Information on EC 3.1.4.35 - 3',5'-cyclic-GMP phosphodiesterase

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

EC NUMBER
COMMENTARY hide
3.1.4.35
-
RECOMMENDED NAME
GeneOntology No.
3',5'-cyclic-GMP phosphodiesterase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
guanosine 3',5'-cyclic phosphate + H2O = GMP
show the reaction diagram
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-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
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-
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Purine metabolism
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SYSTEMATIC NAME
IUBMB Comments
3',5'-cyclic-GMP 5'-nucleotidohydrolase
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CAS REGISTRY NUMBER
COMMENTARY hide
9068-52-4
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
silkworm
-
-
Manually annotated by BRENDA team
PDE6
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-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
strains AX3 and DH1
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-
Manually annotated by BRENDA team
generation of transgenic animals with targeted expression of DmPDE6 to tubule type I (principal) cells. This reveals localization of DmPDE6 primarily at the apical membranes. Overexpression of DmPDE6 results in elevated cG-PDE activity and decreased tubule cGMP content. Such targeted overexpression of DmPDE6 creates a novel phenotype that manifests itself in inhibition of the active transport and efflux of cGMP by tubules
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-
Manually annotated by BRENDA team
Mus musculus C57BL/6J
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-
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Manually annotated by BRENDA team
no activity in Homo sapiens
functional PDE6 not detected in Y79 retinoblastoma cells. Attempts to enhance iexpression with cell culture or with introduction of virus expressing PDE6 are not successful. The results indicate that expression of a fully active stable PDE6 enzyme requires other post-transcriptional events that do not occur or are inhibited in Y79 cells
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-
Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
frog
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-
Manually annotated by BRENDA team
Rattus norvegicus Sprague-Dawley
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-
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
overview
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
mechanisms for PDE activation are similar in mammalian and amphibian photoreceptors as well as in rods and cones
malfunction
metabolism
physiological function
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-anthraniloyl cGMP + H2O
2'-O-anthraniloyl GMP
show the reaction diagram
-
-
-
?
2'-O-anthraniloyl-cGMP + H2O
?
show the reaction diagram
3',5'-cAMP + H2O
5'-AMP
show the reaction diagram
3',5'-cGMP + H2O
5'-GMP
show the reaction diagram
3',5'-cGMP + H2O
guanosine 5'-phosphate
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'-cGMP + H2O
5'-GMP
show the reaction diagram
3',5'-cGMP + H2O
guanosine 5'-phosphate
show the reaction diagram
-
phosphodiesterase 5 converts the second messenger 3',5'-cGMP to its inactive form
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
show the reaction diagram
additional information
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
Zn+-binding motif
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0121 mM, PDE5
(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: 0.00067 mM, PDE5
(4-(4-[2-ethyl-phenylamino)-methylene]-3-methyl-5-oxo-4,5-dihydro-pyrazol-1-yl)-benzoic acid
-
0.00001 mM, 50% inhibition
(E)-1-(3-(cyclopentyloxy)-4-methoxyphenyl)ethanone O-carbamoyl oxime
-
filaminast
1,2-dihydro-2-[(2-methyl-4-pyridinyl)methyl]-1-oxo-8-(2-pyrimidinylmethoxy)-4-(3,4,5-trimethoxyphenyl)-2,7-naphthyridine-3-carboxylic acid methyl ester hydrochloride
-
specific inhibitor of PDE5
1,2-dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium
-
-
1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)pyrazol[3,4d]-pyrimidin-4-(5H)-one
-
0.000006 mM, 50% inhibition in sham operated rats
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
1-(2-ethoxyethyl)-3-ethyl-5-(piperazin-1-yl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
1-(2-ethoxyethyl)-3-methyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
1-(3-chloro-4-methoxybenzyl)-3-(cis-4-hydroxycyclohexyl)-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridine-6-carbonitrile
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-
1-[4-[(1,3-benzodioxol-5-ylmethyl)amino]-6-chloroquinazolin-2-yl]piperidine-4-carboxylic acid
-
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1-[9-[(3-chloro-4-methoxybenzyl)amino]-3-ethyl-3H-pyrazolo[4',3':5,6]pyrido[3,4-d]pyridazin-6-yl]piperidin-4-ol
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-
1-[9-[(3-chloro-4-methoxybenzyl)amino]-3-ethyl-3H-pyrazolo[4',3':5,6]pyrido[3,4-d]pyridazin-6-yl]piperidine-4-carboxylic acid
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1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate
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trivial name sildenafil citrate or Viagra
2',3'-cGMP
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-
2,2',2'',2'''-[(4,8-dipiperidin-1-ylpyrimido[5,4-d]pyrimidine-2,6-diyl)dinitrilo]tetraethanol
-
-
2-(2,4-dihydroxyphenyl)-8-[5-hydroxy-5-methyl-2-(1-methylethenyl)hexyl]-5-methoxy-4H-chromene-3,7-diol
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-
2-(2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
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2-(2-methylpyridin-4-yl)methyl-4-(3,4,5-trimethoxyphenyl)-8-(pyrimidin-2-yl)methoxy-1,2-dihydro-1-oxo-2,7-naphthyridine-3-carboxylic acid methyl ester hydrochloride
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i.e. T-0156, IC50: 0.23 mM, potent and highly selective phosphodiesterase type 5 inhibitor
2-(2-propoxyphenyl)-1,7-dihydro-6H-purin-6-one
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-
2-(5-amino-2-propoxyphenyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-(5-[[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl]-2-propoxyphenyl)-5-methylquinazolin-4(3H)-one
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-
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
-
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
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IC50: 0.0027 mM, PDE5
2-methoxy-7-methyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazin-6(5H)-one
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2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one
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trivial name vardenafil or Levitra
2-[2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
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vardenafil
3',5'-cAMP
3',5'-cIMP
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3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
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3-(4-ethylpiperazin-1-yl)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
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3-(cyclopentylmethoxy)-N-(2,6-dichlorophenyl)-4-methoxybenzamide
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piclamilast
3-(cyclopropylmethoxy)-N-(2,6-dichlorophenyl)-4-(difluoromethoxy)benzamide
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roflumilast
3-([2-[(2-hydroxyethyl)amino]ethyl]amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
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3-ethyl-5-(4-methyl-1,4-diazepan-1-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-(morpholin-4-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-(piperazin-1-yl)-1-(2-propoxyethyl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-(piperazin-1-yl)-1-[2-(propan-2-yloxy)ethyl]-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-(piperazin-1-yl)-N-(pyridin-2-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-(piperazin-1-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-5-[(3R)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-N-(4-fluorophenyl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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-
3-ethyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-N-(6-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-ethyl-N5-(1-methylpiperidin-4-yl)-N7-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidine-5,7-diamine
-
-
3-isobutyl-1-methyl-8-methoxymethylxanthine
-
-
3-isobutyl-1-methylxanthine
3-methyl-5-[(3R)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-methyl-5-[(3S)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-methyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
3-methyl-N-(6-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
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3-[(1R,4R)-2,5-diazabicyclo[2.2.1]hept-2-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
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3-[(2-aminoethyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
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3-[(6-deoxy-alpha-L-mannopyranosyl)oxy]-5-hydroxy-8-(1-hydroxy-2-methylprop-2-en-1-yl)-2-(4-methoxyphenyl)-4-oxo-3,4-dihydro-2H-chromen-7-yl beta-D-glucopyranoside
-
-
3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
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-
3-[4-(2,2-dihydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]-pyrazin-2(1H)-one
-
-
3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5
3-[4-(3-hydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-(3-hydroxypropyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-[(2R)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-[(2R,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-[(2S)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-[4-[(2S,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
4-(1,3-benzodioxol-5-ylmethoxy)-2-(1H-imidazol-1-yl)-5-phenylpyrimidine
-
-
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro20-1724
4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
-
cilomilast
4-[3-ethyl-7-(pyrimidin-4-ylamino)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one
-
-
4-[7-hydroxy-8-[5-hydroxy-5-methyl-2-(1-methylethenyl)hexyl]-5-methoxy-4H-chromen-2-yl]benzene-1,3-diol
-
-
5-(1,4-diazepan-1-yl)-3-ethyl-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
5-(1,4-diazepan-1-yl)-3-methyl-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
5-(2-propoxyphenyl)-2,3-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
-
-
5-(2-propoxyphenyl)-3,6-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
-
zardaverine
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
-
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0025 mM, PDE5
6-benzo[1,3]dioxol-5-yl-2-methyl-2,3,6,7,12,12a-hexahydropyrazinol[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
-
trivial name tadalafil or Cialis
6-deoxy-3-O-[6-deoxy-4-O-[7-(beta-D-glucopyranosyloxy)-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-8-(2-methylprop-1-en-1-yl)-4-oxo-3,4-dihydro-2H-chromen-3-yl]-alpha-L-mannopyranosyl]-alpha-L-mannopyranose
-
-
7-(6-methoxypyridin-3-yl)-3-(piperazin-1-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
8-(5-[[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]sulfonyl]-2-propoxyphenyl)-6-propyl-6,6a,9,9a-tetrahydro-5H-[1,2,4]triazolo[3,4-i]purin-5-one
-
-
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
-
-
8-methoxymethyl-isobutylmethylxanthine
-
; inhibits isoform PDE5, is 3times more potent in inhibiting PDE5 than PDE1
9-[(3-chloro-4-methoxybenzyl)amino]-3-ethyl-N-methyl-3H-pyrazolo[4',3':5,6]pyrido[3,4-d]pyridazine-6-carboxamide
-
-
amentoflavone
-
IC50: 0.0117 mM
amrinone
-
IC50: 0.2296 mM, PDE5
ATP
-
slight inhibition at 1 mM
avanafil
-
TA-1790, highly selective inhibitor of PDE5
BAY 60-7550
-
-
BAY 73-6691
-
specific PDE9A inhibitor
benzamidenafil
-
i.e. N-(3,4-dimethoxy benzyl)-2-[[(1R,S)-2-hydroxy-1-methylethyl]amino]-5-nitrobenzamide, potent and specific inhibitor of PDE-5
bilobetin
-
IC50: 0.00152 mM
Ca2+
-
inhibitory at 1 mM together with Mg2+ below 0.1 mM
Caffeine
cAMP
-
inhibition at high concentrations
cGMP
-
inhibition above 0.001 mM
chamomile
-
weak, but still statistically significant inhibition of PDE5A1
Cilostamide
cilostazol
-
IC50: 0.0044 mM, PDE5
Colchicine
-
-
cone Pgamma subunit
-
PDE6C is potently inhibited by the recombinant cone and rod Pgamma-subunits with slight selectivity for the cone Pgamma
-
CP461
-
-
delphinidin
-
-
delphinidin 3-glucoside
-
-
dibutyryl 3',5'-cAMP
-
-
dioclein
-
dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to PDE5 (16fold)
diosmetin
-
IC50: 0.015 mM, PDB5
dipyridamole
Evo48
-
potent inhibitor of PDE5
-
exisulind
-
-
fructose 1,6-bisphosphate
-
-
fructose 6-phosphate
-
-
genistein
-
IC50: 0.073 mM, PDB5
ginkgetin
-
IC50: 0.00059 mM
GTP
-
slight inhibition at 1 mM
histone
-
-
Inhibitor protein
inhibitory gamma subunit of PDE
-
i.e. Pgamma
-
luteolin
-
IC50: 0.0193 mM, PDB5
malvidin
-
IC50: 0.0354 mM
malvidin-3-O-beta-glucoside
-
IC50: 0.0116 mM
Mg2+
-
inhibitory below 0.1 mM together with Ca2+ at 1 mM
Milrinone
-
IC50: 0.0491 mM, PDE5
MY-5445
-
inhibition significantly increases contractility in hypertrophied myocardium
N-(3-chloro-4-methoxybenzyl)-2-pyridin-4-yl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4-amine
-
-
N-(3-chloro-4-methoxybenzyl)-3-ethyl-6-(pyridin-4-ylmethyl)-3H-pyrazolo[4',3':5,6]pyrido[3,4-d]pyridazin-9-amine
-
-
N-[3-(1,3-dimethyl-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-4-propoxyphenyl]methanesulfonamide
-
-
N-[3-(4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)-4-propoxyphenyl]piperidine-1-carboxamide
-
-
N-[3-(4-oxo-3,4-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl)-4-propoxyphenyl]morpholine-4-carboxamide
-
-
N5-(2-aminoethyl)-3-ethyl-N7-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidine-5,7-diamine
-
-
papaverine
-
-
Pb2+
-
-
peonidin
-
-
peonidin 3-glucoside
-
-
petunidin
-
-
petunidin 3-glucoside
-
-
PF-3717842
high-affinity phosphodiesterase-5 inhibitor
Pgamma-inhibitory peptide
-
-
-
Pgamma-inhibitory peptide Pgamma63-87
-
-
-
Pgamma-inhibitory peptide Pgamma70-87
-
-
-
PgammaPDE6
regulatory subunit of PDE6, inhibition of catalytic activity
-
Phosphate buffer
-
-
-
quercetin-3,5,7,3',4'-O-pentamethylether
-
-
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
-
-
quercetin-3-O-methylether
-
-
quinazolinamine
-
IC50: 0.000021 mM, PDE5
rod Pgamma subunit
-
PDE6C is potently inhibited by the recombinant cone and rod Pgamma-subunits with slight selectivity for the cone Pgamma
-
rolipram
RP-73401
-
IC50: 0.0089 mM, PDE5
SCH 51866
0.0029 mM, 50% inhibition of PDE9A5, 0.0033 mM, 50% inhibition of PDE9A1
sciadopitysin
-
IC50: 0.00324 mM
sequoiaflavone
-
IC50: 0.0199 mM
sildenafil
sildenafil citrate
inhibition of PDE5 activity in the intestine, which might occur during sildenafil citrate ingestion, could result in a transitory diarrhoe
SLx-2101
-
inhibits excellent potency both ex vivo and in vivo
Sodium deoxycholate
-
-
T-1032
-
IC50: 0.041 mM
T0156
-
selective phosphodiesterase type 5 inhibitor
tadalafil
theophylline
trans-4-([2-[(3-chloro-4-methoxyphenyl)carbamoyl]-4-cyanophenyl]carbamoyl)cyclohexanecarboxylic acid
-
-
udenafil
UK-369,003
-
i.e. 1-[6-ethoxy-5-[3-ethyl-6,7-dihydro-2-(2-methoxyethyl)-7-oxo-2H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-pyridyl sulfonyl]-4-ethylpiperazine benzenesulfonate, a potent selective inhibitor of cGMP-specific PDE5 with more than 80fold selectivity for PDE5 over PDE6, more than 3000fold selectivity over PDEs 1-4 and 10, and more than 10000fold selectivity over PDE11
vardenafil
zaprinast
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
8-Bromo-cGMP
-
-
alpha-subunit of transducin
cyclic AMP-dependent protein-kinase
-
phosphorylates alpha- and beta-subunit
-
Glycylglycine buffer
-
-
Imidazole buffer
-
-
-
PgammaPDE6
regulatory subunit of PDE6, activation of cGMP binding to GAF domains of PDE6alpha or beta subunit
-
Protein kinase C
-
phosphorylates alpha- and gamma-subunit
-
S-modulin
-
-
-
S-nitrosoglutathione
-
stimulation of isoform PDE5 phosphorylation and activity, resulting in increased levels of cGMP in gastric smooth muscle cells. Concurrent activation of cells with acetylcholine augments stimulation and attenuates cGMP levels
stable toxin
possibly due to an increase in cGMP resulting from stable toxin treatment
-
Transducin
Triton X-100
-
-
Trypsin
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.012
2'-O-anthraniloyl cGMP
-
37C, pH 7.4
0.0247 - 0.0651
2'-O-anthraniloyl-cGMP
0.00098 - 0.82
3',5'-cAMP
0.00032 - 1
3',5'-cGMP
0.00022 - 1.6
cGMP
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.55 - 4400
3',5'-cGMP
0.00083 - 3.8
cGMP
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000045
1,3-dimethyl-6-(2-propoxy-5-methanesulfonylamidophenyl)pyrazol[3,4d]-pyrimidin-4-(5H)-one
-
sham-operated rats
0.000045
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
-
-
0.000176 - 0.0006608
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
1
3',5'-cAMP
-
-
0.0000487 - 0.0007215
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
0.0085 - 0.09485
3-isobutyl-1-methylxanthine
0.0012
5-(2-propoxyphenyl)-2,3-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
-
-
0.0000173 - 0.001605
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
0.0000026 - 0.0000183
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
1.8
cAMP
-
-
0.078 - 0.14
cone Pgamma subunit
0.0000035 - 0.0001735
E4021
0.0015
Pgamma-inhibitory peptide
-
chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication
-
0.0029
Pgamma-inhibitory peptide Pgamma63-87
-
chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication
-
0.0121
Pgamma-inhibitory peptide Pgamma70-87
-
chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication
-
0.105 - 0.155
rod Pgamma subunit
0.000013 - 0.0000984
sildenafil
0.0001778 - 0.01438
zaprinast
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0121
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0121 mM, PDE5
0.00067
(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: 0.00067 mM, PDE5
0.053
(E)-1-(3-(cyclopentyloxy)-4-methoxyphenyl)ethanone O-carbamoyl oxime
Homo sapiens
-
-
0.019
1,2-dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium
Homo sapiens
-
-
0.000055 - 0.0001
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
0.0000004
1-(2-ethoxyethyl)-3-ethyl-5-(piperazin-1-yl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-(3-chloro-4-methoxybenzyl)-3-(cis-4-hydroxycyclohexyl)-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridine-6-carbonitrile
Homo sapiens
-
-
0.0000037
1-[4-[(1,3-benzodioxol-5-ylmethyl)amino]-6-chloroquinazolin-2-yl]piperidine-4-carboxylic acid
Homo sapiens
-
-
0.00069
2,2',2'',2'''-[(4,8-dipiperidin-1-ylpyrimido[5,4-d]pyrimidine-2,6-diyl)dinitrilo]tetraethanol
Homo sapiens
-
-
0.000005
2-(2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
Homo sapiens
-
-
0.23
2-(2-methylpyridin-4-yl)methyl-4-(3,4,5-trimethoxyphenyl)-8-(pyrimidin-2-yl)methoxy-1,2-dihydro-1-oxo-2,7-naphthyridine-3-carboxylic acid methyl ester hydrochloride
Canis lupus familiaris
-
i.e. T-0156, IC50: 0.23 mM, potent and highly selective phosphodiesterase type 5 inhibitor
0.00001
2-(2-propoxyphenyl)-1,7-dihydro-6H-purin-6-one
Homo sapiens
-
-
0.0000017
2-(5-amino-2-propoxyphenyl)thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0000065
2-(5-[[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl]-2-propoxyphenyl)-5-methylquinazolin-4(3H)-one
Homo sapiens
-
-
0.0027
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0027 mM, PDE5
0.00001
2-methoxy-7-methyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazin-6(5H)-one
Homo sapiens
-
-
0.0000007
2-[2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
Homo sapiens
-
-
0.00000022
3-(4-ethylpiperazin-1-yl)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0035
3-(cyclopentylmethoxy)-N-(2,6-dichlorophenyl)-4-methoxybenzamide
Homo sapiens
-
-
0.017
3-(cyclopropylmethoxy)-N-(2,6-dichlorophenyl)-4-(difluoromethoxy)benzamide
Homo sapiens
-
-
0.00000112
3-([2-[(2-hydroxyethyl)amino]ethyl]amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000648
3-ethyl-5-(4-methyl-1,4-diazepan-1-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000392
3-ethyl-5-(morpholin-4-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
3-ethyl-5-(piperazin-1-yl)-1-(2-propoxyethyl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000086
3-ethyl-5-(piperazin-1-yl)-1-[2-(propan-2-yloxy)ethyl]-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000065
3-ethyl-5-(piperazin-1-yl)-N-(pyridin-2-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000015
3-ethyl-5-(piperazin-1-yl)-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000007
3-ethyl-5-[(3R)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000009
3-ethyl-N-(4-fluorophenyl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000328
3-ethyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000101
3-ethyl-N-(6-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000035
3-ethyl-N5-(1-methylpiperidin-4-yl)-N7-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidine-5,7-diamine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000019 - 0.032
3-isobutyl-1-methylxanthine
0.00000014
3-methyl-5-[(3R)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000094
3-methyl-5-[(3S)-3-methylpiperazin-1-yl]-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000184
3-methyl-N-(4-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000078
3-methyl-N-(6-methylpyridin-2-yl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000238
3-[(1R,4R)-2,5-diazabicyclo[2.2.1]hept-2-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000025
3-[(2-aminoethyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000021
3-[4-(2,2-dihydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000072
3-[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000002
3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]-pyrazin-2(1H)-one
0.00000108
3-[4-(3-hydroxypropyl)-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000018
3-[4-(3-hydroxypropyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000023
3-[4-[(2R)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000003
3-[4-[(2R,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000031
3-[4-[(2S)-2-hydroxypropyl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000033
3-[4-[(2S,3R)-3-hydroxybutan-2-yl]-1,4-diazepan-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000014
4-(1,3-benzodioxol-5-ylmethoxy)-2-(1H-imidazol-1-yl)-5-phenylpyrimidine
Homo sapiens
-
-
0.053
4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
Homo sapiens
-
-
0.00000296
4-[3-ethyl-7-(pyrimidin-4-ylamino)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00000315
5-(1,4-diazepan-1-yl)-3-ethyl-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000979
5-(1,4-diazepan-1-yl)-3-methyl-N-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.081
5-(2-propoxyphenyl)-3,6-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
Homo sapiens
-
-
0.0025
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0025 mM, PDE5
0.00000328
7-(6-methoxypyridin-3-yl)-3-(piperazin-1-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00000034
8-(5-[[4-(2-hydroxyethyl)-1,4-diazepan-1-yl]sulfonyl]-2-propoxyphenyl)-6-propyl-6,6a,9,9a-tetrahydro-5H-[1,2,4]triazolo[3,4-i]purin-5-one
Homo sapiens
-
-
0.0055
8-methoxymethyl-isobutylmethylxanthine
Bos taurus
-
isoform PDE5, pH and temperature not specified in the publication
0.0117
amentoflavone
Homo sapiens
-
IC50: 0.0117 mM
0.2296
amrinone
Bos taurus
-
IC50: 0.2296 mM, PDE5
0.0000011 - 0.00002
benzamidenafil
0.00152
bilobetin
Homo sapiens
-
IC50: 0.00152 mM
0.0000405 - 0.0152
Cilostamide
0.0044
cilostazol
Bos taurus
-
IC50: 0.0044 mM, PDE5
0.023
dioclein
Bos taurus
-
isoform PDE5, pH and temperature not specified in the publication
0.015
diosmetin
Cavia porcellus
-
IC50: 0.015 mM, PDB5
0.0000109 - 0.023
dipyridamole
0.046
E4021
Plasmodium falciparum
Q2V2M6
IC50: 0.046 mM
0.073
genistein
Cavia porcellus
-
IC50: 0.073 mM, PDB5
0.00059
ginkgetin
Homo sapiens
-
IC50: 0.00059 mM
0.0193
luteolin
Cavia porcellus
-
IC50: 0.0193 mM, PDB5
0.0354
malvidin
Homo sapiens
-
IC50: 0.0354 mM
0.0116
malvidin-3-O-beta-glucoside
Homo sapiens
-
IC50: 0.0116 mM
0.0491
Milrinone
Bos taurus
-
IC50: 0.0491 mM, PDE5
0.0000026
N-(3-chloro-4-methoxybenzyl)-2-pyridin-4-yl-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4-amine
Homo sapiens
-
-
0.000003
N-[3-(1,3-dimethyl-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-4-propoxyphenyl]methanesulfonamide
Homo sapiens
-
-
0.0000035
N-[3-(4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)-4-propoxyphenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000018
N-[3-(4-oxo-3,4-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl)-4-propoxyphenyl]morpholine-4-carboxamide
Homo sapiens
-
-
0.00000952
N5-(2-aminoethyl)-3-ethyl-N7-(pyrimidin-4-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidine-5,7-diamine
Homo sapiens
-
pH and temperature not specified in the publication
0.0137
quercetin-3,5,7,3',4'-O-pentamethylether
Cavia porcellus
-
PDE5
0.0111
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
Cavia porcellus
-
PDE5
0.0869
quercetin-3-O-methylether
Cavia porcellus
-
PDE5
0.000021
quinazolinamine
Homo sapiens
-
IC50: 0.000021 mM, PDE5
0.0089
RP-73401
Homo sapiens
-
IC50: 0.0089 mM, PDE5
0.00324
sciadopitysin
Homo sapiens
-
IC50: 0.00324 mM
0.0199
sequoiaflavone
Homo sapiens
-
IC50: 0.0199 mM
0.0000013 - 0.056
sildenafil
0.041
T-1032
Strongylocentrotus purpuratus
-
IC50: 0.041 mM
0.0000018 - 0.01
tadalafil
0.0000004
trans-4-([2-[(3-chloro-4-methoxyphenyl)carbamoyl]-4-cyanophenyl]carbamoyl)cyclohexanecarboxylic acid
Homo sapiens
-
-
0.00000006 - 0.00337
vardenafil
0.0000088 - 0.24
zaprinast
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.000012
-
-
0.00061
-
partially purified PDE5 from N18TG2 neuroblastoma cells
1.44
-
partially purified PDE5 from NG108-15 neuroblastoma cells
20 - 100
-
unactivated purified enzyme
1200 - 1500
-
trypsin-activated enzyme
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
8.3
-
with Tris-acetate as buffer
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 8.5
-
almost no activity at pH 6.0 and 8.5, respectively
6.5 - 8.5
7 - 8
-
3fold increase in activity from pH 7 to pH 8
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
higher expression than in corpus cavernosum
Manually annotated by BRENDA team
-
isoform PDE5
Manually annotated by BRENDA team
-
phosphodiesterase 5 is exclusively detected in smooth muscle cells of the wall, no activity in vascular endothelial layer
Manually annotated by BRENDA team
-
PDE5 is limited to the smooth muscle of the clitoral erectile tissue; presence of isoform PDE5 in smooth muscle of the clitoral erectile tissue
Manually annotated by BRENDA team
-
PDE5A1 and PDE5A3 show an increase from embryonic day 10 to embryonicday18 and from embryonic day 18 to 5-day post-hatching chick. PDE5A2 undergoes a marked increase (about 38fold) in the first period and remains nearly constant between embryonic day 18 and 5-day post-hatching chicken
Manually annotated by BRENDA team
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PDE5
Manually annotated by BRENDA team
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rod outer segment
Manually annotated by BRENDA team
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colon cancer cell
Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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phosphodiesterase 5
Manually annotated by BRENDA team
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phosphodiesterase 5
Manually annotated by BRENDA team
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PDE5 is induced in neuroblastoma-glioma NG108-15 cells after dibutyryl treatment
Manually annotated by BRENDA team
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PFE9A gene expression is higher in neutrophils from sickle cell disease individuals compared to control cells
Manually annotated by BRENDA team
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in freshly isolated peritoneal exudate macrophage, isoform PDE5 is expressed. After 24h of cultures, PDE5 is no longer present
Manually annotated by BRENDA team
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phosphodiesterase 5
Manually annotated by BRENDA team
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PDE5 is expressed in all Purkinje cells
Manually annotated by BRENDA team
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PFE9A gene expression is higher in reticulocytes from sickle cell disease individuals compared to control cells
Manually annotated by BRENDA team