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Information on EC 3.1.4.53 - 3',5'-cyclic-AMP phosphodiesterase and Organism(s) Homo sapiens and UniProt Accession Q13946

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EC Tree
     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.4 Phosphoric-diester hydrolases
                3.1.4.53 3',5'-cyclic-AMP phosphodiesterase
IUBMB Comments
Requires Mg2+ or Mn2+ for activity . 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 .
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Select one or more organisms in this record:
This record set is specific for:
Homo sapiens
UNIPROT: Q13946
Word Map
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
The taxonomic range for the selected organisms is: Homo sapiens
Synonyms
3',5'-cAMP phosphodiesterase, 3',5'-cyclic AMP phosphodiesterase, adenosine 3',5'-cyclic monophosphate PDE, cAMP phosphodiesterase, cAMP phosphodiesterase-4, cAMP-PDE, cAMP-phosphodiesterase, cAMP-specific cyclic nucleotide phosphodiesterase, cAMP-specific PDE, cAMP-specific PDE4A5, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cAMP phosphodiesterase-4
247
-
cAMP-PDE
247
-
cAMP-phosphodiesterase
247
-
cAMP-specific PDE
247
-
cAMP-specific PDE4D2
247
-
cAMP-specific phosphodiesterase
cAMP-specific phosphodiesterase-4D5
cyclic AMP phosphodiesterase-4
247
-
cyclic AMP-specific phosphodiesterase
247
-
cyclic nucleotide phosphodiesterase
247
-
cyclic nucleotide phosphodiesterase 4
247
-
cyclic nucleotide phosphodiesterase 4D
247
-
cyclic nucleotide phosphodiesterase-8A
284994
-
high affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
284994
-
hPDE4A
247
-
hPDE4B
247
-
HSPDE4A4B
247
-
PDE IVB
282188
-
PDE-46
247
-
PDE-4D3
247
-
PDE4A
PDE4A1
282184
isoform
PDE4A10
247
-
PDE4A4
247
isoform
PDE4A8
282184
-
PDE4B
PDE4B2
247
isoform
PDE4C
PDE4C2
247
isoform
PDE4D
PDE4D3
247
isoform
PDE4D5
PDE7A
PDE7A2
286552
isoform
PDE7B
PDE8
247
-
PDE8A
PDE8A1
284994
PDE8A catalytic domain
PDE8B
phosphodiesterase 4
247
-
phosphodiesterase 4 isoform A8
282184
-
phosphodiesterase 4B
247
-
phosphodiesterase 7
247
-
phosphodiesterase 7B
247
isoform
phosphodiesterase type 4
247
-
phosphodiesterase type 5
247
-
phosphodiesterase-4
247
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
adenosine 3',5'-cyclic phosphate + H2O = AMP
show the reaction diagram
catalytic reaction mechanism, overview
-
PATHWAY SOURCE
PATHWAYS
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
-
SUBSTRATE
PRODUCT                       
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
specific substrate
-
-
?
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
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
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
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
-
determination of reaction rate and mechanism using computational modeling, quantum mechanical/molecular mechanical-free energy perturbation, QM/MM-FE, and QM/MM-Poisson-Boltzmann surface area, PBSA, calculations. The onQM/MMreaction-coordinate calculations including the protein environment of any PDE-catalyzed reaction system identifies a unique catalytic reaction mechanism, overview
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
the enzyme requires the presence of at least 1 mM Mn2+ or Mg2+ for maximal activity in vitro
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
-
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
lead compound for Parkinson's disease treatment
(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
-
-
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-[(2-chloro-4-nitrophenyl)thio]-pyridine
-
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
i.e. NVP
6-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4,5-dihydropyridazin-3(2H)-one
-
-
apigenin
-
-
apigenin-7-O-glucoside
-
-
apremilast
-
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
-
-
AWD12-281
-
-
BRL-50481
-
PDE7 inhibitor
BRL50481
-
-
cAMP-N1-oxide
-
-
cGMP
-
5% inhibition at 0.1 mM
chamomile
-
inhibits cAMP-PDE activity
cilomilast
Cilostamide
-
IC50: 0.099 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
-
-
denbufylline
-
-
dipyridamole
dipyridimole
-
-
E4021
-
-
erythro-9-(2-hydroxy-3-nonyl)adenine
-
7.4% inhibition at 0.1 mM
erythro-9-[3-(2-hydroxynonyl)]adenine
-
0.1 mM, 12% inhibition, wild-type enzyme
etazolate
-
-
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
hyperoside
-
-
IR-202
-
PDE7 inhibitor
IR-284
-
dual PDE4/PDE7 inhibitor
LAS-31025
-
-
lodenafil
-
-
luteolin
-
-
luteolin-7-O-glucoside
-
-
Milrinone
mirodenafil
-
-
MK298
-
-
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
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
-
-
papaverine
-
-
patuletin-7-O-glucoside
-
-
quazinone
-
0.1 mM, 26% inhibition, wild-type enzyme
quinazolinamine
-
IC50: 0.34 mM, PDE4
R-rolipram
-
-
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
-
weak inhibitior
vardenafil
vinpocetine
zaprinast
zardaverine
Zn2+
-
more than 90% inhibition at 0.05 mM Zn2+ in the presence of 0.1 mM EDTA, inhibition can be greatly relieved with EDTA at 0.30 mM
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
EDTA
-
EDTA at 0.10 mM slightly activates PDE4
isoproterenol
-
0.001 mM isoproterenol triggers a sustained, 2fold increase in PDE4 activity
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0007 - 0.0088
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
0.000055 - 0.0244
adenosine 3',5'-cyclic phosphate
0.0001 - 0.0058
cAMP
0.24 - 0.427
cGMP
0.124
guanosine 3',5'-cyclic phosphate
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4 - 4.3
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
0.3 - 6.7
cAMP
0.48 - 1.19
cGMP
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000085
(R)-rolipram
-
-
0.000068
apremilast
-
PDE4 purified from U-937 cells, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication
0.000114
cilomilast
30C
0.00025 - 0.00038
R-rolipram
0.000037 - 0.0016
rolipram
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00018
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
Homo sapiens
Q13946
pH not specified in the publication, 30C
0.0021
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
Homo sapiens
Q13946
pH not specified in the publication, 30C
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
0.0322 - 0.175
3-isobutyl-1-methyl-xanthine
0.00737 - 0.698
3-isobutyl-1-methylxanthine
0.0059
3-isobuytl-1-methylxanthine
Homo sapiens
-
-
0.0066 - 0.0073
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
0.00057 - 0.0057
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.0041
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
0.0002
BRL-50481
Homo sapiens
-
pH and temperature not specified in the publication
2.401 - 2.91
cAMP-N1-oxide
0.000101
cilomilast
Homo sapiens
P27815
-
0.099
Cilostamide
Homo sapiens
-
IC50: 0.099 mM, PDE4
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
-
-
0.0011 - 0.00194
dipyridamole
0.009
dipyridimole
Homo sapiens
-
-
0.015
E4021
Homo sapiens
-
-
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
0.0118
hyperoside
Homo sapiens
-
-
0.000085
IR-202
Homo sapiens
-
pH and temperature not specified in the publication
0.00421 - 0.00728
LAS-31025
0.0013
luteolin
Homo sapiens
-
-
0.0149
luteolin-7-O-glucoside
Homo sapiens
-
-
0.0033 - 0.00635
Milrinone
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
0.0149
patuletin-7-O-glucoside
Homo sapiens
-
-
0.34
quinazolinamine
Homo sapiens
-
IC50: 0.34 mM, PDE4
0.000042 - 0.0022
Ro20-1724
0.00001 - 0.18
rolipram
0.0000016
RP-73401
Homo sapiens
-
IC50: 0.0000016 mM, PDE4
0.000001 - 0.0178
RPR-73401
0.000113
SB 207499
Homo sapiens
-
-
0.000105
SCH 351591
Homo sapiens
-
-
0.0015
SCH51866
Homo sapiens
-
PDE7B expressed in transfected COS-7 cells
0.00319 - 0.0861
sildenafil
0.01
tadalafil
Homo sapiens
-
IC50: above 10000 nM, PDE4
0.002055 - 0.0046
vardenafil
0.059
vinpocetine
Homo sapiens
-
-
0.0525
zaprinast
Homo sapiens
-
mutant enzyme D440N
0.01
additional information
Homo sapiens
-
IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
parietal, frontal, temporal cortex, hippocampus, striatum, thalamus, hypothalamus, substantia nigra, nucleus accumbens, cerebellum
Manually annotated by BRENDA team
-
lung epithelial cell
Manually annotated by BRENDA team
-
carcinoma of salivary gland
Manually annotated by BRENDA team
-
phosphodiesterase 4 is detected in smooth muscle cells of the wall, and in the cytoplasm of luminal endothelial cells of cavernous arteries
Manually annotated by BRENDA team
-
PDE4 is observed in the nonvascular smooth musculature of the corpus cavernosum clitoris, sinusoidal endothelial and subendothelial layers, and nerve fibers innervating the tissue; presence of isoform PDE4 in nonvascular smooth musculature of the corpus carnosum, in sinusoidal endothelial and subendothelial layers, and nerve fiber innervating the tissue
Manually annotated by BRENDA team
-
presence of isoform PDE4 in nonvascular smooth musculature of the corpus carnosum
Manually annotated by BRENDA team
-
sinusoidal endothelial and subendothelialn layer of clitoris, presence of isoform PDE4
Manually annotated by BRENDA team
-
human middle ear epithelial cell
Manually annotated by BRENDA team
-
PDE4
Manually annotated by BRENDA team
-
gingiva-derived malignant melanoma cell, expression of variants PDE4B and PDE4D
Manually annotated by BRENDA team
-
monocytic cells may express different PDE4 isozymes, depending on their state of activation or differentiation. These isozymes could thus regulate intracellular cAMP levels at various stages of monocyte activation and could thereby be important in limiting the inflammatory response
Manually annotated by BRENDA team
-
human bronchial epithelial cell
Manually annotated by BRENDA team
-
cultured, PDE7
Manually annotated by BRENDA team
-
abundantly present in the fibromusclular stroma as well as in glandular structures of the transition zone
Manually annotated by BRENDA team
-
carcinoma of salivary gland
Manually annotated by BRENDA team
-
PDE4; PDE7
Manually annotated by BRENDA team
-
of central cavernous arteries
Manually annotated by BRENDA team