Page last updated: 2024-09-26

cilomilast

Cross-References

ID SourceID
PubMed CID151170
CHEMBL ID511115
CHEMBL ID32854
CHEMBL ID27220
CHEBI ID94683
SCHEMBL ID26372
SCHEMBL ID27516
SCHEMBL ID27515
SCHEMBL ID13777301
MeSH IDM0396210

Synonyms (99)

Synonym
HY-10790
sb-207499
ariflo
cis-4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexanecarboxylic acid
cyclohexanecarboxylic acid, 4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)-, cis-
sb 207499
cilomilast [usan:inn]
cis-4-(3-(cyclopentyloxy)-4-methoxyphenyl)-4-cyanocyclohexane-1-carboxylic acid
PDSP2_001271
PDSP1_001287
DB03849
1XOM
1XLX
cis-4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
ariflo (tn)
cilomilast ,
CIO ,
153259-65-5
cilomilast (jan/usan/inn)
D01704
cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
NCGC00167520-01
4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid
sb207499
bdbm14773
4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)cyclohexane-1-carboxylic acid
4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylic acid
CHEMBL511115 ,
FT-0665037
4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-1-cyclohexanecarboxylic acid
A809409
unii-8atb1c1r6x
8atb1c1r6x ,
dtxsid6046686 ,
cas-153259-65-5
dtxcid4026686
tox21_112517
CHEMBL32854
CHEMBL27220
4-cyano-3-cyclopentyloxy-4-(4-methoxy-phenyl)-cyclohexanecarboxylic acid
4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)-cyclohexanecarboxylic acid methyl ester
6-(3,4-dimethoxy-phenyl)-5-methyl-4,5-dihydro-2h-pyridazin-3-one
4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)-cyclohexanecarboxylic acid
bdbm50346088
4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)-cyclohexanecarboxylic acid (ariflo)
(1r,4r)-4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)-cyclohexanecarboxylic acid(ariflo)
BCP9000529
AKOS015967197
BCPP000280
NCGC00167520-03
CS-0470
S1455
BRD-K62982419-001-01-2
gtpl7407
(1s,4s)-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid
SCHEMBL26372
SCHEMBL27516
SCHEMBL27515
cilomilast [mart.]
cilomilast [who-dd]
cilomilast [usan]
cilomilast [inn]
cilomilast [jan]
cilomilast [mi]
cilomilast [vandf]
SCHEMBL13777301
4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
164414-71-5
cilomilast (sb-207499)
J-520044
trans-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
153259-69-9
AKOS030526103
(1r,4r)-4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexane-1-carboxylic acid
CHEBI:94683
HMS3654F10
J-008995
NCGC00485415-01
SW219280-1
CS-B1491
Q5120034
cilomilast, sb 207499, ariflo
EX-A1554
BCP02394
CS-15164
SB19573
HMS3884K17
CCG-267954
NCGC00167520-06
AT10133
C13118
MS-25260
cyclohexanecarboxylic acid,4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, trans-
GLXC-25763
NCGC00390705-01
DTXSID40861410
trans-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylicacid
AKOS040759016

Research Excerpts

Overview

ExcerptReference
"Cilomilast is a phosphodiesterase 4 (PDE4) inhibitor for treating inflammatory lung diseases. "( Elzoghby, AO; Fang, JY; Hwang, TL; Lin, CY; Liu, FC; Yu, HP, 2018)
"Cilomilast is an orally active, potent, and selective inhibitor of PDE-4. "( Amit, O; Rennard, SI; Rickard, K; Schachter, N; Strek, M, 2006)
"Cilomilast is a systemically available, second-generation, selective PDE IV inhibitor."( Daley-Yates, P; Down, G; Lim, S; Siederer, S, 2006)
"Cilomilast is a systemically available, second- generation, selective phosphodiesterase-4 inhibitor."( Schachter, EN, 2006)
"Cilomilast is a second-generation PDE4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with chronic obstructive pulmonary disease (COPD). "( Ismail, MS; Martina, SD; Vesta, KS, 2006)
"Cilomilast is an orally active, selective phosphodiesterase 4 inhibitor currently in clinical development for the treatment of chronic obstructive pulmonary disease."( Clark, DJ; Collie, H; Kelly, J; Murdoch, RD; Schubert, C; Zussman, BD, 2001)
"Cilomilast is an orally active, potent, selective phosphodiesterase type 4 inhibitor, which in vitro can affect cells thought to be of clinical importance in COPD."( Amit, O; Ayres, JG; Bakst, A; Barnes, NC; Brambilla, C; Compton, CH; Creemers, JP; Edelson, J; Gubb, J; Nieman, R; Schultze-Werninghaus, G, 2001)

Effects

ExcerptReference
"Cilomilast has been shown to exert potent anti-inflammatory effects both in vitro and in vivo."( Foerster, M; Kroegel, C, 2007)
"Cilomilast has been evaluated in Phase I, Phase II and Phase III trials and dose-response experiments have demonstrated a clinically significant increase in lung function and a perceived improvement in quality of life in patients with COPD."( Giembycz, MA, 2001)

Treatment

ExcerptReference
"Cilomilast treatment markedly decreased the presence of CD11b+ antigen-presenting cells in the central and peripheral cornea (P ≤ 0.05), and led to decreased conjunctival expression of cytokines IL-6, IL-23, and IL-17 (P ≤ 0.05)."( Amparo, F; Chauhan, SK; Chen, Y; Dana, R; Dohlman, TH; Hua, J; Okanobo, A; Sadrai, Z; Stevenson, W, 2012)

Drug Classes (1)

ClassDescription
methoxybenzenesAny aromatic ether that consists of a benzene skeleton substituted with one or more methoxy groups.
[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]

Protein Targets (47)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency14.12540.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency18.83750.000811.382244.6684AID686979
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.84930.000229.305416,493.5996AID743079
GVesicular stomatitis virusPotency10.68400.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency33.78580.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency10.68400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency1.18830.002319.595674.0614AID651631
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency10.00000.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
[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 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain B, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.01800.00001.947220.0000AID977608
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)46.91970.00001.77679.2000AID159063; AID1797296
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)IC50 (µMol)50.27600.00001.85239.2000AID1797296
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)46.91970.00001.18439.6140AID157955; AID1797296
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)IC50 (µMol)10.08480.00032.723210.0000AID158407; AID159964; AID195536; AID219415
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)IC50 (µMol)10.08480.00032.723210.0000AID158407; AID159964; AID195536; AID219415
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)IC50 (µMol)8.12980.00032.663810.0000AID157915; AID158407; AID159964; AID195536; AID219415
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)0.31130.00001.068010.0000AID155682; AID157302; AID157303; AID157775; AID157777; AID157778; AID157780; AID158466; AID159656; AID159783; AID159789; AID159796; AID159799; AID159934; AID159935; AID159936; AID1703915; AID1720007; AID240760; AID275702; AID759595
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki0.03800.00041.43528.7600AID159663; AID159806
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)0.06200.00030.81978.4900AID759595
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)IC50 (µMol)10.08480.00032.723210.0000AID158407; AID159964; AID195536; AID219415
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC50 (µMol)10.00000.23002.510510.0000AID158893
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50 (µMol)46.91970.00002.14179.2000AID158893; AID1797296
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)14.36750.00001.104010.0000AID1060995; AID1060996; AID155682; AID157302; AID157303; AID157912; AID158466; AID159656; AID159783; AID159789; AID159796; AID159799; AID159934; AID159935; AID159936; AID1625374; AID1703916; AID1720007; AID1797296; AID1895842; AID225256; AID240760; AID275701; AID462321; AID600390; AID647425
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki0.03800.00041.16418.7600AID159663; AID159806
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)0.81800.00001.465110.0000AID155682; AID157302; AID157303; AID157918; AID157919; AID158466; AID159656; AID159783; AID159789; AID159796; AID159799; AID159934; AID159935; AID159936; AID1703917; AID1720007; AID240760; AID275703
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki0.03800.00040.12471.0000AID159663; AID159806
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)14.73490.00001.146310.0000AID155682; AID157302; AID157303; AID157922; AID157923; AID158466; AID159656; AID159783; AID159789; AID159796; AID159799; AID1598959; AID159934; AID159935; AID159936; AID1619495; AID1625378; AID1703907; AID1703918; AID1720007; AID1797296; AID240760; AID275704; AID462320; AID600391
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki0.03800.00041.52938.7600AID159663; AID159806
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)41.15700.00002.072410.0000AID157297; AID159345; AID159363; AID1797296
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC50 (µMol)10.00000.23001.98149.0000AID158893
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)7.72080.00031.990110.0000AID157297; AID159345; AID159363
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.12000.00040.16800.9772AID1060996
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)IC50 (µMol)50.27600.00001.97009.2000AID1797296
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)IC50 (µMol)50.27600.00002.05139.2000AID1797296
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC50 (µMol)50.27600.00001.49049.2000AID1797296
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (250)

Processvia Protein(s)Taxonomy
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)
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)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo 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)
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-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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo 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 (79)

Processvia Protein(s)Taxonomy
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)
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)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo 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)
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 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 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo 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 (58)

Processvia Protein(s)Taxonomy
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)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo 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)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
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)
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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo 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 (219)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary 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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID159363Inhibition of dual cGMP-inhibited phosphodiesterase 3 (PDE3) was determined in homogenates from human platelets.2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
AID363125Selectivity for PDE4D over PDE4C2008Journal 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.
AID159799Inhibition of [3H]rolipram binding in human peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID157923Inhibition of human Phosphodiesterase 4D from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID600499Toxicity in ferret assessed as induction of emesis at 10 mg/kg, po measured 6 hrs post dose2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID1703901Antiinflammatory activity against A/J mouse assessed as decrease in LPS-induced TNFalpha production in lungs at 3 umol/kg, po treated via gavage for 1 hr before LPS stimulation and measured after 24 hrs by ELISA relative to control2020European 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.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID131014Reversal of reserpine-induced hypothermia in the 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.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID76864Percent inhibition of eosinophil infiltration in the guinea pig at 30 uM/kg (ip)2001Bioorganic & 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.
AID363124Selectivity for PDE4D over PDE4B2008Journal 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.
AID133070Percent inhibition of arachidonic acid (AA) formation, induced mouse ear edema after pretreatment at a concentration of 30 umol/kg (po)2002Journal 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.
AID160115Inhibition of phosphodiesterase 4 from rat liver at 10 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.
AID157780Inhibition of human Phosphodiesterase 4A from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
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.
AID139980Inhibition of arachidonic acid (AA)-induced mouse ear edema after pretreatment with compound (1 h before AA) at a drug concentration of 30 umol/kg po.2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
AID600390Inhibition of human PDE4B1 incubated for 10 mins using cAMP and [3H]cAMP substrates2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID157919Inhibition of human Phosphodiesterase 4C from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID1703910Inhibition of human recombinant PDE4B1 using FAM-cAMP as substrate at 10 uM measured after 1 hr by IMAP TR-FRET assay2020European 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.
AID92877Inhibition of LPS-induced TNF-alpha formation in human whole blood.2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID1187901Antiparasitic activity against Trypanosoma brucei after 22 to 24 hrs by Alamar blue cell viability assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.
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.
AID218768Emetic effect in dogs by intravenous 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.
AID210149In vitro inhibition of TNF-alpha-release from human peripheral blood monocytes (not tested)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.
AID43769In vivo inhibition of antigen induced eosinophil recruitment in Brown-Norvway Rats at 10 mg/kg peroral dose (non-significant)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.
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.
AID1703911Inhibition of human recombinant PDE4D3 using FAM-cAMP as substrate at 10 uM measured after 1 hr by IMAP TR-FRET assay2020European 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.
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.
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.
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.
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.
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.
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.
AID157955Inhibition of human Phosphodiesterase 5 from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID13016In vitro metabolic stability in rat hepatocytes2001Bioorganic & 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.
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.
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.
AID759552Toxicity in po 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.
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.
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.
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.
AID72534PDE4-related emetic activity in ferrets after intravenous administration at 10 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.
AID155665Inhibition of Phosphodiesterase 3 (PDE3) from dog aorta (not tested)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.
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.
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.
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.
AID133068Percent 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.
AID76974Inhibition of SRS-A-mediated bronchoconstriction and airway microvascular leakage in sensitized guinea pigs at 0.15 mg/kg peroral dose 1 hr prio to challenge2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Orally active PDE4 inhibitors with therapeutic potential.
AID1703892Inhibition of human recombinant PDE4A1A using FAM-cAMP as substrate measured after 1 hr by IMAP TR-FRET assay relative to control2020European 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.
AID704140Antiinflammatory activity in A/J mouse assessed as inhibition of neutrophil accumulation in bronchoalveolar space at 3 mg/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.
AID1703898Antiinflammatory activity against A/J mouse assessed as decrease in LPS-induced airway hyperreactivity at 3 umol/kg, po treated via gavage for 1 hr before LPS stimulation measured after 24 hrs by whole body plethysmography relative to control2020European 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.
AID159934inhibition of cAMP-specific phosphodiesterase 4 (PDE4) was determined in cytosol from human neutrophils2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
AID157303Inhibition of PDE4 in the cytosol of human neutrophils2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
AID196728EPO activity for activation of eosinophil cells in BALF from actively sensitized Brown norway rats2000Journal 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.
AID16446Calculated partition coefficient (clogP)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Highly potent PDE4 inhibitors with therapeutic potential.
AID16446Calculated partition coefficient (clogP)2004Bioorganic & medicinal chemistry, Sep-01, Volume: 12, Issue:17
Highly potent PDE4 inhibitors with therapeutic potential.
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.
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.
AID181500Increased acid secretion in the isolated whole rat stomach2001Bioorganic & 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.
AID76856Inhibition of SRS-A-mediated bronchoconstriction and airway microvascular leakage in sensitized guinea pigs at 0.15 mg/kg 1 hr after oral dose2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Highly potent PDE4 inhibitors with therapeutic potential.
AID76856Inhibition of SRS-A-mediated bronchoconstriction and airway microvascular leakage in sensitized guinea pigs at 0.15 mg/kg 1 hr after oral dose2004Bioorganic & medicinal chemistry, Sep-01, Volume: 12, Issue:17
Highly potent PDE4 inhibitors with therapeutic potential.
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.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID160116In vitro inhibitory activity against phosphodiesterase 4 from rat liver at concentration of 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.
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.
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.
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.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1703888Drug absorption of the compound incubated for 8 hrs by PAMPA-TGI assay2020European 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.
AID182977Inhibition of gastric emptying in rats after peroral administration2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Highly potent PDE4 inhibitors with therapeutic potential.
AID182977Inhibition of gastric emptying in rats after peroral administration2004Bioorganic & medicinal chemistry, Sep-01, Volume: 12, Issue:17
Highly potent PDE4 inhibitors with therapeutic potential.
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.
AID92882Inhibition of LPS induced TNF-alpha production in human whole blood2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Orally active PDE4 inhibitors with therapeutic potential.
AID600408Inhibition of neutropenia in ferret assessed as inhibition of LPS-induced change in number of neutrophils in lung lavage at 10 mg/kg, po2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID43767Percent inhibition of protein concentration in bronchoalveolar lavage fluid (BALF) from actively sensitized Brown norway rats at 2 mg/kg2000Journal 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.
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.
AID462321Inhibition of human PDE4B2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
AID72236Emetic effect in fasted ferrets at 10 mg/kg peroral dose (n=2 not tested)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID92858Inhibition of LPS-induced TNF-alpha production in human whole blood2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Highly potent PDE4 inhibitors with therapeutic potential.
AID92858Inhibition of LPS-induced TNF-alpha production in human whole blood2004Bioorganic & medicinal chemistry, Sep-01, Volume: 12, Issue:17
Highly potent PDE4 inhibitors with therapeutic potential.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID363081Inhibition of PDE42008Journal 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.
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.
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.
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.
AID600411Toxicity in ferret assessed as induction of emesis at 0.3 mg/kg, po measured 6 hrs post dose2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID78020In vivo inhibition of slow reacting substance of anaphylaxis (SRS-A) mediated bronchoconstriction in guinea pig2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID647420Inhibition of PDE42012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
AID1703906Inhibition of human recombinant PDE4C using FAM-cAMP as substrate at 10 uM measured after 1 hr by IMAP TR-FRET assay2020European 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.
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.
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.
AID1703890Inhibition of human recombinant PDE4D3 using FAM-cAMP as substrate measured after 1 hr by IMAP TR-FRET assay relative to control2020European 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.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID157912Inhibition of human Phosphodiesterase 4B from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
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.
AID222153Inhibition of fMLP-induced oxidative burst in human eosinophils (no data)2000Journal 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.
AID363105Inhibition of TNFalpha release in human whole blood2008Journal 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.
AID157778Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells.2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID155463Inhibition of TNF-alpha release from human peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID600407Inhibition of LPS-induced TNFalpha production in po dosed mouse2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID196730Percent inhibition of eosinophil activation in BALF from actively sensitized Brown norway rats at 2 mg/kg2000Journal 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.
AID1895842Inhibition of human recombinant PDE4B by liquid scintillation counter method2021European journal of medicinal chemistry, Dec-15, Volume: 226Zinc enzymes in medicinal chemistry.
AID158407Inhibition of [3H]-Rolipram binding to rat brain membranes2000Journal 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.
AID240760Inhibition 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.
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.
AID13399Oral bioavailability in rat2001Bioorganic & 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.
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.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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.
AID72367Emetic effect in fasted ferrets at 30 mg/kg peroral dose (n=2 not tested)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID158922Inhibition of Phosphodiesterase 1/5 (PDE1/5) from guinea pig trachea (not tested)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.
AID1703907Inhibition of human recombinant PDE4D3 using FAM-cAMP as substrate measured after 1 hr by IMAP TR-FRET assay2020European 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.
AID215253Inhibition of lipopolysaccharide-induced tumor necrosis factor alpha production in rats by peroral administration2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID222470Inhibition 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.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID182978Inhibition of gastric emptying in rats2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Orally active PDE4 inhibitors with therapeutic potential.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID159063Inhibition of human Phosphodiesterase 2 from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
AID704132Antiinflammatory activity in A/J mouse assessed as inhibition of LPS-induced airway elastance provoked by methacholine at 3 mg/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.
AID704135Antiinflammatory activity in A/J mouse assessed as inhibition of LPS-induced airway resistance provoked by methacholine at 3 mg/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.
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.
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.
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.
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.
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.
AID158893Inhibition of human Phosphodiesterase 1 from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
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.
AID92733Inhibition of TNF-alpha production in human whole blood2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID600391Inhibition of human PDE4D3 incubated for 10 mins using cAMP and [3H]cAMP substrates2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID1187900Cytotoxicity against mouse NIH/3T3 cells by Alamar blue cell viability assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.
AID363011Inhibition of human PDE4 at 0.075 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.
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.
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.
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.
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.
AID72239Emetic effect in fasted ferrets at 3 mg/kg peroral dose (n=2 not tested)2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
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.
AID92871Inhibitory concentration of compound against LPS- induced TNF-alpha production in whole human blood assay2002Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID600392Selectivity ratio, ratio of IC50 for human PDE4D3 to IC50 for human PDE4B12009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID183115Inhibition of LPS-induced TNF-alpha production in rats 0.5 hr after oral dose2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Orally active PDE4 inhibitors with therapeutic potential.
AID157777Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells2002Bioorganic & medicinal chemistry letters, Jun-03, Volume: 12, Issue:11
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
AID600406Inhibition of LPS-induced TNFalpha production in mouse PBMCs2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID1703909Inhibition of human recombinant PDE4A1A using FAM-cAMP as substrate at 10 uM measured after 1 hr by IMAP TR-FRET assay2020European 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.
AID1187897Inhibition of Trypanosoma brucei recombinant PDEB1 pre-incubated for 5 mins prior to substrate addition2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.
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.
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.
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.
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.
AID182640Inhibition of gastric emptying in rats by peroral dose2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
New orally active PDE4 inhibitors with therapeutic potential.
AID182970Inhibition of LPS-induced TNF-alpha production in rats 0.5 hr after peroral administration2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
Highly potent PDE4 inhibitors with therapeutic potential.
AID182970Inhibition of LPS-induced TNF-alpha production in rats 0.5 hr after peroral administration2004Bioorganic & medicinal chemistry, Sep-01, Volume: 12, Issue:17
Highly potent PDE4 inhibitors with therapeutic potential.
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.
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.
AID1187899Selectivity index, ratio of IC50 for Trypanosoma brucei recombinant PDEB1 to IC50 for human PDE4B2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID1060995Inhibition of PDE4B2 (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.
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.
AID195021Percent inhibition of T-lymphocyte activation in BALF from actively sensitized Brown norway rats at 2 mg/kg2000Journal 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.
AID600412Toxicity in ferret assessed as induction of emesis at 1 mg/kg, po measured 6 hrs post dose2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Discovery of selective PDE4B inhibitors.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID759557Inhibition of LPS-induced neutrophilia in ferret COPD model BAL-fluid at 10 mg/kg, po2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
AID1703889Permeability of the compound incubated for 8 hrs by PAMPA-TGI assay2020European 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.
AID195593Percent inhibition of neutrophil activation in BALF from actively sensitized Brown norway rats at 2 mg/kg2000Journal 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.
AID220554Emetic effect in dog on intravenous administration2001Bioorganic & 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.
AID363121Selectivity for PDE4D over PDE4A2008Journal 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.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID222151Inhibition of fMLP-induced oxidative burst in human eosinophils (no data)2000Journal 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.
AID1720007Inhibition of PDE4 (unknown origin)2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Advances in the Development of Phosphodiesterase-4 Inhibitors.
AID363126Inhibition of gastric emptying in po dosed rat2008Journal 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.
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.
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.
AID1703904Inhibition of human recombinant PDE4A1A using FAM-cAMP as substrate measured after 1 hr by IMAP TR-FRET assay2020European 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.
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.
AID159789Inhibition of PDE4 from U937 monocytic cells2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Orally active PDE4 inhibitors with therapeutic potential.
AID159345Inhibition of human Phosphodiesterase 3 from peripheral blood mononuclear cells2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine 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.
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.
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.
AID1187896Inhibition of Trypanosoma brucei recombinant PDEB1 at 10 uM pre-incubated for 5 mins prior to substrate addition2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Repurposing human PDE4 inhibitors for neglected tropical diseases: design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2004Structure (London, England : 1993), Dec, Volume: 12, Issue:12
Structural basis for the activity of drugs that inhibit phosphodiesterases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (160)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (4.38)18.2507
2000's105 (65.63)29.6817
2010's36 (22.50)24.3611
2020's12 (7.50)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 (%)
Trials13 (8.02%)5.53%
Reviews35 (21.60%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other114 (70.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, 24-week, Double-blind, Placebo-controlled, Parallel-group Study to Evaluate the Efficacy, Safety and Tolerability of ARIFLO® (15mg BID) in Patients With Chronic Obstructive Pulmonary Disease (COPD)[NCT00103922]Phase 3600 participants (Actual)Interventional2004-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Research Highlights

Safety/Toxicity (1)

ArticleYear
The efficacy and safety of cilomilast in COPD.
Drugs, Volume: 68 Suppl 2
2008
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (7)

ArticleYear
Physicochemical determinants of human renal clearance.
Journal of medicinal chemistry, Aug-13, Volume: 52, Issue: 15
2009
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Drug metabolism and disposition: the biological fate of chemicals, Volume: 36, Issue: 7
2008
Lack of pharmacokinetic interactions between cilomilast and theophylline or smoking in healthy volunteers.
Journal of clinical pharmacology, Volume: 44, Issue: 9
2004
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue: 20
2002
Warfarin pharmacodynamics unaffected by cilomilast.
The Annals of pharmacotherapy, Volume: 35, Issue: 12
2001
An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers.
Journal of clinical pharmacology, Volume: 41, Issue: 9
2001
Cilomilast: pharmacokinetic and pharmacodynamic interactions with digoxin.
Clinical therapeutics, Volume: 23, Issue: 6
2001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (6)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Journal of medicinal chemistry, Feb-11, Volume: 53, Issue: 3
2010
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
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue: 20
2002
An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers.
Journal of clinical pharmacology, Volume: 41, Issue: 9
2001
Bioavailability of the oral selective phosphodiesterase 4 inhibitor cilomilast.
Pharmacotherapy, Volume: 21, Issue: 6
2001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (7)

ArticleYear
Evaluation of oral corticosteroids and phosphodiesterase-4 inhibitor on the acute inflammation induced by inhaled lipopolysaccharide in human.
Pulmonary pharmacology & therapeutics, Volume: 20, Issue: 6
2007
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
Journal of medicinal chemistry, May-08, Volume: 46, Issue: 10
2003
Cilomilast: a second generation phosphodiesterase 4 inhibitor for asthma and chronic obstructive pulmonary disease.
Expert opinion on investigational drugs, Volume: 10, Issue: 7
2001
An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers.
Journal of clinical pharmacology, Volume: 41, Issue: 9
2001
Cilomilast: pharmacokinetic and pharmacodynamic interactions with digoxin.
Clinical therapeutics, Volume: 23, Issue: 6
2001
Bioavailability of the oral selective phosphodiesterase 4 inhibitor cilomilast.
Pharmacotherapy, Volume: 21, Issue: 6
2001
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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]