Information on EC 3.1.4.53 - 3',5'-cyclic-AMP phosphodiesterase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
3.1.4.53
-
RECOMMENDED NAME
GeneOntology No.
3',5'-cyclic-AMP phosphodiesterase
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
adenosine 3',5'-cyclic phosphate + H2O = AMP
show the reaction diagram
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Purine metabolism
-
-
SYSTEMATIC NAME
IUBMB Comments
3',5'-cyclic-AMP 5'-nucleotidohydrolase
Requires Mg2+ or Mn2+ for activity [2]. This enzyme is specific for 3',5'-cAMP and does not hydrolyse other nucleoside 3',5'-cyclic phosphates such as cGMP (cf. EC 3.1.4.17, 3,5-cyclic-nucleotide phosphodiesterase and EC 3.1.4.35, 3,5-cyclic-GMP phosphodiesterase). It is involved in modulation of the levels of cAMP, which is a mediator in the processes of cell transformation and proliferation [3].
CAS REGISTRY NUMBER
COMMENTARY hide
9036-21-9
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
plasmodium stage
-
-
Manually annotated by BRENDA team
gene cpdA; strain PAK
UniProt
Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
additional information
-
PDE4 is a cAMP-specific PDE which has four subfamilies, A thru D, that include over 50 isoforms
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2'-O-(N-methylanthraniloyl)adenosine-3',5'-cyclic monophosphate + H2O
2'-O-(N-methylanthraniloyl)adenosine-5'-monophosphate
show the reaction diagram
fluorescent cAMP analogue
-
-
?
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
3',5'-cAMP + H2O
adenosine 5'-phosphate
show the reaction diagram
3',5'-cGMP + H2O
5'-AMP
show the reaction diagram
-
low activity
-
-
?
3',5'-cGMP + H2O
5'-GMP
show the reaction diagram
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
show the reaction diagram
cAMP + H2O
5'-AMP
show the reaction diagram
cAMP + H2O
AMP
show the reaction diagram
-
-
-
?
cGMP + H2O
5'-GMP
show the reaction diagram
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
show the reaction diagram
-
-
-
?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Fe2+
Fe2+ is required for enzyme activity. The catalytic mechanism for CpdA utilizes a Fe3+-Fe2+ center. Addition of 0.01 mM FeCl2, as a source of Fe2+, results in an 2fold stimulation of CpdA activity; iron and conserved residues are essential for CpdA activity
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.1195 mM, PDE7
(2E)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
-
IC50: 0.31 mM, PDE4
(2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
IC50: 0.00043 mM, PDE4
(4aS,8aR)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
(R)-rolipram
-
-
1,10-phenanthroline
-
0.3 mM, more than 95% inhibition
1-(2,4-dichlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
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-
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
10-(3-pyrrolidin-1-ylpropyl)-2-(trifluoromethyl)-10H-phenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-trifluoromethylphenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-trifluoromethylphenoxazine
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-
10-(4'-N-pyrrolidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
-
increase of Km value in presence of inhibitor
10-[3'-[(beta-hydroxyethyl)-piperazino]propyl]-2-trifluoromethylphenoxazine
-
-
10-[30-[(beta-hydroxy ethyl)-piperazino]propyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)-butyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)butyl]-2-trifluoromethylphenoxazine
-
-
10-[4'-[(beta-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
-
-
10-[4'-[(beta-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
-
-
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
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IC50: 0.0203 mM, PDE7; IC50: 0.0453 mM, PDE4
3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide
-
-
3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride
-
-
3-isobutyl-1-methyl-xanthine
3-isobutyl-1-methylxanthine
3-isobuytl-1-methylxanthine
-
-
4-(3,4-dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one
-
PDE4 inhibitor, potent inhibitor of isoform PDE4D3
4-(3,4-dimethoxyphenyl)-2-{5-[(2-{5-[2-(2-fluoro-5-methoxyphenyl)ethyl]tetrahydrofuran-2-yl}ethyl)amino]pentyl}-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
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the dual PDE4 inhibitor/selective serotonin reuptake inhibitor shows potent and selective serotonin reuptake inhibition
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
-
4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone
-
competitive
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
i.e. NVP; i.e. NVP; i.e. NVP
6-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4,5-dihydropyridazin-3(2H)-one
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6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
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IC50: 0.0513 mM, PDE7; IC50: 0.1008 mM, PDE4
8-(4-chlorophenyl)thioguanosine 3',5'-cyclic monophosphate
-
-
8-bromoguanosine 3',5'-cyclic monophosphate
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8-methoxymethyl-isobutylmethylxanthine
-
inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5
alpha-alpha'-dipyridyl
treatment of CpdA with the Fe2+-specific chelator alpha-alpha'-dipyridyl results in a nearly complete loss of activity
apigenin
-
-
apigenin-7-O-glucoside
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apremilast
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CC-10004, i.e. (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide, oral phosphodiesterase-4 inhibitor, apremilast shows no marked selectivity among PDE4 isozymes
avanafil
-
-
AWD 12-250
-
-
AWD 12-281
-
selective PDE4 inhibitor
AWD12-281
-
-
ayanin
-
i.e. quercetin-3,7,4'-O-trimethylether, non-selective phosphodiesterase 1-4 inhibitor
Biochanin A
-
IC50: 0.0085 mM, more selectively inhibits PDE4 than PDE1 or PDE2
BRL-50481
-
PDE7 inhibitor
BRL50481
-
-
Caffeine
-
50 mM, 30% inhibition of soluble enzyme
cAMP-N1-oxide
-
-
cGMP
-
5% inhibition at 0.1 mM
chamomile
-
inhibits cAMP-PDE activity
CI-1044
-
i.e. (R)-N-[9-amino-3,4,6,7-tetrahydro-4-oxo-1-phenylpyrrolo[3,2,1-j,k][1,4] benzodiazepin-3-yl]-3-pyridinecarboxamide, selective inhibitor of PDE4, administration of 160 mg/kg of CI-1044 causes perivascular and interstitial inflammation, with infiltrates of admixed neutrophils and macrophages but without evidence of vascular necrosis, PDE4 inhibitor CI-1044 induces changes of vascular tone that could lead to histological alterations in the mesenteric area
Cibacron blue
-
-
cilomilast
Cilostamide
cilostazol
-
IC50: 0.0214 mM, PDE7; IC50: 0.088 mM, PDE4
cis-(+)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+/-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[(E)-4-(1H-imidazol-1-yl)but-2-enyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[2-[2-(1H-imidazol-1-yl)ethoxy]ethyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylmethyl)-benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-[(1H-imidazol-1-yl)methyl]benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[2-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[3-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(piperidin-1-ylmethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-oxopiperidin-1-yl)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(dimethylamino)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.2.0]oct-4-en-2-one hydrochloride
-
-
D-22888
-
-
DC-TA 46
-
the inhibitor affects memory retention in a visible/hidden-platform water maze task. This memory impairment can be correlated to the decrease of cAMP nucleotide, due to the induction of a PDE4D cAMP-specific PDE isoform
denbufylline
-
-
dexamethasone
-
dexmethasone at 0.1 mg/kg inhibits the activity of PDE4
dioclein
-
dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 19fold more selective for the activated PDE1 isoform compared to PDE3
diosmetin
-
IC50: 0.0202 mM, PDE4
dipyridamole
dipyridimole
-
-
E4021
-
-
erythro-9-(2-hydroxy-3-nonyl)-adenine hydrochloride
-
erythro-9-(2-hydroxy-3-nonyl)adenine
erythro-9-[3-(2-hydroxynonyl)]-adenine
-
erythro-9-[3-(2-hydroxynonyl)]adenine
-
0.1 mM, 12% inhibition, wild-type enzyme
etazolate
ethaverine
-
IC50: 0.008 mM
ethyl 2-([4-(3-carbamoylpiperazin-1-yl)-6-[4-(dimethylamino)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[(3,4-dimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-[3-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([7-ethyl-6-[(4-sulfamoylbenzyl)amino]-7H-purin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4,6-bis(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00027 mM, PDE4D; IC50: 0.00031 mM, PDE4B
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
-
IC50: 0.017 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
-
IC50: 0.015 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00088 mM, PDE4D; IC50: 0.0015 mM, PDE4B
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
-
IC50: 0.06 mM, PDE4B; IC50: 0.082 mM, PDE4D
ethyl 4-methyl-2-([4-(4-methylpiperazin-1-yl)-6-[methyl(3,4,5-trimethoxybenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(methylamino)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(piperazin-1-yl)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[methyl(3,4,5-trimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-[[4-(piperazin-1-yl)-7-(3,4,5-trimethoxybenzyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,3-thiazole-5-carboxylate
-
-
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
-
IC50: 0.025 mM, PDE4B; IC50: 0.05 mM, PDE4D
genistein
-
IC50: 0.0095 mM, PDE4
hesperetin
-
IC50: 0.0282 mM, PDE4
hyperoside
-
-
IBMX
non-selective PDE inhibitor
imperatorin
-
potent PFE4 inhibitor, imperatorin is significantly more active against PDE4B than PDE4A
IR-202
-
PDE7 inhibitor
IR-284
-
dual PDE4/PDE7 inhibitor
isobutylmethylxanthine
L-826,141
-
PDE4-selective inhibitor
LAS-31025
-
-
lodenafil
-
-
luteolin
luteolin-7-glucoside
-
IC50: 0.043 mM, PDB4, dual inhibition of PDE2 and PDE4
luteolin-7-O-glucoside
-
-
methylisobutylxanthine
-
-
Milrinone
mirodenafil
-
-
MK298
-
-
myricetin
-
IC50: 0.0389 mM, PDE4
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
10% inhibition at 0.01 mM; 11% inhibition at 0.01 mM; lead compound for Parkinson's disease treatment
N-[3-(1H-imidazol-1-yl)propyl]-2-[cis-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,8,8a-tetrahydrophthalazin-2(1H)-yl]acetamide
-
-
N6-Monobutyryl-cAMP
-
-
N6-monobutyyl-cAMP
-
-
O-phospho-L-serine
-
PdeA and PdeB show 59% and 73% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphoserine
O-phospho-L-tyrosine
-
PdeA and PdeB show 44% and 52% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphotyrosine
orthovanadate
-
PdeA and PdeB show 26% and 29% residual activity, respectively, for 3',5'-cAMP hydrolysis at 1 mM orthovanadate
papaverine
patuletin-7-O-glucoside
-
-
PF-04957325
-
a selective PDE8 inhibitor
prunetin
-
IC50: 0.0114 mM, PDE4
quazinone
-
0.1 mM, 26% inhibition, wild-type enzyme
quercetin
quercetin-3,5,7,3',4'-O-pentaacetate
-
-
quercetin-3,5,7,3',4'-O-pentamethylether
-
-
quercetin-3,7,4'-O-trimethylether
-
ayanin
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
-
-
quercetin-3-O-methylether
-
-
quinazolinamine
-
IC50: 0.34 mM, PDE4
R-rolipram
-
-
Ro 20-1724
RO 201724
-
-
Ro-20-1724
-
inhibition of PDE4, resulting in increased intacelular cAMP
Ro20-1724
roflumilast
rolipram
RP-73401
-
IC50: 0.0000016 mM, PDE4
RPR-73401
-
-
RS-25344
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-25344 about 100fold
RS-33793
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-33793 about 330fold
SB 207499
SCH 351591
SCH51866
sildenafil
tadalafil
theophylline
trequinsin
vardenafil
vinpocetine
XAP2
-
noncompetitive inhibition, aryl-hydrocarbon receptor-interacting protein XAP2 inhibits PDE4A5 activity by XAP2 does not require any intermediate proteins. XAP2 inhibits PDE4A5 and not other PDE4 isoforms
-
zaprinast
zardaverine
Zl-n-91
-
selective PDE4 inhibitor, Zl-n-91 at 0.03, 0.3 or 3 mg/kg dose dependently inhibits PDE4 activity
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Calmodulin
-
required, Km value 0.000057 mM
cAMP
binds to N-terminus and GAF domain, affinity of 0.0005 mM; binds to N-terminus and GAF domain, affinity of 0.001 mM
cGMP
binds to N-terminus and GAF domain, affinity of 0.003 mM
EDTA
-
EDTA at 0.10 mM slightly activates PDE4
extract of Ginkgo biloba
-
some beneficial effects of extract of Ginkgo biloba might be due to its modulating influences on cellular cyclic AMP levels via activation of membrane-bound PDE
-
follicle-stimulating hormone
-
stimulation
-
haloperidol
-
chronic treatment with 20 mg/kg clozapine increases PDE4B2 and PDE4B4 expression by 102 and 71%, respectively
isoproterenol
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00025 - 0.01
3',5'-cAMP
1.6
3',5'-cGMP
-
wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24C
0.00003 - 0.277
adenosine 3',5'-cyclic phosphate
0.0001 - 0.191
cAMP
0.24 - 0.427
cGMP
0.124
guanosine 3',5'-cyclic phosphate
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00093 - 4.3
3',5'-cAMP
1.6
3',5'-cGMP
Homo sapiens
-
wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24C
0.3 - 6.7
cAMP
0.48 - 1.19
cGMP
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.19 - 0.29
3',5'-cAMP
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000085
(R)-rolipram
-
-
0.001
10-(3-pyrrolidin-1-ylpropyl)-2-(trifluoromethyl)-10H-phenoxazine
-
pH 7.5, 30C
0.0008
10-(4'-N-morpholinobutyl)-2-chlorophenoxazine
-
-
0.00101
10-(4'-N-morpholinobutyl)-2-trifluoromethylphenoxazine
-
-
0.0007
10-(4'-N-piperidinobutyl)-2-chlorophenoxazine
-
-
0.00054
10-(4'-N-piperidinobutyl)-2-trifluoromethylphenoxazine
-
-
0.00058
10-(4'-N-pyrrolidinobutyl)-2-chlorophenoxazine
-
-
0.00018
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
-
-
0.00097
10-[3'-[(beta-hydroxyethyl)-piperazino]propyl]-2-trifluoromethylphenoxazine
-
-
0.00087
10-[30-[(beta-hydroxy ethyl)-piperazino]propyl]-2-chlorophenoxazine
-
-
0.00105
10-[4'-(N-diethylamino)-butyl]-2-chlorophenoxazine
-
-
0.0006
10-[4'-(N-diethylamino)butyl]-2-trifluoromethylphenoxazine
-
-
0.00038
10-[4'-[(beta-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
-
-
0.00055
10-[4'-[(beta-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
-
-
0.000002
4-(3,4-dimethoxyphenyl)-2-{5-[(2-{5-[2-(2-fluoro-5-methoxyphenyl)ethyl]tetrahydrofuran-2-yl}ethyl)amino]pentyl}-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
isoform PDE4D3, pH and temperature not specified in the publication
0.0018
4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone
-
-
0.000068
apremilast
-
PDE4 purified from U-937 cells, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.000097 - 0.000114
cilomilast
0.0183 - 0.0493
diazepam
0.00025 - 0.00038
R-rolipram
0.0076
RO 201724
-
-
0.000037 - 0.074
rolipram
0.000099
XAP2
-
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.1195
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.1195 mM, PDE7
0.31
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
Homo sapiens
-
IC50: 0.31 mM, PDE4
0.00043
(2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
Homo sapiens
-
IC50: 0.00043 mM, PDE4
0.000085
(4aS,8aR)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0001
1-(2,4-dichlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0011
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0009
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0012
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0024
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0034
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0002
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0006
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0009
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.002
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0012
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0023
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
Bos taurus
-
-
0.0031
10-[4'-[(b-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
Bos taurus
-
-
0.0044
10-[4'-[(b-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
Bos taurus
-
-
0.0203 - 0.0453
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
0.00381 - 3
3-isobutyl-1-methyl-xanthine
0.0021 - 0.698
3-isobutyl-1-methylxanthine
0.0059
3-isobuytl-1-methylxanthine
Homo sapiens
-
-
0.0087
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
Cavia porcellus
-
PDE4
0.00018 - 0.0073
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
0.00057 - 0.0057
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.0513 - 0.1008
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0041
apigenin
Homo sapiens
-
-
0.0102
apigenin-7-O-glucoside
Homo sapiens
-
-
0.00002 - 0.000074
apremilast
0.0004 - 0.0097
AWD 12-250
0.000015 - 0.0205
AWD12-281
0.0085
Biochanin A
Cavia porcellus
-
IC50: 0.0085 mM, more selectively inhibits PDE4 than PDE1 or PDE2
0.0002
BRL-50481
Homo sapiens
-
pH and temperature not specified in the publication
19
Caffeine
Leishmania mexicana
-
particulate enzyme
2.401 - 2.91
cAMP-N1-oxide
0.0005
CI-1044
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008 - 0.02
Cibacron blue
0.000101 - 0.000114
cilomilast
0.022 - 0.099
Cilostamide
0.0214 - 0.088
cilostazol
0.0000003
cis-(+)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000088
cis-(-)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000004
cis-2-[(E)-4-(1H-imidazol-1-yl)but-2-enyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000052
cis-2-[2-[2-(1H-imidazol-1-yl)ethoxy]ethyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000013
cis-2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylmethyl)-benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000007
cis-2-[4-[(1H-imidazol-1-yl)methyl]benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000013
cis-4-(3,4-dimethoxyphenyl)-2-[2-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000014
cis-4-(3,4-dimethoxyphenyl)-2-[3-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.000001
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000009
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000082
cis-4-(3,4-dimethoxyphenyl)-2-[4-(piperidin-1-ylmethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.000002
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000009
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-oxopiperidin-1-yl)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000097
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(dimethylamino)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000459
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.0000164
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.2.0]oct-4-en-2-one hydrochloride
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.00008 - 0.0048
D-22888
0.0005
denbufylline
Homo sapiens
-
-
0.0094 - 0.043
diazepam
0.0168
dioclein
Bos taurus
-
isoform PDE4, pH and temperature not specified in the publication
0.0202
diosmetin
Cavia porcellus
-
IC50: 0.0202 mM, PDE4
0.000146 - 0.042
dipyridamole
0.009
dipyridimole
Homo sapiens
-
-
0.015
E4021
Homo sapiens
-
-
0.128
EHNA
Trypanosoma cruzi
Q49UB9
30C, pH 7.5
0.217
erythro-9-(2-hydroxy-3-nonyl)-adenine hydrochloride
Trypanosoma cruzi
Q6XG56
-
0.13
erythro-9-[3-(2-hydroxynonyl)]-adenine
Mus musculus
P70453
-
0.0013 - 1.3
etazolate
0.008
ethaverine
Trypanosoma brucei
-
IC50: 0.008 mM
0.000082
ethyl 2-([4-(3-carbamoylpiperazin-1-yl)-6-[4-(dimethylamino)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000031
ethyl 2-([4-[(3,4-dimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000076
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000083
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00013
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00012
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-[3-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 2-([7-ethyl-6-[(4-sulfamoylbenzyl)amino]-7H-purin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000063
ethyl 2-[[4,6-bis(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000056
ethyl 2-[[4-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00027 - 0.00031
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
0.017 - 0.019
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
0.015 - 0.019
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
0.00088 - 0.0015
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
0.06 - 0.082
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
0.000039
ethyl 4-methyl-2-([4-(4-methylpiperazin-1-yl)-6-[methyl(3,4,5-trimethoxybenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0001
ethyl 4-methyl-2-([4-(methylamino)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 4-methyl-2-([4-(piperazin-1-yl)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00022
ethyl 4-methyl-2-([4-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00001
ethyl 4-methyl-2-([4-[methyl(3,4,5-trimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.000006
ethyl 4-methyl-2-[[4-(piperazin-1-yl)-7-(3,4,5-trimethoxybenzyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,3-thiazole-5-carboxylate
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.025 - 0.05
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
0.0095
genistein
Cavia porcellus
-
IC50: 0.0095 mM, PDE4
0.0282
hesperetin
Cavia porcellus
-
IC50: 0.0282 mM, PDE4
0.0118
hyperoside
Homo sapiens
-
-
0.000085
IR-202
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004 - 0.0000013
L-826,141
0.00421 - 0.00728
LAS-31025
0.0013 - 0.0191
luteolin
0.043
luteolin-7-glucoside
Cavia porcellus
-
IC50: 0.043 mM, PDB4, dual inhibitionof PDE2 and PDE4
0.0149
luteolin-7-O-glucoside
Homo sapiens
-
-
0.04
methylisobutylxanthine
Rattus norvegicus
-
-
0.0033 - 0.0583
Milrinone
0.0389
myricetin
Cavia porcellus
-
IC50: 0.0389 mM, PDE4
0.0021
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
Homo sapiens
Q13946
pH not specified in the publication, 30C
0.0000143
N-[3-(1H-imidazol-1-yl)propyl]-2-[cis-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,8,8a-tetrahydrophthalazin-2(1H)-yl]acetamide
Homo sapiens
-
in Tris-HCl (pH 7.6), 100 mM NaCl, 150 mM MgCl2, and 0.5% (w/v) polyethylene glycol 6000, at 30C
0.561 - 1.13
N6-monobutyyl-cAMP
0.3 - 0.8
OPC-3911
0.0125 - 0.174
papaverine
0.0149
patuletin-7-O-glucoside
Homo sapiens
-
-
0.0000002 - 0.0000007
PF-04957325
0.0114
prunetin
Cavia porcellus
-
IC50: 0.0114 mM, PDE4
0.0099
quercetin
0.0185
quercetin-3,5,7,3',4'-O-pentaacetate
Cavia porcellus
-
PDE4
0.0051
quercetin-3,5,7,3',4'-O-pentamethylether
Cavia porcellus
-
PDE4
0.0158
quercetin-3,7,4'-O-trimethylether
Cavia porcellus
-
PDE4
0.0039
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
Cavia porcellus
-
PDE4
0.0285
quercetin-3-O-methylether
Cavia porcellus
-
PDE4
0.34
quinazolinamine
Homo sapiens
-
IC50: 0.34 mM, PDE4
0.000042 - 0.0022
Ro20-1724
0.0000001 - 0.0000006
roflumilast
0.00001 - 10.46
rolipram
0.0000016
RP-73401
Homo sapiens
-
IC50: 0.0000016 mM, PDE4
0.000001 - 0.0178
RPR-73401
0.000113 - 0.000117
SB 207499
0.000105 - 0.000109
SCH 351591
0.0015 - 0.044
SCH51866
0.001 - 0.0861
sildenafil
0.01
tadalafil
Homo sapiens
-
IC50: above 10000 nM, PDE4
3 - 30
theophylline
0.0025 - 1.958
trequinsin
0.002055 - 0.0046
vardenafil
0.059 - 0.134
vinpocetine
0.04 - 2.8
zaprinast
0.01
additional information
Homo sapiens
-
IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5 - 8.5
-
PdeA and PdeB have slightly alkaline pH optima (pH 7.5-8.5) for 3',5'-cAMP hydrolysis in 0.1 M Tris-HCl buffer
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.3 - 9.2
-
pH 6.3: about 40% of maximal activity, pH 9.2: about 80% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
40
-
the optimum temperatures for the 3',5'-cAMP phosphodiesterase activity of PdeA is 40C
50
-
the optimum temperatures for the 3',5'-cAMP phosphodiesterase activity of PdeB is 50C
pI VALUE
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UNIPROT
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