736493Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay2013European journal of medicinal chemistry, Apr, Volume: 62Montmorillonite K-10 catalyzed green synthesis of 2,6-unsubstituted dihydropyridines as potential inhibitors of PDE4.
AID260838Inhibition of LTB4 mediated human eosinophil chemotaxis2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID74184Inhibition of antigen-induced bronchoconstriction in anesthetized guinea pig at 0.1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1353618Cytotoxicity against human PBMC assessed as cell viability at 10 um after 24 hrs by WST-1 assay relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation.
AID517457Inhibition of PDE4A4 expressed in yeast2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
AID1335401Inhibition of human PDE4 catalytic domain using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID222461Inhibition of TNF-alpha synthesis in human monocytes2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
AID363085Inhibition of human PDE4A4B in particular fraction of inflammatory cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID159952Affinity for the high affinity rolipram binding site of phosphodiesterase (PDE IV) by [3H]rolipram displacement.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
AID159796Inhibitory activity on human eosinophil phosphodiesterase 4.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID1773990Inhibition of PDE4D2 (86-413) (unknown origin) expressed in Escherichia coli BL21 assessed as using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counting analysis
AID1335412Inhibition of human PDE11A using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID226828Ratio of inhibitory activity against PDE4 to that of binding affinity towards rolipram binding site on PDE4 was determined2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
AID159350Inhibition of Phosphodiesterase 3 at 50 uM1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID1166733Inhibition of human recombinant PDE4D3 assessed after 60 mins by IMAP fluorescence polarization assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID209003Emetic effect in shrews at 10 mg/kg peroral dose, 3 of 3 animals affected1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.
AID1598202Memory enhancement effect in ICR mouse assessed as improvement in novel object discrimination at 0.1 mg/kg, ip administered via gavage measured for 5 mins by open field test2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.
AID314438Inhibition of PDE4B2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID214056Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID1773163Induction of apoptosis in human A549 cells assessed as increase in viable cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 98.4%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1420144Anti-inflammatory activity in Sprague-Dawley rat model of LPS-induced asthma/COPD assessed as inhibition of neutrophilia in BALF at 10 mg/kg, po administered 30 mins prior to LPS challenge for 40 mins and measured after 6 hrs relative to control2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID15809950% inhibitory concentration against phosphodiesterase 5 (PDE5) from porcine platelets2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
AID704169Inhibition of bovine PDE4 using [3H]cAMP as substrate2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID179558Evaluated for Ca++ independent phosphodiesterase activity. 1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
AID159778Inhibition of Phosphodiesterase 4 (PDE-4) from human U937 cells2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID157915Inhibitory activity against Phosphodiesterase 4B (PDE4B) from rat source expressed in Saccharomyces cerevisiae2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID363089Inhibition of human PDE4B1 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1703893Vasorelaxant activity in OVA-sensitized guinea pig-derived trachea assessed as decrease in CCh-induced tracheal tonic contraction in presence of functional epithelium treated with compound after contraction stabilised2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1335404Inhibition of full length human PDE4C1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID363092Inhibition of human PDE4B3 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID363094Inhibition of human PDE4B4 in cytosolic fraction of liver and brain2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID158469Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase type 4A (PDE4A).1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID155675Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
AID232680Selectivity as ratio of IC50 against PDE III to IC50 against PDE IV from guinea pig1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1625373Inhibition of human PDE4B catalytic domain (152 to 528 residues)2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID363078Binding affinity to PDE4 catalytic domain2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID159939Inhibition of human Phosphodiesterase 4B1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.
AID517456Inhibition of PDE4B1 expressed in yeast2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
AID1404139Inhibition of PDE11A (unknown origin) using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID1272079Anti-inflammatory activity in BALB/c mouse assessed as inhibition of LPS-induced TNFalpha expression at 10 mg/kg, po pre-treated for 1 hr followed by LPS administration measured 2.5 hrs after LPS challenge by ELISA2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Analogues of boswellic acids as inhibitors of pro-inflammatory cytokines TNF-α and IL-6.
AID363102Inhibition of human PDE4D5 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1335400Inhibition of human PDE3B using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID233754Evaluated for the ratio of binding affinity to rolipram binding site to that of PDE-4 inhibitory activity2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID1370518Antiviral activity against Zika virus infected in human A549 cells assessed as virus titer preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID260826Inhibition of PDE4D2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1157536Induction of bronchodilation in ovalbumin-sensitized guinea pig at 10 mg/kg, po administered 4 hrs prior to ovalbumin challenge measured for 20 mins relative to vehicle-treated control2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID425688Inhibition of PDE5A12009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1783024Inhibition of PDE4B (unknown origin) using [3H]cAMP as substrate incubated for 30 mins by scintillation proximity assay2021European journal of medicinal chemistry, Oct-05, Volume: 221PdCl
AID462320Inhibition of human PDE4D2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
AID1727187Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum aspartate aminotransferase level at 50 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID1187754Inhibition of PDE4D1 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID1545635Inhibition of human recombinant full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells at 10'-5.5 M using cAMP as substrate incubated for 20 mins followed by substrate addition by luciferase assay relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
AID1605538Toxicity in Beagle dog assessed as animals exhibiting emesis at 1 mg/kg, po observed for 180 mins2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
AID33406Evaluated for the binding affinity towards the Adenosine A2 receptor in corpora striata of rats using [3H]NECA as radioligand.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
AID241179Inhibition of Phosphodiesterase 52005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID158919Inhibition of phosphodiesterase 1/5 isozyme (PDE1/5) mixture isolated from the guinea pig trachea.2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID260827Inhibition of PDE52006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1157543Toxicity in Marshall ferret assessed as vomiting at 10 mg/kg, po after 2 hrs2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID160111In vitro inhibitory activity against phosphodiesterase 4 from rat liver at concentration of 0.3 uM2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID155792Inhibition of LPS induced TNF-alpha release by human peripheral blood mononuclear cells.1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID349551Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID159940Inhibition of cAMP hydrolysis by the human phosphodiesterase 4B enzyme1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID1703916Inhibition of PDE4B (unknown origin)2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID89020Inhibition of LPS-induced TNF-alpha secretion from purified human peripheral blood monocytes1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.
AID1335409Inhibition of human PDE8A1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID157922Inhibitory activity against Phosphodiesterase 4D (PDE4D) from human source expressed in Saccharomyces cerevisiae2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID1623111Cognition enhancement activity in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as swimming path length in virtual platform at 4 mg/kg/day, ig administered for 26 consecutive days by Morris water maze test (2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1623116Neuroprotection in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as reduction in ratio of apoptotic neuron in CA1 hippocampus region at 4 mg/kg/day, ig administered for 26 consecutive days by hematoxylin and2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID126633Percent cytokine IL-8 inhibition in monkeys at 10 mg/kg oral dose1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID1153962Inhibition of LPS-induced TNF-alpha production in rat PBMC2014Bioorganic & medicinal chemistry letters, Jul-01, Volume: 24, Issue:13
Synthesis and structure-activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-α.
AID260821Inhibition of PDE22006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1254337Inhibition of human full-length PDE4B1 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assay2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
AID425679Inhibition of PDE1C2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID159351Inhibition of human platelet Phosphodiesterase 3 at 20 uM2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID1272077Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 expression at 10 uM after 5 hrs2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Analogues of boswellic acids as inhibitors of pro-inflammatory cytokines TNF-α and IL-6.
AID425694Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID695680Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID704163Proemetic activity in A/J mouse assessed as reversal of xylazine/katamine-induced anesthesia at 1 to 50 umol/kg, sc administered 30 mins prior xylazine/ketamine-administration2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID159489Inhibition of phosphodiesterase 3 at 200 uM1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID1623078Effective permeability of the compound at 100 ug/ml after 10 hrs by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1464266Inhibition of PDE4D isolated from human U937 cells using [3H]-cAMP incubated for 30 mins2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID159219Inhibition of guinea pig ventricular Phosphodiesterase 31997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
AID1335411Inhibition of human PDE10A2 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID1427214Inhibition of human U937 cells-derived PDE4B using [3H]cAMP as substrate after 30 mins
AID1420133Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate measured after 30 mins2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.
AID1724979Inhibition of recombinant human N-terminal GST-tagged PDE4D3 expressed in baculovirus infected Sf9 cells by radioligand binding assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Synthesis and SAR Studies of 1
AID440700Inhibition of human recombinant PDE4D2 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID78186Inhibition of eosinophil recruitment in guinea pig lung asthma model at 10 mg/kg1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
PDE4 inhibitors: new xanthine analogues.
AID76563Inhibition of bronchoconstriction in passively-sensitized guinea pig at 1 mg/kg iv dose 10 min prior to challenge2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID363095Inhibition of human PDE4D1 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1335407Inhibition of human PDE6C using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID160105Inhibition of Phosphodiesterase 4 from rat liver2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
AID229961Relative inhibition of PDE 4 activity and rolipram binding1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
AID1247790Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID1743667Antiinflammatory activity in LPS induced Swiss albino mouse model of sepsis assessed as inhibition of TNFalpha production at 10 mg/kg, po preincubated for 30 mins followed by LPS stimulation and measured after 90 mins by ELISA relative to control2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID157775Inhibitory activity against Phosphodiesterase 4A (PDE4A) from human source expressed in Saccharomyces cerevisiae2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID229338Relative inhibition of rolipram binding and PDE4 activity2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID318120Inhibition of HIV1 reverse transcriptase2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1773152Cell cycle arrest in human U-251 cells assessed as G2/M phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 14.43%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID158584Inhibitory activity against cGMP-phosphodiesterase from porcine aorta1994Journal of medicinal chemistry, Jun-24, Volume: 37, Issue:13
Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
AID226824Ratio inhibition of phosphodiesterase 4 to Rolipram binding site activity was reported.1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID45804Inhibition of cAMP-specific calcium-independent phosphodiesterase (IPDE)1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.
AID1187753Inhibition of recombinant human PDE4D3 expressed in baculoviral system at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID77843Change in heart rate in guinea pigs after 0.1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID349557Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID78274Schultz-Dale (SD) reaction in tracheal strip isolated from passively sensitized guinea pigs1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones.
AID318122Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID637704Inhibition of recombinant His-tagged PDE4B using cAMP as substrate at 30 uM preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay2012European journal of medicinal chemistry, Feb, Volume: 48Montmorillonite K-10 mediated green synthesis of cyano pyridines: Their evaluation as potential inhibitors of PDE4.
AID1335398Inhibition of human PDE1A using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID1370513Antiviral activity against Zika virus infected in human A549 cells preincubated for 5 hrs followed by compound wash measured after 48 hrs by viral plague-forming assay2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID1381681Inhibition of human GST-tagged PDE4B expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.
AID239333Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4BL (PDE4BL) in baculovirus expression system2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID225256Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytes2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
AID241176Inhibition of Phosphodiesterase 22005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID260823Inhibition of PDE4A2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1374973Anti-inflammatory activity in Sprague-Dawley rat model of LPS-induced asthma/COPD assessed as inhibition of neutrophilia in BALF at 10 mg/kg, po administered 30 mins prior to LPS challenge for 40 mins relative to control2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID72088Emetic effect in ferrets at 0.03 mg/kg peroral dose, 2 of 10 animals affected1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
AID363098Inhibition of human PDE4D3 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1187761Inhibition of PDE4B2 (unknown origin)2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID260832Inhibition of PDE112006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID766607Antiinflammatory activity in mouse assessed as inhibition ovalbumin-induced eosinophil infiltration into lung at 10 mg/kg, po administered 30 mins prior to ovalbumin challenge followed by once per day compound administration measured after 2 days relative2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors.
AID1460297Inhibition of recombinant His-tagged PDE4B1 (unknown origin) expressed in baculovirus infected sf9 cells at 10 uM using cAMP as substrate preincubated for 15 mins followed by cAMP addition measured after 1 hr by PDE light HTS assay relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
1,2,3-Triazole-nimesulide hybrid: Their design, synthesis and evaluation as potential anticancer agents.
AID1261705Inhibition of recombinant human Amyloid beta (1 to 42) self-induced aggregation at 5 uM after 48 hrs by thioflavin T-based fluorescence assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
AID1884589Neuroprotective activity against rat PC-12 cells assessed as inhibition of Abeta(25-35)-induced cytotoxicity by measuring increase in cell viability at 10 uM incubated for 24 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease.
AID751649Displacement of [3H]Rolipram from rolipram binding site in Wistar rat brain after 60 mins2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1773151Cell cycle arrest in human U-251 cells assessed as G0/G1 phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 67.34%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1380118Inhibition of PDE4 (unknown origin)2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.
AID219165Inhibitory activity against phosphodiesterase was determined in vitro using bovine aorta, at 1 uM cAMP for cAMP-PDE.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
AID751715Displacement of [3H]Rolipram from rolipram binding site in Wistar rat brain at 10 uM after 60 mins relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID157937Inhibition of Phosphodiesterase 5 of guinea pig lung1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID1480256Increase in thermal withdrawal latency in naive Sprague-Dawley rat at 3 mg/kg administered via oral gavage measured over 4 hrs2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
AID1773164Induction of apoptosis in human A549 cells assessed as increase in early apoptotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.955%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1703915Inhibition of PDE4A (unknown origin)2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID155682Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line.2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID1335402Inhibition of full length human PDE4A4 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID1427217Anti-inflammatory activity in LPS-induced Swiss albino mouse sepsis model assessed as inhibition of TNF-alpha release in serum at 10 mg/kg, po administered 30 mins prior to LPS challenge measured after 90 mins by ELISA relative to control
AID157304Inhibition of rolipram binding to PDE4 from human neutrophils2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
AID234199Relative inhibition of PDE4 activity and [3H]rolipram binding to guinea pig brain1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID349564Antiinflammatory activity in mouse ear edema model assessed as inhibition of PMA-induced ear edema at 1 mg/ear administered 2 times 30 mins before and 15 mins after PMA challenge measured after 6 hrs of PMA application relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID666554Antiinflammatory activity in rat astrocytes assessed as inhibition of LPS-induced nitrite production at 30 uM incubated for 1 hr prior to LPS-challenge measured after 24 hrs by Griess method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds.
AID159517Inhibition of Canine Tracheal Smooth Muscle PDE 41992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones.
AID1231630Inhibition of human recombinant PDE4B2 expressed in baculoviral system using cAMP as substrate at 10 uM by fluorescence polarization assay relative to control2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
AID704149Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID1596207Inhibition of PDE4C (unknown origin) at 10 uM using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry relative to control2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1596202Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID1187759Inhibition of PDE4C2 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID159941Displacement of [3H]rolipram from mouse brain homogenates1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
AID159222Inhibitory potency against guinea pig ventricular phosphodiesterase 32000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID1703917Inhibition of PDE4C (unknown origin)2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID133090Inhibition of immobility in mouse forced swim test by peroral dose1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID1161988Inhibition of recombinant His-tagged PDE4B1 (unknown origin) expressed in Sf9 cells at 30 uM pre-incubated for 15 mins before cAMP substrate addition by luminescence assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Ligand-free Pd-catalyzed C-N cross-coupling/cyclization strategy: an unprecedented access to 1-thienyl pyrroloquinoxalines for the new approach towards apoptosis.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID158278Inhibition of Phosphodiesterase 72004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID363087Inhibition of human PDE4A10 in particular fraction of brain and lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1353617Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta production after 24 hrs by ELISA2018European journal of medicinal chemistry, Mar-10, Volume: 147Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation.
AID130856Percent inhibition of arachidonic acid induced mouse ear edema after 30 uM/kg peroral pretreatment2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.
AID517458Inhibition of PDE4D3 expressed in yeast2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
AID1374977Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 mins2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID59504Emetic effect in dogs on intravenous dose (2/2)1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Orally active indole N-oxide PDE4 inhibitors.
AID1166731Inhibition of human recombinant PDE3A assessed as inhibition of hydrolysis of [3H]cAMP at 10 uM after 20 mins by scintillation proximity assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID1231638Toxicity in mouse assessed as sedative effect by measuring prolongation of immobility time at 10 mg/kg, po measured over 60 mins by open-field test2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
AID704167Inhibition of human recombinant PDE4B2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID1058566Inhibition of recombinant His-tagged PDE4B1 (unknown origin) expressed in insect Sf9 cells using cAMP as substrate at 30 uM preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay relative to control2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Synthesis and biological evaluation of nimesulide based new class of triazole derivatives as potential PDE4B inhibitors against cancer cells.
AID704142Antiinflammatory activity in A/J mouse assessed as inhibition of neutrophil accumulation in bronchoalveolar space at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID158118Inhibition of Phosphodiesterase 51997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
AID363100Inhibition of human PDE4D4 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1743668Antiinflammatory activity in LPS induced Sprague-Dawley rat model of asthma and COPD assessed as inhibition of neutrophilia at 10 mg/kg, po preincubated for 30 mins followed by LPS stimulation and measured after 6 hrs relative to control2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID440696Inhibition of human recombinant PDE4A4 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID1335408Inhibition of human PDE7A using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID363123Displacement of [3H]rolipram from PDE4 at 100 uM by RBA2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1420140Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 mins2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID363101Inhibition of human PDE4D5 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1166749Emetogenic potential in surrogate emesis CD1 mouse model assessed as effect on xyclacine/ketamine-induced loss of righting reflex at 5 mg/kg, sc2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID1420134Inhibition of PDE4 in human PBMC assessed as reduction in LPS-stimulated TNFalpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.
AID126631Percent Eosinophil inhibition in monkeys at 10 mg/kg oral dose1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID503307Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID260837Inhibition of release of TNF alpha in human whole blood2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID159969Inhibitory activity against purified rat liver phosphodiesterase 42003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID77072In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 50 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1261708Permeability of the compound at 100 ug/ml after 10 hrs by PAMPA assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
AID1404136Inhibition of recombinant full length human N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID1605515Inhibition of human PDE4D2 (86 to 413 residues) expressed in Escherichia coli BL21 codon-plus cells using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation counting method2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
AID314445Inhibition of PDE11A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID1395052Inhibition of PDE4 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibitors of phosphodiesterase as cancer therapeutics.
AID1166727Inhibition of human recombinant PDE7A1 assessed as inhibition of hydrolysis of [3H]cAMP at 10 uM after 20 mins by scintillation proximity assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID159935Inhibitory activity against phosphodiesterase 4 carried out in the cytosol of human neutrophils2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.
AID318125Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1404141Inhibition of recombinant human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID425682Inhibition of PDE3B2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1404142Inhibition of recombinant human full length N-terminal GST-tagged PDE4C1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID314440Inhibition of PDE5A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID440699Inhibition of human recombinant PDE4D1 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID440710Inhibition of human recombinant PDE4D3 expressed in baculovirus system by radiometric assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID58399Emetic effect in dogs at 0.2 mg/kg intravenous dose, 2 of 2 animals affected1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
AID1596204Inhibition of PDE4D2 (unknown origin) using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry2019European journal of medicinal chemistry, Jul-15, Volume: 174InCl
AID318127Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID76100Inhibition of Eosinophilia after peroral administration at 10 mg/Kg compound in guinea pig2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID159498Inhibition of phosphodiesterase (PDE) 31998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID1774030Toxicity in dog assessed as emesis at 1 mg/kg, po
AID543624Antiinflammatory activity against human neutrophils assessed as inhibition of LPS-stimulated TNFalpha production at 100 ug/ml after 3 hrs by FACS analysis2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Evaluation of the antimicrobial, antioxidant, and anti-inflammatory activities of hydroxychavicol for its potential use as an oral care agent.
AID58625Minimum emetic dose in dogs after intravenous administration2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID1773175Induction of apoptosis in human U-251 cells assessed as increase in viable cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 98.3%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID59481Emetic effect in dogs after intravenous dose2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
AID1727166Inhibition of human recombinant PDE4B using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID1365234Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production at 10 uM pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents.
AID159628Inhibitory activity against phosphodiesterase 4 isolated from guinea pig ventricular tissue1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
AID159640Inhibition of guinea pig ventricular Phosphodiesterase 41997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
AID314434Inhibition of PDE1A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID159074Inhibition of phosphodiesterase 2 at 200 uM1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID159777Inhibition of Phosphodiesterase 4 from human U937 cells2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
AID234774Selectivity as ratio of IC50 against PDE3 to IC50 against PDE41999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID160121Inhibition of [3H]rolipram binding to Phosphodiesterase 4 of rat forebrain membrane2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
AID239332Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4AL (PDE4AL) in baculovirus expression system2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID363084Inhibition of human PDE4A4B in cytosolic fraction of inflammatory cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID159634In vitro inhibition of Phosphodiesterase 4 from guinea pig lung1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID91106Inhibition of fMLP induced oxidative burst in human eosinophils.1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID159057Inhibition of guinea pig cardiac ventricle Phosphodiesterase 21999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID58398Emetic effect in dogs at 0.03 mg/kg intravenous dose, 2 of 2 animals affected1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
AID132956Reversal of reserpine-induced hypothermia in mice by intraperitoneal dose1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.
AID158405Inhibition of phosphodiesterase 4 (PDE4) from porcine liver2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
AID157921In vitro inhibitory activity on unpurified recombinant Phosphodiesterase 4D1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID159653Inhibition of Phosphodiesterase 4 from guinea pig lung1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID158894Inhibition of human Phosphodiesterase 1 at 10 uM1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID159358Inhibition of Phosphodiesterase 3 from human platelets2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
AID160114In vitro inhibitory activity against phosphodiesterase 4 from rat liver at concentration of 10 uM2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID57331Emetic effect in dogs administered at 0.03 mg/kg intravenously (No effect)2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.
AID314442Inhibition of PDE7B2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID275700Inhibition of human eosinophil phosphodiesterase2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
AID132958Minimum effective peroral dose (MED) in mouse forced-swim test1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.
AID192815Percentage inhibition of carrageenan-induced rat foot edema at a dose of 32 mg/kg when administered perorally (po).1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID158112Inhibition of phosphodiesterase 5 at 20 uM1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID1512231Antiinflammatory activity against LPS-induced sepsis Swiss albino mouse model assessed as downregulation of TNFalpha production in serum at 10 mg/kg, po administered once at 1.5 hrs before LPS challenge and measured after 90 mins by ELISA2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID1743665Selectivity ratio of IC50 for inhibition of human U937 cells derived PDE4D to inhibition of human U937 cells derived PDE4B2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID1331250Inhibition of PDE4 (unknown origin)2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Design and synthesis of 4,5,6,7-tetrahydro-1H-1,2-diazepin-7-one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors.
AID46326Inhibitory activity against phosphodiesterase was determined in vitro using bovine aorta, at 1 uM cGMP in the presence of calcium (10 uM) and calmodulin (15 nM)1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
AID155664Inhibition of phosphodiesterase 3 (PDE3) isolated from the dog aorta2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID156987Inhibition of cAMP PDE in canine cardiac tissue1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase.
AID1884574Inhibition of PDE4D7 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease.
AID1724982Inhibition of LPS-induced TNFalpha production in C57BL/6 mouse bone marrow derived Macrophage at 1 to 10 uM preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by ELISA2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Synthesis and SAR Studies of 1
AID1187758Inhibition of PDE4B2 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID440695Inhibition of human recombinant PDE4D expressed in Sf9 cells2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID90830Inhibition of TNF-alpha release from LPS-stimulated human mononuclear cells1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
AID155789Inhibition of anti-CD3 induced IFN-gamma-release in human peripheral blood mononuclear cells.1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID157941Inhibition of Phosphodiesterase 5 from guinea pig lung1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID1420139Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 mins2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID238295Inhibition of human phosphodiesterase 42005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
AID232652Relative activity against human Phosphodiesterase type 4 (PDE4) and rat rolipram binding protein (RBA)2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
AID395330Inhibition of human recombinant PDE4D32009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
AID159663Inhibition of rolipram binding to PDE42001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
AID425685Inhibition of PDE4B22009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1492733Inhibition of PDE4 (unknown origin) using FAM-Cyclic-3',5'-AMP as substrate after 1 hr by fluorescence polarization assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Design, synthesis and biological evaluation of substituted aminopyridazin-3(2H)-ones as G0/G1-phase arresting agents with apoptosis-inducing activities.
AID181692Increased acid secretion in isolated whole rat stomach2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
AID157952Inhibitory concentration against phosphodiesterase 5 (PDE5) from human platelet2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID160124Ratio of inhibition of [3H]rolipram binding to that of inhibitory activity against Phosphodiesterase 4 was determined2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID159951Displacement of [3H]rolipram binding to Phosphodiesterase 4 in rat brain1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID666553Antiinflammatory activity in rat microglia cells assessed as inhibition of LPS-induced nitrite production at 30 uM incubated for 1 hr prior to LPS-challenge measured after 24 hrs by Griess method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds.
AID72066Emetic effect in ferrets after peroral administration at 0.03 mg/kg (2/5)2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID1372329Cytotoxicity against human PBMC by MTS assay2018Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-α production.
AID1773153Cell cycle arrest in human U-251 cells assessed as S phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 18.23%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID440701Inhibition of human recombinant PDE4D3 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID219078Emetic effect in ferrets, plasma concentration2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
AID363093Inhibition of human PDE4B3 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1272080Anti-inflammatory activity in BALB/c mouse assessed as inhibition of LPS-induced IL-6 expression at 10 mg/kg, po pre-treated for 1 hr followed by LPS administration measured 2.5 hrs after LPS challenge by ELISA2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Analogues of boswellic acids as inhibitors of pro-inflammatory cytokines TNF-α and IL-6.
AID1335405Inhibition of full length human PDE4D7 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID702885Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei brucei Squib-427 after 72 hrs by fluorescence assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
AID363090Inhibition of human PDE4B2 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1404140Inhibition of recombinant human N-terminal GST-tagged PDE4A4 (2 to 886 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID1625374Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID152782Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID318126Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis at 100 uM2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1727199Antiinflammatory activity in LPS-induced Wistar rat endotoxemia model assessed as decrease in plasma TNFalpha level at 5 mg/kg, ip measured after 2 hr2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID695683Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID1420143Anti-inflammatory activity in Swiss albino mouse model of sepsis assessed as inhibition of LPS-induced TNFalpha release at 10 mg/kg, po administered 30 mins prior to LPS challenge for 90 mins by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID159347Inhibition of Phosphodiesterase 3 (PDE3) from human platelet at 20 uM2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID340315Inhibition of human phosphodiesterase 42008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID1254336Inhibition of core catalytic domains of human PDE4 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assay2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
AID179556Evaluated for Ca++ dependent phosphodiesterase activity. 1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
AID155676PDE4-related emetic activity in ferrets after intravenous administration at 0.6 mg/kg2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID1464265Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP incubated for 30 mins2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID76954Effective dose (mg/kg) in Aerosolized Antigen Induced airway Obstruction assay in guinea pig1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
AID425693Inhibition of PDE11A42009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID181540Binding affinity against high affinity rolipram binding site (HARBS) was determined by displacing radioactive [3H]rolipram from brain membrane suspensions of Wistar rats2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.
AID225259Affinity for rolipram binding site of phosphodiesterase type IV (PDE4)1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Orally active indole N-oxide PDE4 inhibitors.
AID733565Inhibition of human PDE4B22013Journal of natural products, Mar-22, Volume: 76, Issue:3
Benzoquinones and terphenyl compounds as phosphodiesterase-4B inhibitors from a fungus of the order Chaetothyriales (MSX 47445).
AID1420136Anti-inflammatory activity in Sprague-Dawley rat model of LPS-induced asthma/COPD assessed as inhibition of neutrophilia in BALF at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.
AID731227Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.
AID45806Inhibition of phosphodiesterase 4 from rat brain cortex1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID157916Inhibition of phosphodiesterase (PDE) 4B1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID160117Inhibition of phosphodiesterase 4 from rat liver at 3 uM (not determined)2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID209811Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID195536Binding affinity to rolipram binding site in isolated rat brain by rolipram binding assay2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID159957Inhibition of rolipram binding in rat brain2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID1187760Inhibition of recombinant human PDE4D3 expressed in baculoviral system2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID1335410Inhibition of human PDE9A2 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
AID184448Tested in vivo for lowest active dose that induced inhibitory effect on gastric emptying in rats2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
AID1727193Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum IFNgamma level at 10 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID704164Inhibition of human recombinant PDE4D2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID158890Inhibition of Phosphodiesterase 1 of guinea pig cardiac ventricle1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID159636Inhibition of solubilized eosinophil PDE IV1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID159654Inhibition of Phosphodiesterase 4 from human neutrophils2000Bioorganic & medicinal chemistry letters, Oct-02, Volume: 10, Issue:19
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
AID1727184Inhibition of human recombinant PDE4D using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID363010Inhibition of human PDE4 at 2 uM after 20 mins2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID349552Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID1370516Cytotoxicity against human A549 cells assessed as cell viability at 10 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID517459Antiinflammatory activity against LPS-induced TNFalpha production in human whole blood by ELISA2010Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
AID318119Inhibition of PDE3A2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Rhodanine derivatives as novel inhibitors of PDE4.
AID90658Evaluated in vitro for its inhibitory activity on LPS-induced TNF-Alpha release in human monocyte.1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID1625377Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID1727191Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum IFNgamma level at 50 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID58397Emetic effect in dogs at 0.01 mg/kg intravenous dose, 1 of 2 animals affected1998Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
AID440698Inhibition of human recombinant PDE4C2 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID1512227Inhibition of PDE4B in human PBMC assessed as inhibition in LPS-induced TNFalpha production preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET analysis2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID1623118Neuroprotection in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as reduction in ratio of apoptotic neuron in DG hippocampus region at 4 mg/kg/day, ig administered for 26 consecutive days by hematoxylin and 2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1069505Inhibition of PDE4B (unknown origin) expressed in HEK293 cells assessed as increase in forskolin-stimulated cAMP level at 30 uM preincubated for 30 mins followed by forskolin-stimulation measured after 4 hrs by luciferase reporter gene assay relative to c2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
Synthesis of 2H-1,3-benzoxazin-4(3H)-one derivatives containing indole moiety: their in vitro evaluation against PDE4B.
AID76949Effect on Aerosolized Antigen Induced Airway Obstruction (AAIAO) in guinea pig after oral dose1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID363091Inhibition of human PDE4B2 in particular fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1374976Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 mins2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID1420135Anti-inflammatory activity in Swiss albino mouse model of sepsis assessed as inhibition of LPS-induced TNFalpha release at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.
AID1783023Inhibition of PDE4B (unknown origin) using [3H]cAMP as substrate at 10 uM incubated for 30 mins by scintillation proximity assay relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221PdCl
AID425683Inhibition of PDE4A1A2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1743663Inhibition of human U-937 cells derived PDE4B using [3H] cAMP as substrate measured after 30 mins2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID440697Inhibition of human recombinant PDE4B2 expressed in baculovirus system at 10 uM by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID117194Evaluated for antiinflammatory activity in the TPA induced ear inflammation model at a dose 2 mg/kg (50 ug)2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
AID260835Inhibition of release of Eosinophil derived neurotoxin in human whole blood2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1374974Anti-inflammatory activity in Swiss albino mouse model of sepsis assessed as inhibition of LPS-induced TNFalpha release at 10 mg/kg, po administered 30 mins prior to LPS challenge for 90 mins by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID77070In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 20 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID159650Inhibition of rolipram binding to Phosphodiesterase 41998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.
AID75781In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 20 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1404143Inhibition of recombinant human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
AID314443Inhibition of PDE9A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID425675Inhibition of PDE10A12009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1773176Induction of apoptosis in human U-251 cells assessed as increase in early apoptotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 1.12%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1773136Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID260828Inhibition of PDE8A2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1254338Inhibition of human full-length PDE4D7 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assay2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
AID160113In vitro inhibitory activity against phosphodiesterase 4 from rat liver at concentration of 1 uM2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID210152In vivo inhibition of LPS-stimulated TNF-alpha release in Wistar rats at 10 mg/kg oral dose2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID314437Inhibition of PDE4A2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Identification of a potent new chemotype for the selective inhibition of PDE4.
AID76038In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 10 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1464281Inhibition of LPS-induced neutropenia in Sprague-Dawley rat model of asthma assessed as reduction in neutrophils in BAL fluid at 10 mg/kg, po pre-treated 30 mins before LPS challenge and measured 6 hrs after LPS injection relative to untreated control2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
AID363096Inhibition of human PDE4D2 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID219079Emetic effect in ferrets, peroral mg/kg dose2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
AID31403Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
AID159787Inhibition of human phosphodiesterase 4 from U937 cells2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
AID759553Binding affinity to human serum albumin2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
AID1512255Antiinflammatory activity against LPS-induced asthma/COPD Sprague-Dawley rat model assessed as inhibition of LPS-induced neutrophilia treated 30 mins prior to LPS challenge measured after 6 hrs2019Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
AID77242Inhibition of histamine induced bronchoconstriction in guinea pig after intravenous administration2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID241175Inhibition of Phosphodiesterase 12005Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
AID195719Displacement of [3H]rolipram from high affinity binding site (HARBS) in rat brain membrane.2000Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
Synthesis and biological evaluation of 2,5-dihydropyrazol.
AID159964Concentration for inhibitory activity against phosphodiesterase 4 from rat liver2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
AID1773140Inhibition of PDE4 CAT (unknown origin) at 1 uM relative to control2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID425698Inhibition of beta2 adrenergic receptor expressed in HEK293 cells co-transfected with PKA fragments Reg-F[1] and cat-F[2]-fused renilla luciferase assessed as effect on receptor regulated PKA activation at 100 uM after 30 mins by protein-fragment compleme2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1623105Cognition enhancement activity in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as swimming speed at 30 mg/kg/day, ig administered for 26 consecutive days by Morris water maze test (Rvb = 15.6 +/- 2.4 cm/sec2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID158913Inhibition of calcium-calmodulin dependent Phosphodiesterase 11997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
AID1703895Vasorelaxant activity in non-sensitized guinea pig-derived trachea assessed as decrease in CCh-induced tracheal tonic contraction in presence of functional epithelium2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID158463Inhibition of phosphodiesterase 4 from U937 cells1998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Thalidomide analogs and PDE4 inhibition.
AID160129Relative inhibition of phosphodiesterase 4 activity and Rolipram binding to PDE41998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID157930Inhibition of bovine arterial Phosphodiesterase 51996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Studies of cardiotonic agents. 8. Synthesis and biological activities of optically active 6-(4-(benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl-3(2H)- pyridazinone (KF15232).
AID1773141Inhibition of PDE4 CAT (unknown origin)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1427216Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha secretion preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay
AID349565Antiinflammatory activity in mouse ear edema model assessed as inhibition of PMA-induced ear edema at 3 mg/ear administered 2 times 30 mins before and 15 mins after PMA challenge measured after 6 hrs of PMA application relative to control2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID21669Compound tested for plasma levels in monkeys dosed at 10 mg/kg, po1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
AID1727192Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum IL-6 level at 10 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID1166748Emetogenic potential in surrogate emesis CD1 mouse model assessed as effect on xyclacine/ketamine-induced loss of righting reflex at 1 mg/kg, sc2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
AID1724978Inhibition of recombinant human C-terminal His-tagged N-terminal GST-tagged PDE4B2 expressed in baculovirus infected Sf9 cells by radioligand binding assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Synthesis and SAR Studies of 1
AID239335Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D3 (PDE4D3) in baculovirus expression system2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID1427218Anti-inflammatory activity in Sprague-Dawley rat model of LPS-induced asthma/COPD assessed as inhibition of neutrophilia in lungs at 10 mg/kg, po administered 30 mins prior to LPS challenge for 40 mins measured after 6 hrs relative to control
AID425692Inhibition of PDE9A22009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID759589Aqueous solubility of the compound at pH 7.42013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
AID90807Inhibition of TNF-alpha release by lipopolysaccharide stimulated human monocytes1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID158904Inhibition of [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of rabbit renal cortex1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
AID395521Antidepressant activity in ICR mouse assessed as decrease in immobility duration at 0.5 mg/kg, ip by forced swimming test2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
AID260822Inhibition of PDE32006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1625379Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cells2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
AID1157533Induction of bronchodilation in ovalbumin-sensitized guinea pig at 10 mg/kg, po administered 1 hr prior to ovalbumin challenge measured for 20 mins relative to vehicle-treated control2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID704137Antiinflammatory activity in A/J mouse assessed as inhibition of LPS-induced airway resistance provoked by methacholine at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID1420142Inhibition of PDE4 in human PBMC assessed as reduction in LPS-stimulated TNFalpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.
AID1187757Inhibition of PDE4A4 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID440702Inhibition of human recombinant PDE4D3 expressed in baculovirus system by IMAP assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID702886Cytotoxicity against human MRC5 cells after 72 hrs by resazurin assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
AID318121Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID184683Minimal effective dose in an rat anti-immobility effect using behavioral despair test1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
AID1157544Toxicity in Marshall ferret assessed as vomiting at 300 mg/kg, po after 2 hrs2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
AID157924Inhibition of phosphodiesterase (PDE) 4D1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID1727188Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum alanine aminotransferase level at 10 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID1272076Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha expression at 10 uM after 5 hrs2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Analogues of boswellic acids as inhibitors of pro-inflammatory cytokines TNF-α and IL-6.
AID1773144Cell cycle arrest in human A549 cells assessed as S phase at 500 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 14.78%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID157918Inhibitory activity against Phosphodiesterase 4C (PDE4C) from human source expressed in Saccharomyces cerevisiae2000Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
AID1372331Inhibition of LPS-induced TNF-alpha production in human MNC suspension after 20 hrs by radioimmunoassay2018Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-α production.
AID77068In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 10 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1198119Inhibition of PDE4B (unknown origin) transfected into Sf9 cells at 10 uM by PDElight HTS cAMP phosphodiesterase assay2015Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
Design of new hybrid template by linking quinoline, triazole and dihydroquinoline pharmacophoric groups: A greener approach to novel polyazaheterocycles as cytotoxic agents.
AID1727197Antiinflammatory activity in LPS-induced Wistar rat endotoxemia model assessed as decrease in plasma TNFalpha level at 5 mg/kg, ip measured after 1 hr2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID160119Binding affinity towards rolipram binding site on phosphodiesterase 4 using [3H]rolipram as radioligand in crude rat brain homogenate2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID158457Inhibitory activity against Phosphodiesterase type IV (PDE4) obtained from guinea-pig macrophage was evaluated1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
AID115570Percentage inhibition of serum TNF-alpha in lipopolysaccharide injected mice at 10 mg/kg peroral dose1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID198611Inhibition of rolipram binding to rat brain tissue at 20 uM2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
AID425874Inhibition of PDE4C1 at 10 uM2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1623101Cognition enhancement activity in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as decrease in escape latancy at 4 mg/kg/day, ig administered for 26 consecutive days by Morris water maze test2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID157785Inhibition of recombinant human Phosphodiesterase 4B1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID1353615Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA2018European journal of medicinal chemistry, Mar-10, Volume: 147Phenylpyridine-2-ylguanidines and rigid mimetics as novel inhibitors of TNFα overproduction: Beneficial action in models of neuropathic pain and of acute lung inflammation.
AID418770Antiinflammatory activity in human neutrophils assessed as inhibition of LPS-induced intracellular TNFalpha expression at 10 ug/mL after 3 hrs by flow cytometry2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Semi-synthetic analogs of pinitol as potential inhibitors of TNF-alpha cytokine expression in human neutrophils.
AID425691Inhibition of PDE8A12009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID159793Inhibition of Phosphodiesterase 41996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
AID159961Inhibition of [3H]- rolipram binding to phosphodiesterase 4 of rat cerebral cortex membranes.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones.
AID425680Inhibition of PDE2A2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID349555Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IFN-gamma release after 24 hrs by FACSArray analysis2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID440708Inhibition of human recombinant PDE4D1 expressed in baculovirus system by radiometric assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID160103Inhibitory concentration against phosphodiesterase 4 (PDE4) from rat kidney2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
AID1480235Inhibition of recombinant human sEH using MNPC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
AID260841Inhibition of Eotaxin mediated by human eosinophil chemotaxis2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID160135Inhibition of phosphodiesterase 41998Bioorganic & medicinal chemistry letters, Oct-06, Volume: 8, Issue:19
Aryl sulfonamides as selective PDE4 inhibitors.
AID1420132Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate measured after 30 mins2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.
AID1261707Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 10 mins followed by AAPH challenge measured every min for 120 mins by ORAC-FL assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.
AID159067Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
AID1160998Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF assay2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Novel Roflumilast analogs as soft PDE4 inhibitors.
AID1370515Cytotoxicity against human A549 cells assessed as cell viability at 1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID363099Inhibition of human PDE4D4 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1593012Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by fluorescence polarization assay2019European journal of medicinal chemistry, Apr-15, Volume: 168Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.
AID473492Antiinflammatory activity in mouse assessed as inhibition of phorbol ester-induced ear edema at 3 mg/ear2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
AID1370514Cytotoxicity against human A549 cells assessed as cell viability at 0.1 uM by MTT assay relative to control2018Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
Identification of novel small-molecule inhibitors of Zika virus infection.
AID1743664Inhibition of human U-937 cells derived PDE4D using [3H] cAMP as substrate measured after 30 mins2020European journal of medicinal chemistry, Dec-01, Volume: 207Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.
AID1623076Inhibition of human PDE4D2 (86 to 413 residues) catalytic domain using [3H]-cAMP as substrate after 15 mins by liquid scintillation counting method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1543154Inhibition of PDE4D2 (unknown origin) by preincubated for 30 mins before substrate addition and measured after 60 mins by IMAP TR-FRET phosphodiesterase evaluation assay
AID159490Inhibition of Phosphodiesterase 31997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
AID349553Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
AID704144Antiinflammatory activity in A/J mouse assessed as inhibition of leukocyte accumulation in bronchoalveolar space at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID158465Evaluated in vitro for its inhibitory activity on human monocyte cytosol Phosphodiesterase type 4 (PDE4).1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
AID1427215Inhibition of human U937 cells-derived PDE4D using [3H]cAMP as substrate after 30 mins
AID704148Antiinflammatory activity in A/J mouse lung assessed as inhibition of LPS-induced TNFalpha production at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID425681Inhibition of PDE3A2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID75783In vivo bronchodilator effect on histamine-induced bronchospasm in anaesthetized guinea pigs at 50 ug intravenous dose1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1773166Induction of apoptosis in human A549 cells assessed as increase in necrotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.365%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID215076TNF-alpha production in PBMC by ELISA method1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha.
AID1421679Inhibition of recombinant human PDE7A using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.
AID1623112Cognition enhancement activity in amyloid beta (25 to 35 residues) induced C57BL/6J mouse model of Alzheimer's disease assessed as swimming time in effective region at 4 mg/kg/day, ig administered for 26 consecutive days by Morris water maze test (4.3 +/-2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1545627Inhibition of human recombinant full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells at 10'-5 M using cAMP as substrate incubated for 20 mins followed by substrate addition by luciferase assay relative to control2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
AID440711Selectivity ratio of Ki for human PDE4D1 to Ki for human PDE4D32009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.
AID260836Inhibition of release of LTE4 in human whole blood2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID650863Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
C-C bond formation at C-2 of a quinoline ring: synthesis of 2-(1H-indol-3-yl)quinoline-3-carbonitrile derivatives as a new class of PDE4 inhibitors.
AID425678Inhibition of PDE1B2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID1351564Inhibition of human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli strain BL21 using [3H]cAMP as substrate after 15 mins by liquid scintillation counter analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.
AID1480257Decrease in self-motivated exploration of LPS-induced Sprague-Dawley rat inflammatory pain model at 3 mg/kg administered via oral gavage measured after 1 hr by open field assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain.
AID1773137Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID766610Inhibition of Hartley guinea pig eosinophil PDE4 assessed as cAMP hydrolysis by two-step radioisotope method2013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors.
AID159214In vitro inhibition of Phosphodiesterase 3 activity from guinea pig cardiac ventricle1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID78148Inhibition of superoxide O2-generation from guinea pig peritoneal eosinophils1994Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
AID1727190Hepatoprotective activity in ConA-induced BALB/c hepatitis mouse model assessed as decrease in serum IL-6 level at 50 mg/kg, ip administration and measured after 8 hrs relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID159810Inhibition of cAMP hydrolysis by human Phosphodiesterase 41995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specifi
AID155790Inhibition of anti-CD3 induced IL-4 release by human peripheral blood mononuclear cells.1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID45803Inhibition of phosphodiesterase 4 from guinea pig lung1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
AID159648Displacement of [3H]- rolipram binding to guinea pig brain1999Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
AID260824Inhibition of PDE4B2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID260829Inhibition of PDE8B2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID662986Inhibition of rabbit corpus cavernosum PDE62012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of chalcones as potent and selective PDE5A1 inhibitors.
AID1177596Inhibition of human PDE4D2 catalytic domain (86 to 413 amino acids) expressed in Escherichia coli strain BL21 after 15 mins using [3H]-cAMP by liquid scintillation counting2014Journal of natural products, Aug-22, Volume: 77, Issue:8
Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi.
AID1727198Antiinflammatory activity in LPS-induced Wistar rat endotoxemia model assessed as decrease in plasma TNFalpha level at 5 mg/kg, ip measured after 1.5 hr2021European journal of medicinal chemistry, Jan-01, Volume: 209New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
AID702890Inhibition of Trypanosoma brucei recombinant TbrPDEB1 expressed in Sf21 insect cells assessed as reduction of [3H]-cAMP hydrolysis by scintillation proximity assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
AID157758Inhibition of rolipram binding to phosphodiesterase 42003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
AID110206Inhibition of LPS-induced TNF-alpha production in mice after 30 min peroral dose2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
AID77844Change in heart rate in guinea pigs after 1 mg/kg intravenous dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
AID363097Inhibition of human PDE4D3 in cytosolic fraction of lung2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID1703894Vasorelaxant activity in non-sensitized guinea pig-derived trachea assessed as decrease in CCh-induced tracheal tonic contraction in absence of functional epithelium treated with compound after contraction stabilised2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID425684Inhibition of PDE4B12009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
AID117193Evaluated for antiinflammatory activity in the TPA induced ear inflammation model at a dose 1 mg/kg (25 ug)2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
AID389802Inhibition of LPS-induced TNFalpha production in human PBMC2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.
AID155791Inhibition of anti-CD3 induced T-cell proliferation in human peripheral blood mononuclear cells.1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
AID159065Inhibition of cGMP hydrolysis by human Phosphodiesterase 21995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
AID152781Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Structure-activity relationships of quinazoline derivatives: dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation.
AID1231637Toxicity in mouse assessed as sedative effect by measuring reduction of total distance traveled at 10 mg/kg, po measured over 60 mins by open-field test2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
AID1381682Inhibition of human GST-tagged PDE7A expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.
AID1623077Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity at 10 to 20 uM preincubated for 10 mins followed by AAPH addition measured every minute for 120 mins by ORAC fluorescein assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1187755Inhibition of PDE4D2 (unknown origin) at 10 uM2014Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.
AID156982Inhibition of cAMP PDE from canine brain1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase.
AID662985Inhibition of bovine platelet PDE52012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of chalcones as potent and selective PDE5A1 inhibitors.
AID1773142Cell cycle arrest in human A549 cells assessed as G0/G1 phase at 500 nM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 79.14%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1783046Inhibition of TNF-alpha (unknown origin) at 0.1 uM relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221PdCl
AID1724983Effect on TNFalpha production in C57BL/6 mouse bone marrow derived Macrophage at 1 to 10 uM incubated for 30 mins by ELISA2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Synthesis and SAR Studies of 1
AID78168Eosinophil infiltration in passively-sensitized guinea pig at 30 mg/kg peroral dose 90 min prior to challenge2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
AID704134Antiinflammatory activity in A/J mouse assessed as inhibition of LPS-induced airway elastance provoked by methacholine at 45 umol/kg, po administered 1 hr prior to LPS-challenge measured after 18 hrs relative to vehicle-treated control2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
AID210147In vitro inhibition of TNF-alpha release from human peripheral blood monocytes2000Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
AID260840Inhibition of PAF mediated human eosinophil chemotaxis2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
AID1421678Inhibition of recombinant human PDE4B using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1797296Phosphodiesterase (PDE) Inhibition Assay from Article 10.1016/j.str.2004.10.004: \\Structural basis for the activity of drugs that inhibit phosphodiesterases.\\2004Structure (London, England : 1993), Dec, Volume: 12, Issue:12
Structural basis for the activity of drugs that inhibit phosphodiesterases.
AID1797212PDE Activity Assay from Article 10.1021/jm030603w: \\8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors.\\2005Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.
AID1799753Enzymatic Assay from Article 10.1074/jbc.M111.326777: \\Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.\\2012The Journal of biological chemistry, Apr-06, Volume: 287, Issue:15
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.
AID1799063PDE4 Enzyme Assay from Article 10.1021/jm8010993: \\Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.\\2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
AID1345234Human phosphodiesterase 4B (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))1997Biochemical and biophysical research communications, May-19, Volume: 234, Issue:2
Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
AID1345251Human phosphodiesterase 4A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))1997Biochemical and biophysical research communications, May-19, Volume: 234, Issue:2
Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
AID1345281Human phosphodiesterase 4C (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))1997Biochemical and biophysical research communications, May-19, Volume: 234, Issue:2
Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
AID1345239Human phosphodiesterase 4D (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))1997Biochemical and biophysical research communications, May-19, Volume: 234, Issue:2
Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,590)

TimeframeStudies, This Drug (%)All Drugs %
pre-199087 (5.47)18.7374
1990's494 (31.07)18.2507
2000's552 (34.72)29.6817
2010's380 (23.90)24.3611
2020's77 (4.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials17 (1.06%)5.53%
Reviews0 (0.00%)6.00%
Reviews38 (2.37%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies2 (0.12%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other26 (100.00%)84.16%
Other1,547 (96.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Antidepressant Effects on cAMP Specific Phosphodiesterase (PDE 4) in Depressed Patients[NCT00369798]Phase 1100 participants (Actual)Interventional2006-08-02Completed
PET Imaging of Phosphodiesterase-4 (PDE4) in Brain and Peripheral Organs of Mccune-Albright Syndrome[NCT02743377]Phase 1/Phase 216 participants (Actual)Interventional2018-04-04Completed
An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain PDE4 Engagement, Pharmacokinetics and Safety of Single Oral Doses of GSK356278, Using 11C-(R)-Rolipram as a PET Ligand(s)[NCT01602900]Phase 18 participants (Actual)Interventional2011-11-22Completed
Safety, Tolerability & Effects of Rolipram on Inflammatory Activity in the Central Nervous System in Multiple Sclerosis. A Phase II, Open Label Crossover Trial Using MRI as an Outcome Measure[NCT00011375]Phase 252 participants Interventional2001-02-28Completed
PET Whole Body Biodistribution and Test Retest Brain Imaging Studies Using a Phosphodiesterase 4 Inhibitor (R)-[11C]Rolipram[NCT00250172]Phase 126 participants (Actual)Interventional2005-10-31Completed
[11C]-(R)-Rolipram to Measure cAMP Signaling Before and After Ketamine[NCT05522673]Phase 135 participants (Anticipated)Interventional2023-02-08Enrolling by invitation
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

MAS Affected Bone SUV AUC(60-120min) - Blocked

To assess whether uptake in dysplastic bone reflects parent radioligand binding to the enzyme or merely accumulation of radiometabolites (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Subjects With McCune-Albright Syndrome (MAS)11.1

MAS Affected Bone SUV AUC(60-120min) - for Baseline and Blocked Subjects With MAS

Determine if PDE4 levels are different in areas of fibrous dysplasia as compared to unaffected bones in patients with MAS (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Subjects With McCune-Albright Syndrome (MAS)13.5

MAS Affected Bone SUV AUC(60-120min) at Baseline

To assess whether uptake in dysplastic bone reflects parent radioligand binding to the enzyme or merely accumulation of radiometabolites (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Subjects With McCune-Albright Syndrome (MAS)11.2

Normal Bone SUV AUC (60-120min) - for Healthy Controls

Determine if PDE4 levels are different in areas of fibrous dysplasia as compared to unaffected bones in patients with MAS (NCT02743377)
Timeframe: 120 minutes after the start of the scan

InterventionSUV x min (Mean)
Healthy Control4.2

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Bladder

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls. (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control575.1
Subjects With McCune-Albright Syndrome (MAS)650.8

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Heart

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls. (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control27.4
Subjects With McCune-Albright Syndrome (MAS)25.4

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Kidneys

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls. (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control63.3
Subjects With McCune-Albright Syndrome (MAS)80.4

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Liver

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control47.6
Subjects With McCune-Albright Syndrome (MAS)52.4

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Lungs

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control10.2
Subjects With McCune-Albright Syndrome (MAS)9.6

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) - Stomach

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control39.4
Subjects With McCune-Albright Syndrome (MAS)34.1

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) -Gallbladder

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls. (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control581.2
Subjects With McCune-Albright Syndrome (MAS)417.9

Standard UptakeValue (SUV) Area Under the Curve (AUC) (30-120min) -Spleen

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the periphery of patients with McCune-Albright Syndrome (MAS) compared to healthy controls (NCT02743377)
Timeframe: 120 minutes

InterventionSUV x min (Mean)
Healthy Control20.1
Subjects With McCune-Albright Syndrome (MAS)18.7

Whole Brain Total Distribution Volume (VT)

Determine if there is a difference in PDE4 levels (measured using [11C]rolipram) in the brain of patients with McCune-Albright Syndrome (MAS) compared to healthy controls (NCT02743377)
Timeframe: 90 minutes

InterventionmL x cm-3 (Mean)
Healthy Control0.67
Subjects With McCune-Albright Syndrome (MAS)0.52

Research Highlights

Safety/Toxicity (10)

ArticleYear
GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species.
The Journal of pharmacology and experimental therapeutics, Volume: 350, Issue: 1
2014
Evaluation of longevity enhancing compounds against transactive response DNA-binding protein-43 neuronal toxicity.
Neurobiology of aging, Volume: 34, Issue: 9
2013
Safety and efficacy of new 3,6-diaryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine analogs as potential phosphodiesterase-4 inhibitors in NIH-3T3 mouse fibroblastic cells.
Chemical biology & drug design, Volume: 78, Issue: 3
2011
Genistein, a competitive PDE1-4 inhibitor, may bind on high-affinity rolipram binding sites of brain cell membranes and then induce gastrointestinal adverse effects.
European journal of pharmacology, Sep-15, Volume: 643, Issue: 1
2010
Alterations of pre- and postsynaptic noradrenergic signaling in a rat model of adriamycin-induced cardiotoxicity.
Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology, Volume: 17, Issue: 2
2010
Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety.
Nature biotechnology, Volume: 28, Issue: 1
2010
Alpha2 adrenergic modulation of NMDA receptor function as a major mechanism of RGC protection in experimental glaucoma and retinal excitotoxicity.
Investigative ophthalmology & visual science, Volume: 49, Issue: 10
2008
Beneficial effects of rolipram in a quinolinic acid model of striatal excitotoxicity.
Neurobiology of disease, Volume: 25, Issue: 2
2007
The toxicity of repeated exposures to rolipram, a type IV phosphodiesterase inhibitor, in rats.
Pharmacology & toxicology, Volume: 78, Issue: 1
1996
PGE1 and prostacyclin suppression of NK-cell mediated cytotoxicity and its relation to cyclic AMP.
Medical biology, Volume: 61, Issue: 6
1983
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (14)

ArticleYear
Inhibition of phosphodiesterase-4 reverses the cognitive dysfunction and oxidative stress induced by Aβ25-35 in rats.
Metabolic brain disease, Volume: 31, Issue: 4
2016
Inhibition of phosphodiesterase-4 reverses memory deficits produced by Aβ25-35 or Aβ1-40 peptide in rats.
Psychopharmacology, Volume: 212, Issue: 2
2010
Systemic administration of rolipram increases medullary and spinal cAMP and activates a latent respiratory motor pathway after high cervical spinal cord injury.
The journal of spinal cord medicine, Volume: 32, Issue: 2
2009
Antidepressant- and anxiolytic-like effects of the phosphodiesterase-4 inhibitor rolipram on behavior depend on cyclic AMP response element binding protein-mediated neurogenesis in the hippocampus.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Volume: 34, Issue: 11
2009
Administration of phosphodiesterase inhibitors and an adenosine A1 receptor antagonist induces phrenic nerve recovery in high cervical spinal cord injured rats.
Experimental neurology, Volume: 210, Issue: 2
2008
The potential of PDE4 inhibitors in respiratory disease.
Current drug targets. Inflammation and allergy, Volume: 3, Issue: 3
2004
Effect of a novel anti-inflammatory compound, YM976, on antigen-induced eosinophil infiltration into the lungs in rats, mice, and ferrets.
The Journal of pharmacology and experimental therapeutics, Volume: 295, Issue: 3
2000
Differential effects of chronic administration of the antidepressants amitriptyline and rolipram on adenylyl cyclase activity.
Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology, Volume: 18, Issue: 1
1998
Effects of chronic caffeine administration on respiration and schedule-controlled behavior in rhesus monkeys.
The Journal of pharmacology and experimental therapeutics, Volume: 283, Issue: 1
1997
Chronic antidepressant administration increases the expression of cAMP response element binding protein (CREB) in rat hippocampus.
The Journal of neuroscience : the official journal of the Society for Neuroscience, Apr-01, Volume: 16, Issue: 7
1996
Antidepressants and endogenous opioid peptide systems.
Neuropeptides, Volume: 5, Issue: 4-6
1985
Chronic treatment with the potential antidepressant drug rolipram: the effect on the behavioural responses to adrenergic and dopaminergic receptor agonists with some biochemical correlates.
Journal of neural transmission, Volume: 64, Issue: 3-4
1985
Effect of long-term rolipram administration on the sensitivity of alpha 2-adrenoceptors in rat brain.
European journal of pharmacology, Mar-29, Volume: 148, Issue: 2
1988
The pharmacodynamic action of the cyclic AMP phosphodiesterase inhibitor rolipram on prolactin producing rat pituitary adenoma (GH4C1) cells.
Bioscience reports, Volume: 10, Issue: 4
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (8)

ArticleYear
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.
Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue: 13
2015
Regulation of alveolar fluid clearance and ENaC expression in lung by exogenous angiotensin II.
Respiratory physiology & neurobiology, Apr-15, Volume: 181, Issue: 1
2012
Phosphodiesterase 4 inhibition attenuates plasma volume loss and transvascular exchange in volume-expanded mice.
The Journal of physiology, Jan-15, Volume: 590, Issue: 2
2012
Phosphodiesterase 4 inhibition attenuates atrial natriuretic peptide-induced vascular hyperpermeability and loss of plasma volume.
The Journal of physiology, Jan-15, Volume: 589, Issue: Pt 2
2011
Dissociation of the PAF-receptor from NADPH oxidase and adenylate cyclase in human neutrophils results in accelerated influx and delayed clearance of cytosolic calcium.
British journal of pharmacology, Volume: 136, Issue: 1
2002
Pharmacokinetics of rolipram in the rhesus and cynomolgus monkeys, the rat and the rabbit. Studies on species differences.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 18, Issue: 5
1988
Pharmacokinetics of the antidepressant rolipram in healthy volunteers.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 19, Issue: 6
1989
Pharmacokinetics of (+)-rolipram and (-)-rolipram in healthy volunteers.
European journal of clinical pharmacology, Volume: 38, Issue: 1
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (10)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
The Journal of biological chemistry, 11-15, Volume: 294, Issue: 46
2019
Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.
European journal of medicinal chemistry, Apr-15, Volume: 168
2019
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Journal of medicinal chemistry, Jan-25, Volume: 50, Issue: 2
2007
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Journal of medicinal chemistry, Jun-29, Volume: 43, Issue: 13
2000
The regulation of lung liquid absorption by endogenous cAMP in postnatal sheep lungs perfused in situ.
The Journal of physiology, Sep-01, Volume: 511 ( Pt 2)
1998
Pharmacokinetics of rolipram in the rhesus and cynomolgus monkeys, the rat and the rabbit. Studies on species differences.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 18, Issue: 5
1988
Pharmacokinetics of the antidepressant rolipram in healthy volunteers.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 19, Issue: 6
1989
Pharmacokinetics of (+)-rolipram and (-)-rolipram in healthy volunteers.
European journal of clinical pharmacology, Volume: 38, Issue: 1
1990
In-vitro and in-vivo characterisation of two sustained release formulations for the antidepressant rolipram.
Arzneimittel-Forschung, Volume: 40, Issue: 11
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (38)

ArticleYear
Genetic Understanding of Stroke Treatment: Potential Role for Phosphodiesterase Inhibitors.
Advances in neurobiology, Volume: 17
2017
Reduction of alcohol drinking of alcohol-preferring (P) and high-alcohol drinking (HAD1) rats by targeting phosphodiesterase-4 (PDE4).
Psychopharmacology, Volume: 232, Issue: 13
2015
Rolipram improves renal perfusion and function during sepsis in the mouse.
The Journal of pharmacology and experimental therapeutics, Volume: 347, Issue: 2
2013
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Journal of medicinal chemistry, Oct-25, Volume: 55, Issue: 20
2012
Drug-eluting microfibrous patches for the local delivery of rolipram in spinal cord repair.
Journal of controlled release : official journal of the Controlled Release Society, Aug-10, Volume: 161, Issue: 3
2012
Effects of protein kinase A and G inhibitors on hippocampal cholinergic markers expressions in rolipram- and sildenafil-induced spatial memory improvement.
Pharmacology, biochemistry, and behavior, Volume: 101, Issue: 3
2012
Action of a Novel PDE4 inhibitor ZL-n-91 on lipopolysaccharide-induced acute lung injury.
International immunopharmacology, Volume: 10, Issue: 4
2010
Evidence that corticotropin-releasing hormone modulates myometrial contractility during human pregnancy.
Endocrinology, Volume: 150, Issue: 12
2009
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue: 17
2009
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue: 14
2008
Preclinical assessment of curcumin as a potential therapy for B-CLL.
American journal of hematology, Volume: 82, Issue: 1
2007
Synergistic effects of cAMP-dependent signalling pathways and IL-1 on IL-6 production by H19-7/IGF-IR neuronal cells.
Cellular signalling, Volume: 18, Issue: 10
2006
A novel mechanism for the modulation of luteinizing hormone receptor mRNA expression in the rat ovary.
Molecular and cellular endocrinology, Apr-15, Volume: 233, Issue: 1-2
2005
Comparison of PDE 4 inhibitors, rolipram and SB 207499 (ariflo), in a rat model of pulmonary neutrophilia.
Pulmonary pharmacology & therapeutics, Volume: 14, Issue: 2
2001
Effects of several glucocorticosteroids and PDE4 inhibitors on increases in total lung eosinophil peroxidase (EPO) levels following either systemic or intratracheal administration in sephadex- or ovalbumin-induced inflammatory models.
Inflammation, Volume: 24, Issue: 4
2000
Cereport (RMP-7) increases the permeability of human brain microvascular endothelial cell monolayers.
Pharmaceutical research, Volume: 16, Issue: 9
1999
Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret.
Neuropharmacology, Volume: 38, Issue: 2
1999
Age-related effects of rolipram on [3H]quinuclidinyl benzilate and [3H]phorbol 12,13-dibutyrate binding in the rat brain.
The Tohoku journal of experimental medicine, Volume: 185, Issue: 2
1998
Rolipram and its optical isomers, phosphodiesterase 4 inhibitors, attenuated the scopolamine-induced impairments of learning and memory in rats.
Japanese journal of pharmacology, Volume: 75, Issue: 3
1997
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.
Journal of medicinal chemistry, Sep-26, Volume: 40, Issue: 20
1997
Pure glucagon antagonists: biological activities and cAMP accumulation using phosphodiesterase inhibitors.
Peptides, Volume: 18, Issue: 5
1997
Effects of inhibitors of phosphodiesterase, on antigen-induced bronchial hyperreactivity in conscious sensitized guinea-pigs and airway leukocyte infiltration.
British journal of pharmacology, Volume: 120, Issue: 2
1997
Phosphodiesterase specific inhibitors control cell growth of a human neuroepithelioma cell line.
Journal of neuro-oncology, Volume: 31, Issue: 1-2
1997
The human cyclic AMP-specific phosphodiesterase PDE-46 (HSPDE4A4B) expressed in transfected COS7 cells occurs as both particulate and cytosolic species that exhibit distinct kinetics of inhibition by the antidepressant rolipram.
The Journal of biological chemistry, Dec-06, Volume: 271, Issue: 49
1996
Inhibition of bronchospasm and ozone-induced airway hyperresponsiveness in the guinea-pig by CDP840, a novel phosphodiesterase type 4 inhibitor.
British journal of pharmacology, Volume: 118, Issue: 5
1996
Effects of theophylline and rolipram on antigen-induced airway responses in neonatally immunized rabbits.
British journal of pharmacology, Volume: 117, Issue: 7
1996
Effects of adenosine agonists on ventilation during hypercapnia, hypoxia and hyperoxia in rhesus monkeys.
The Journal of pharmacology and experimental therapeutics, Volume: 265, Issue: 2
1993
Pulmonary antiallergic and bronchodilator effects of isozyme-selective phosphodiesterase inhibitors in guinea pigs.
The Journal of pharmacology and experimental therapeutics, Volume: 264, Issue: 2
1993
cAMP-specific phosphodiesterase inhibitor, rolipram, reduces eosinophil infiltration evoked by leukotrienes or by histamine in guinea pig conjunctiva.
Inflammation, Volume: 17, Issue: 1
1993
Reversal of pulmonary capillary ischemia-reperfusion injury by rolipram, a cAMP phosphodiesterase inhibitor.
Journal of applied physiology (Bethesda, Md. : 1985), Volume: 77, Issue: 2
1994
Phosphodiesterase inhibitors reduce bronchial hyperreactivity and airway inflammation in unrestrained guinea pigs.
European journal of pharmacology, Feb-24, Volume: 275, Issue: 1
1995
Species differences in behavioural effects of rolipram and other adenosine cyclic 3H, 5H-monophosphate phosphodiesterase inhibitors.
Journal of neural transmission, Volume: 56, Issue: 2-3
1983
Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors.
Psychopharmacology, Volume: 77, Issue: 4
1982
A study to assess the anticholinergic activity of rolipram in healthy elderly volunteers.
Pharmacopsychiatry, Volume: 21, Issue: 5
1988
The effect of a selective phosphodiesterase inhibitor, rolipram, on muricide in olfactory bulbectomized rats.
Japanese journal of pharmacology, Volume: 48, Issue: 3
1988
Effect of long-term rolipram administration on the sensitivity of alpha 2-adrenoceptors in rat brain.
European journal of pharmacology, Mar-29, Volume: 148, Issue: 2
1988
In-vitro and in-vivo characterisation of two sustained release formulations for the antidepressant rolipram.
Arzneimittel-Forschung, Volume: 40, Issue: 11
1990
A multicenter double-blind study of three different doses of the new cAMP-phosphodiesterase inhibitor rolipram in patients with major depressive disorder.
Neuropsychobiology, Volume: 26, Issue: 1-2
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Interactions (4)

ArticleYear
Ibudilast, a phosphodiesterase inhibitor, in combination with low-dose aspirin potently inhibits guinea pig carotid artery thrombosis without extending bleeding time and causing gastric mucosal injury.
Arzneimittel-Forschung, Volume: 62, Issue: 12
2012
Uterus-relaxing effect of β2-agonists in combination with phosphodiesterase inhibitors: studies on pregnant rat in vivo and on pregnant human myometrium in vitro.
The journal of obstetrics and gynaecology research, Volume: 39, Issue: 1
2013
The specific type IV phosphodiesterase inhibitor rolipram combined with adenosine reduces tumor necrosis factor-alpha-primed neutrophil oxidative activity.
International journal of immunopharmacology, Volume: 17, Issue: 10
1995
The inotropic mechanism of the phosphodiesterase inhibitor OPC 3911 alone and in combination with rolipram, studied in papillary muscles of ferret and guinea-pig and isolated myocytes of guinea-pig ventricular muscle.
Acta physiologica Scandinavica, Volume: 150, Issue: 3
1994
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]