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2'-O-anthraniloyl cGMP + H2O
2'-O-anthraniloyl GMP
-
-
-
?
2'-O-anthraniloyl-cGMP + H2O
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
additional information
?
-
2'-O-anthraniloyl-cGMP + H2O
?
-
phosphorylation increases affinity for hydrolysis of 2'-O-anthraniloyl-cGMP by about 3fold
-
-
?
2'-O-anthraniloyl-cGMP + H2O
?
-
phosphorylation increases affinity for hydrolysis of 2'-O-anthraniloyl-cGMP by about 3fold
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
very low activity
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
allosteric cGMP-binding sites of PDE5 could regulate cGMP signaling by sequestering cGMP from cGMP-dependent protein kinase and perhaps from the PDE5 catalytic site as well. The cGMP sequestered by binding of cGMP to PDE5 R domain significantly dampens activation of cGMP-dependent protein kinase and hydrolysis of cGMP by PDE5 C domain
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE5 and PDE6 show specificity for cGMP relative to cAMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
specific for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
667547, 691533, 691945, 692724, 693333, 694879, 710776, 711409, 711619, 711841, 711934, 711948, 712091, 713068, 750045 -
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE5A1
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
selective for 3',5'-cGMP, PDE9
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
specific for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
PDE5 hydrolyses selectively 3',5'-cGMP with high affinity
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE5 is cGMP-specific
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE6 shows specificity for cGMP relative to cAMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
specific for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE5 is specific for cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
PDE5A has a higher selectivity for cGMP due to much lower cAMP binding affinity
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
Q2V2M6
specific for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
135314, 135340, 691558, 694285, 711626, 711687, 711772, 711773, 711829, 711920, 711923, 712621, 712815, 713199, 750479 -
-
?
3',5'-cGMP + H2O
5'-GMP
PDE5 specifically targets 3',5'-cyclic GMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
suPDE5 regulates cGMP levels in sperm, which in turn modulate sperm motility
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
specific for 3',5'-cGMP, no activity with 3',5'-cAMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
-
PDE5
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
-
phosphodiesterase 5 converts the second messenger 3',5'-cGMP to its inactive form
-
-
?
cGMP + H2O
5'-GMP
-
degradation of intracellular cGMP
-
-
?
cGMP + H2O
5'-GMP
-
-
-
?
cGMP + H2O
5'-GMP
-
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
very low activity with cAMP
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
-
?
additional information
?
-
-
preincubation with cGMP increases catalytic activity for cGMP degradation, thus elevated cellular cGMP initiates a physiological negative feedback on the cGMP pathway by increasing the affinity of the PDE5 catalytic site for cGMP
-
-
?
additional information
?
-
-
tadalafil is not degraded by PDE5
-
-
?
additional information
?
-
-
analysis of diverse complxes formed by subunits Pgamma with GTP or GDP and outer segments, the complexes are extracted from membranes and isolated. Analysis of the function of the single complexes in PDE regulation, overview
-
-
?
additional information
?
-
-
interaction between the PDE6 gamma subunit with tubulin alpha and beta, specificity and mechanism, detailed overview
-
-
?
additional information
?
-
-
prenylation of the enzyme is required for plasma-membrane targeting
-
-
?
additional information
?
-
Drosophila sp. (in: flies)
-
role for cG-PDE in modulating cGMP transport and efflux
-
-
?
additional information
?
-
PDE6 contains two regulatory GAF domains, of which one (GAF A) binds cGMP and regulates the activity of the PDE6 holoenzyme
-
-
?
additional information
?
-
-
PDE6 contains two regulatory GAF domains, of which one (GAF A) binds cGMP and regulates the activity of the PDE6 holoenzyme
-
-
?
additional information
?
-
-
human chorionic gonadotropin reduces PDE5 expression and enzyme activity in smooth muscle cells, possibly through a pathway involving cAMP
-
-
?
additional information
?
-
-
PDE5 gene expression and activity are androgen-dependent in vas deferens
-
-
?
additional information
?
-
-
PDE5 may be involved in the cyclic nucleotide-mediated control of smooth muscle tone
-
-
?
additional information
?
-
-
PDE5 regulation of cGMP intracellular levels is not involved in the control of progression of smooth muscle cell cycle, but may represent one of the markers of the contractile phenotype
-
-
?
additional information
?
-
-
isoform PDE5 regulation of cGMP intracellular levels is not involved in the control of smooth muscle cell cycle progression, but may represent one of the markers of the contractile phenotype
-
-
?
additional information
?
-
-
tadalafil is not degraded by PDE5
-
-
?
additional information
?
-
-
PDE5 in Pukinje neurons may play a role in limiting the cGMP-mediated long-term depression response
-
-
?
additional information
?
-
-
interaction between the PDE6 gamma subunit with tubulin alpha and beta, specificity and mechanism, detailed overview
-
-
?
additional information
?
-
-
PDE5 gene expression and activity are androgen-dependent in vas deferens
-
-
?
additional information
?
-
-
in mammals the enzyme might play key roles in the aquisition and maintenance of the myoid cell contractile phenotype and more generally in the testis maturation
-
-
?
additional information
?
-
-
kinetics of a cellular nitric oxide/cGMP/phosphodiesterase-5 pathway
-
-
?
additional information
?
-
-
PDE5 controls the soluble but not the particulate pool of cGMP in rat cardiomyocytes
-
-
?
additional information
?
-
cGMP levels in the spinal cord are controlled by a number of enzyme isoforms, that can be present in the same cell. Role of NO-cGMP signaling in nociceptive processing
-
-
?
additional information
?
-
-
isoform PDE5 regulates bladder smooth muscle tone, strongly limiting the nitric oxide/cGMP signaling
-
-
?
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(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0121 mM, PDE5
(1R,3S)-2-acetyl-1-(2H-1,3-benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-b-carboline-3-carboxylate
ZINC03024617
(1S,3R)-2-acetyl-1-(2H-1,3-benzodioxol-5-yl)-2,3,4,9-tetrahydro-1H-b-carboline-3-carboxylate
ZINC03024615
(1S,3S,4aS,9aR)-1-(2H-1,3-benzodioxol-5-yl)-2-(chloroacetyl)-2,3,4,4a,9,9a-hexahydro-1H-b-carboline-3-carboperoxoic acid
ZINC21986065
(2R)-4-[(2H-1,3-benzodioxol-5-yl)methyl]-1-(3-methoxybenzoyl)-N-methylpiperazine-2-carboxamide
ZINC24891165
(2R)-N-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-(methylsulfanyl)butanamide
ZINC32995888
(2S)-N-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl]-2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-4-(methylsulfanyl)butanamide
ZINC32995890
(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
(3R)-1-(2H-1,3-benzodioxole-5-carbonyl)-4-(2-methoxyphenyl)-N-[(pyridin-3-yl)methyl]pyrrolidine-3-carboxamide
ZINC36055139
(3S)-N-[(2,3-dihydro-1,4-benzodioxin-6-yl)methyl]-2-(furan-2-carbonyl)-N-methyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
ZINC23055991
(4-(4-[2-ethyl-phenylamino)-methylene]-3-methyl-5-oxo-4,5-dihydro-pyrazol-1-yl)-benzoic acid
-
0.00001 mM, 50% inhibition
(6R,12aR)-2-propyl-6-(3,4,5-trimethoxyphenyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC02092043
(6R,12aR)-6-(2H-1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC12360812
(6R,12aR)-6-(4-ethoxy-3-methoxyphenyl)-2-(2-methylpropyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC15955458
(6R,12aS)-2-methyl-6-(3,4,5-trimethoxyphenyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC16031243; ZINC16042566
(6R,12aS)-2-propyl-6-(3,4,5-trimethoxyphenyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC11692256
(6R,12aS)-6-(4-ethoxy-3-methoxyphenyl)-2-(3-methylbutyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC02120502
(6S,12aR)-2-benzyl-6-(3,4-dimethoxyphenyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC16043001
(6S,12aS)-2-methyl-6-(3,4,5-trimethoxyphenyl)-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC02093785
(6S,12aS)-2-[(furan-2-yl)methyl]-6-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC00490454
(6S,12aS)-2-[2-(3,4-dimethoxyphenyl)ethyl]-6-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC26772005
(6S,12aS)-6-(2H-1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
ZINC08204637
(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
-
-
1-benzyl-2-[4-[2-(2-phenyl-1H-benzimidazol-1-yl)ethoxy]phenyl]-1H-benzimidazole
-
-
1-benzyl-2-[4-[2-cyclohexyl-2-(2-phenyl-1H-benzimidazol-1-yl)ethoxy]phenyl]-1H-benzimidazole
-
-
1-[(3R)-1-(2H-1,3-benzodioxol-5-yl)-5-oxopyrrolidine-3-carbonyl]-N-(4-methoxyphenyl)-L-prolinamide
ZINC40146722
1-[4-[(1,3-benzodioxol-5-ylmethyl)amino]-6-chloroquinazolin-2-yl]piperidine-4-carboxylic acid
-
-
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
-
-
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
-
-
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
trivial name sildenafil citrate or Viagra
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
-
-
2-(2-ethoxyphenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
-
-
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
-
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
-
-
2-(5-amino-2-propoxyphenyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
-
2-(5-[[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl]-2-propoxyphenyl)-5-methylquinazolin-4(3H)-one
-
-
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
-
IC50: 0.0027 mM, PDE5
2-methoxy-7-methyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazin-6(5H)-one
-
-
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
-
IC50: 0.002 mM, PDE5
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
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
-
vardenafil
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
-
-
3-(4-ethylpiperazin-1-yl)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
3-(cyclopentylmethoxy)-N-(2,6-dichlorophenyl)-4-methoxybenzamide
-
piclamilast
3-(cyclopropylmethoxy)-N-(2,6-dichlorophenyl)-4-(difluoromethoxy)benzamide
-
roflumilast
3-([2-[(2-hydroxyethyl)amino]ethyl]amino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
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
-
-
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
-
-
3-ethyl-5-(piperazin-1-yl)-1-(2-propoxyethyl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
3-ethyl-5-(piperazin-1-yl)-1-[2-(propan-2-yloxy)ethyl]-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
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
-
-
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
-
-
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
-
-
3-ethyl-N-(4-fluorophenyl)-5-(piperazin-1-yl)-1-[2-(2,2,2-trifluoroethoxy)ethyl]-1H-pyrazolo[4,3-d]pyrimidin-7-amine
-
-
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
-
-
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
-
-
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
-
-
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
-
-
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
-
-
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
-
-
3-[(2-aminoethyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
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
-
-
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 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
cAMP
-
inhibition at high concentrations
cGMP
-
inhibition above 0.001 mM
chamomile
-
weak, but still statistically significant inhibition of PDE5A1
cilostazol
-
IC50: 0.0044 mM, PDE5
cone Pgamma subunit
-
PDE6C is potently inhibited by the recombinant cone and rod Pgamma-subunits with slight selectivity for the cone Pgamma
-
delphinidin 3-glucoside
-
-
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
Evo48
-
potent inhibitor of PDE5
-
fructose 1,6-bisphosphate
-
-
genistein
-
IC50: 0.073 mM, PDB5
ginkgetin
-
IC50: 0.00059 mM
GTP
-
slight inhibition at 1 mM
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
methyl 2-[(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-carboxylate
ZINC29158966
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-[(1S)-1-[1-(2H-1,3-benzodioxole-5-carbonyl)piperidin-4-yl]-2-oxo-2-(pyrrolidin-1-yl)ethyl]-2-methylbenzamide
ZINC36210867
N-[(S)-[(3R)-1-(2H-1,3-benzodioxole-5-carbonyl)piperidin-3-yl](pyridin-2-yl)methyl]acetamide
ZINC19020327
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
-
-
N-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl]-4-(2,5-dioxopyrrolidin-1-yl)-N-methylbenzamide
ZINC23183710
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
-
-
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
-
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
-
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 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
T0156
-
selective phosphodiesterase type 5 inhibitor
trans-4-([2-[(3-chloro-4-methoxyphenyl)carbamoyl]-4-cyanophenyl]carbamoyl)cyclohexanecarboxylic acid
-
-
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
[4-[(1S,2S)-2-(2H-1,3-benzodioxol-5-yl)cyclopropane-1-carbonyl]piperazin-1-yl](1H-indol-2-yl)methanone
ZINC44448076
[4-[(1S,2S)-2-(2H-1,3-benzodioxol-5-yl)cyclopropane-1-carbonyl]piperazin-1-yl](1H-indol-3-yl)methanone
ZINC44448130
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
-
i.e. BAY 73-6691, IC50: 55 nM
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
i.e. BAY 73-6691, IC50: 100 nM
3',5'-cAMP
-
-
3',5'-cAMP
-
20% inhibition at 0.1 mM, 50% inhibition at 1 mM
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
0.0058 mM, 50% inhibition
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
0.06 mM, 50% inhibition
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
0.0058 mM, 50% inhibition
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
the inhibitor binds to a subpocket that comprises key residues Val782, Ph2786, Gln817 and Phe820 of PDE5A1. This subpocket may be a common site for binding nonselective inhibitors
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
IBMX, a PDE6 inhibitor
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
0.0054 mM, 50% inhibition
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
IC50: 0.032 mM
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
-
Caffeine
-
-
carboxyamidotriazole
-
non-selective inhibition
carboxyamidotriazole
-
non-selective inhibition
Cilostamide
-
-
Cilostamide
-
IC50: 0.0152 mM, PDE5
Cilostamide
-
IC50: 0.006 mM, PDE5
dipyridamole
-
-
dipyridamole
-
IC50: 0.00026 mM, PDE5
dipyridamole
-
0.0013 mM, 50% inhibition
dipyridamole
-
0.00075 mM, 50% inhibition
dipyridamole
PDE5 is specifically inhibited by dipyridamole
dipyridamole
-
0.0012 mM, 50% inhibition
dipyridamole
Q2V2M6
IC50: 0.022 mM
dipyridamole
-
IC50: 0.023 mM
E4021
-
-
E4021
Q2V2M6
IC50: 0.046 mM
EDTA
-
completely inhibits at 10 mM
EDTA
0.5 mM, 35% inhibition of activity in the absence of a divalent metal ion
Inhibitor protein
-
gamma-subunit of enzyme
-
Inhibitor protein
-
gamma-subunit of enzyme; inhibitory in the dark
-
Inhibitor protein
-
gamma-subunit of enzyme
-
Inhibitor protein
-
gamma-subunit of enzyme; inhibitory in the dark
-
Inhibitor protein
-
gamma-subunit of enzyme
-
Inhibitor protein
-
gamma-subunit of enzyme
-
Inhibitor protein
-
gamma-subunit of enzyme
-
rolipram
-
-
sildenafil
-
IC50: 49 nM, PDE6
sildenafil
-
IC50: 3.7 nM
sildenafil
-
preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor
sildenafil
-
0.0000017 mM, 50% inhibition
sildenafil
-
IC50: 3.6 nM
sildenafil
-
IC50: IC50: 0.000025 mM
sildenafil
0.011 mM, 50% inhibition of PDE9A5, 0.008 mM, 50% inhibition of PDE9A1
sildenafil
-
0.0000036 mM, 50% inhibition
sildenafil
-
IC50: 8.5 nM, PDE5; IC50: above 10000 nM, PDE9
sildenafil
-
IC50: 3.7 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
sildenafil
-
binding to the active site
sildenafil
-
blocking of 70% of total cGMP hydrolizing activity
sildenafil
-
70% inhibition at 100 nM
sildenafil
-
potent competitive inhibitor of phosphodiesterase 5
sildenafil
-
high sensitivity of PDE5 for sildenafil can be obtained through cGMP-induced activation of PDE or through cGMP-independent modulation of PDE5 in the nonactivated state
sildenafil
-
0.0000035 mM, 50% inhibition
sildenafil
potent PDE5 inhibitor
sildenafil
-
potent inhibitor of phosphodiesterase-5
sildenafil
-
0.000003 mM, 50% inhibition
sildenafil
-
IC50: 7.8 nM
sildenafil
Q2V2M6
IC50: 0.056 mM
sildenafil
-
pharmacologic inhibition of PDE5 in uterus blunts myometrical contractility during active labor without a significant cardiovascular effect. Potential role for sildenafil as an adjunct for the treatment of preterm labor
sildenafil
-
inhibition significantly increases contractility in hypertrophied myocardium
sildenafil
-
blocking of 70% of total cGMP hydrolizing activity
sildenafil
UK-92,480, trade name Viagra
sildenafil
-
commercial name Viagra
sildenafil
-
selective PDE5 inhibitor
sildenafil
-
PDE5 inhibitor
sildenafil
-
specific PDE5 inhibitor
sildenafil
-
a PDE5 inhibitor, reduces phenylephrine-induced maximal contraction similarly in angiotensin II and control rats
sildenafil
-
IC50: 0.005 mM
sildenafil
-
nerve-induced relaxation of urethral preparations are enhanced at low concentrations of sildenafil, with direct smooth muscle-relaxant actions of the inhibitors at high concentrations
sildenafil
0.01 mM sildenafil inhibits 84% and 68% of the activity measured in detergent-resistant membranes and detergent-soluble fractions, respectively; 0.01 mM sildenafil inhibits 84% and 68% of the activity measured in detergent-resistant membranes and detergent-soluble fractions, respectively
tadalafil
-
IC50: 1.8 nM
tadalafil
-
preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor
tadalafil
-
cGMP modestly but significantly increases the affinity of PDE5 for tadalafil by 1.7fold
tadalafil
-
IC50: 9.4 nM, PDE5; IC50: above 10000 nM, PDE9
tadalafil
-
IC50: 1.8 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
tadalafil
-
blocking of 70% of total cGMP hydrolizing activity
tadalafil
-
cGMP modestly but significantly increases the affinity of PDE5 for tadalafil by 1.7fold
tadalafil
potent PDE5 inhibitor
tadalafil
-
blocking of 70% of total cGMP hydrolizing activity
tadalafil
-
commercial name Cialis
tadalafil
-
nerve-induced relaxation of urethral preparations are enhanced at low concentrations of tadalafil, with direct smooth muscle-relaxant actions of the inhibitors at high concentrations
theophylline
-
-
udenafil
-
trade name Zydena, a PDE5 inhibitor developed as a medical treatment for erectile dysfunction
udenafil
-
DA-8159 or Zydena, potent PDE5 inhibitor
vardenafil
-
IC50: 11 nM, PDE6
vardenafil
-
IC50: 0.091 nM
vardenafil
-
preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor
vardenafil
-
IC50: 0.89 nM, PDE5; IC50: 3370 nM, PDE9
vardenafil
-
IC50: 0.091 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
vardenafil
-
blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme
vardenafil
-
vardenafil inhibits the activity of PDE-5 and results in relaxation of smooth muscle
vardenafil
potent PDE5 inhibitor
vardenafil
-
blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme
vardenafil
-
selective inhibitor of phosphodiesterase-5
vardenafil
-
nerve-induced relaxation of urethral preparations are enhanced at low concentrations of vardenafil, with direct smooth muscle-relaxant actions of the inhibitors at high concentrations
zaprinast
-
-
zaprinast
-
0.0002 mM, 50% inhibition
zaprinast
-
IC50: 0.00065 mM
zaprinast
Drosophila sp. (in: flies)
-
-
zaprinast
0.046 mM, 50% inhibition of PDE9A5, 0.043 mM, 50% inhibition of PDE9A1
zaprinast
-
0.0003 mM, 50% inhibition
zaprinast
-
0.0006 mM, 50% inhibition
zaprinast
-
0.000053 mM, 50% inhibition
zaprinast
Q2V2M6
IC50: 0.0038 mM for wild-type enzyme and 0.0056 for mutant enzyme G788A
zaprinast
-
0.00046 mM, 50% inhibition in sham-operated rats
zaprinast
-
IC50: 0.24 mM
Zn2+
-
complete inhibition above 0.1 mM
Zn2+
-
strong inhibition above 0.01 mM, almost complete inhibition at 0.1 mM
Zn2+
-
strong inhibition above 0.01 mM, complete inhibition at 0.1 mM
additional information
-
not inhibited by quercetin, quercetin-3,7,3',4'-O-tetramethylether, quercetin-3,5,7,3',4'-O-pentaacetate, and quercetin-3,7,4'-O-trimethylether
-
additional information
-
recombinant and native PDE6s exhibit differential sensitivity to inhibitors. This data caution the use of recombinant catalytic subunits of PDE6 in drug discovery or in structural/functional studies
-
additional information
-
red wine and extract from grape skin inhibit isoenzyme PDE5A1 activity, seed extract has negligible effect. Polyphenol-induced vasorelexation may be sustained by smooth muscle PDE inhibition by anthocyanins present in red wines and grapes. trans-Resveratrol and trans-piceid exhibit negligible effects. hydroxycinnamates are completely inactive
-
additional information
-
Gingko biloba dimeric flavonoids inhibit the cGMP-specific PDE5A1
-
additional information
Q2V2M6
3-isobutyl-1-methylxanthine, theophylline and the antimalarial chloroquine show IC50-value of over 0.1 mM
-
additional information
-
3-isobutyl-1-methylxanthine, theophylline and the antimalarial chloroquine show IC50-value of over 0.1 mM
-
additional information
-
not affected by cilostazol and rolipram
-
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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
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
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
0.000176
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
30°C, pH 7.4, native PDE6
0.0003616
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
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
-
30°C, pH 7.4, recombinant cone PDE6alpha'
0.0000487
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.0000546
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione
-
30°C, pH 7.4, recombinant cone PDE6alpha'
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
-
30°C, pH 7.4, native PDE6
0.0085
3-isobutyl-1-methylxanthine
-
chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication
0.01212
3-isobutyl-1-methylxanthine
-
30°C, pH 7.4, native PDE6
0.06084
3-isobutyl-1-methylxanthine
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.09485
3-isobutyl-1-methylxanthine
-
30°C, pH 7.4, recombinant
0.0000173
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
30°C, pH 7.4, native PDE6
0.001206
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.001605
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one
-
30°C, pH 7.4, recombinant cone PDE6alpha'
0.0000026
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.0000036
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
-
30°C, pH 7.4, recombinant cone PDE6alpha'
0.0000183
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione
-
30°C, pH 7.4, native PDE6
0.078
cone Pgamma subunit
-
recombinant human cone PDE6C, pH and temperature not specified in the publication
-
0.14
cone Pgamma subunit
-
recombinant human cone PDE6AB, pH and temperature not specified in the publication
-
0.0000035
E4021
-
30°C, pH 7.4, native PDE6
0.0001014
E4021
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.0001735
E4021
-
30°C, pH 7.4, recombinant cone PDE6alpha'
0.105
rod Pgamma subunit
-
recombinant human cone PDE6AB, pH and temperature not specified in the publication
-
0.155
rod Pgamma subunit
-
recombinant human cone PDE6C, pH and temperature not specified in the publication
-
0.000013
sildenafil
-
37°C, pH 7.4, recombinant isoenzyme PDE5A3
0.000014
sildenafil
-
37°C, pH 7.4, recombinant isoenzyme PDE5A2
0.0000245
sildenafil
-
30°C, pH 7.4, native PDE6
0.000025
sildenafil
-
chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication
0.000028
sildenafil
-
37°C, pH 7.4, recombinant isoenzyme PDE5A1
0.0000936
sildenafil
-
30°C, pH 7.4, recombinant rod PDE6alphabeta
0.0000984
sildenafil
-
30°C, pH 7.4, recombinant cone PDE6alpha'
0.0001778
zaprinast
-
30°C, pH 7.4, native PDE6
0.00031
zaprinast
-
sham-operated rats
0.0013
zaprinast
-
37°C, pH 7.4, recombinant isoenzyme PDE5A2
0.0016
zaprinast
-
37°C, pH 7.4, recombinant isoenzyme PDE5A3
0.0032
zaprinast
-
37°C, pH 7.4, recombinant isoenzyme PDE5A1
0.01145
zaprinast
-
30°C, pH 7.4 cone PDE6alpha'
0.01438
zaprinast
-
30°C, pH 7.4 rod PDE6alphabeta
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
-
-
0.002
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
Homo sapiens
-
IC50: 0.002 mM, PDE5
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
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
Rattus norvegicus
-
pH and temperature not specified in the publication
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
0.000429 - 0.0115
carboxyamidotriazole
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
0.000055
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
Homo sapiens
-
i.e. BAY 73-6691, IC50: 55 nM
0.0001
1-(2-chlorophenyl)-6-((2R)-3,3,3-trifluoro-2-methylpropyl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
Mus musculus
i.e. BAY 73-6691, IC50: 100 nM
0.0000019
3-isobutyl-1-methylxanthine
Homo sapiens
mutant Y612F, pH 7.5, 30°C
0.000003
3-isobutyl-1-methylxanthine
Homo sapiens
mutant L765A, pH 7.5, 30°C
0.0000035
3-isobutyl-1-methylxanthine
Homo sapiens
wild-type, pH 7.5, 30°C
0.0000423
3-isobutyl-1-methylxanthine
Homo sapiens
mutant H613A, pH 7.5, 30°C
0.0000425
3-isobutyl-1-methylxanthine
Homo sapiens
mutant V782A, pH 7.5, 30°C
0.0000433
3-isobutyl-1-methylxanthine
Homo sapiens
mutant F786A, pH 7.5, 30°C
0.000152
3-isobutyl-1-methylxanthine
Homo sapiens
mutant Y612A, pH 7.5, 30°C
0.000214
3-isobutyl-1-methylxanthine
Homo sapiens
mutant Q817A, pH 7.5, 30°C
0.000327
3-isobutyl-1-methylxanthine
Homo sapiens
mutant F820A, pH 7.5, 30°C
0.032
3-isobutyl-1-methylxanthine
Strongylocentrotus purpuratus
-
IC50: 0.032 mM
0.0000011
benzamidenafil
Homo sapiens
-
PDE-5, pH and temperature not specified in the publication
0.00002
benzamidenafil
Homo sapiens
-
PDE-6, pH and temperature not specified in the publication
0.000429
carboxyamidotriazole
Mus musculus
-
enzyme from lung, at pH 8.0 and 30°C
0.00267
carboxyamidotriazole
Mus musculus
-
enzyme from peritoneal macrophage, at pH 8.0 and 30°C
0.00475
carboxyamidotriazole
Rattus norvegicus
-
enzyme from brain, at pH 8.0 and 30°C
0.00705
carboxyamidotriazole
Mus musculus
-
enzyme from RAW264.7 cells, at pH 8.0 and 30°C
0.00898
carboxyamidotriazole
Mus musculus
-
enzyme from Lewis lung carcinoma cells, at pH 8.0 and 30°C
0.0115
carboxyamidotriazole
Mus musculus
-
enzyme from L1210 cells, at pH 8.0 and 30°C
0.0000405
Cilostamide
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.006
Cilostamide
Homo sapiens
-
IC50: 0.006 mM, PDE5
0.0152
Cilostamide
Bos taurus
-
IC50: 0.0152 mM, PDE5
0.0000109
dipyridamole
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.00026
dipyridamole
Bos taurus
-
IC50: 0.00026 mM, PDE5
0.022
dipyridamole
Plasmodium falciparum
Q2V2M6
IC50: 0.022 mM
0.023
dipyridamole
Strongylocentrotus purpuratus
-
IC50: 0.023 mM
0.0000013
sildenafil
Homo sapiens
mutant Y612F, pH 7.5, 30°C
0.0000016
sildenafil
Homo sapiens
-
non-activated PDE5 from blood platelets, at 0.0001 mM cGMP, at pH 7.5 and 30°C
0.00000193
sildenafil
Mus musculus
-
enzyme from lung, at pH 8.0 and 30°C
0.000002
sildenafil
Bos taurus
-
isoform PDE5, pH and temperature not specified in the publication
0.0000032
sildenafil
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.0000033
sildenafil
Homo sapiens
wild-type, pH 7.5, 30°C
0.0000036
sildenafil
Canis lupus familiaris
-
IC50: 3.6 nM
0.0000037
sildenafil
Bos taurus
-
IC50: 3.7 nM
0.0000037
sildenafil
Homo sapiens
-
IC50: 3.7 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
0.0000043
sildenafil
Homo sapiens
-
PDE-5, pH and temperature not specified in the publication
0.000005
sildenafil
Homo sapiens
-
cGMP-activated PDE5 from blood platelets, at 0.0001 mM cGMP, at pH 7.5 and 30°C
0.0000078
sildenafil
Oryctolagus cuniculus
-
IC50: 7.8 nM
0.0000085
sildenafil
Homo sapiens
-
IC50: 8.5 nM, PDE5
0.0000101
sildenafil
Homo sapiens
mutant L765A, pH 7.5, 30°C
0.0000132
sildenafil
Homo sapiens
mutant H613A, pH 7.5, 30°C
0.000015
sildenafil
Homo sapiens
-
PDE-6, pH and temperature not specified in the publication
0.0000206
sildenafil
Homo sapiens
mutant F786A, pH 7.5, 30°C
0.000025
sildenafil
Drosophila melanogaster
-
IC50: 0.000025 mM
0.0000319
sildenafil
Homo sapiens
mutant V782A, pH 7.5, 30°C
0.000049
sildenafil
Bos taurus
-
IC50: 49 nM, PDE6
0.0000983
sildenafil
Homo sapiens
mutant Y612A, pH 7.5, 30°C
0.000141
sildenafil
Homo sapiens
mutant Q817A, pH 7.5, 30°C
0.000235
sildenafil
Homo sapiens
mutant F820A, pH 7.5, 30°C
0.00127
sildenafil
Mus musculus
-
enzyme from Lewis lung carcinoma cells, at pH 8.0 and 30°C
0.00185
sildenafil
Rattus norvegicus
-
enzyme from brain, at pH 8.0 and 30°C
0.00301
sildenafil
Mus musculus
-
enzyme from L1210 cells, at pH 8.0 and 30°C
0.00332
sildenafil
Mus musculus
-
enzyme from RAW264.7 cells, at pH 8.0 and 30°C
0.00436
sildenafil
Mus musculus
-
enzyme from peritoneal macrophage, at pH 8.0 and 30°C
0.005
sildenafil
Strongylocentrotus purpuratus
-
IC50: 0.005 mM
0.01
sildenafil
Homo sapiens
-
IC50: above 10000 nM, PDE9
0.056
sildenafil
Plasmodium falciparum
Q2V2M6
IC50: 0.056 mM
0.0000018
tadalafil
Bos taurus
-
IC50: 1.8 nM
0.0000018
tadalafil
Homo sapiens
-
IC50: 1.8 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
0.0000022
tadalafil
Homo sapiens
wild-type, pH 7.5, 30°C
0.0000058
tadalafil
Homo sapiens
mutant Y612F, pH 7.5, 30°C
0.00000607
tadalafil
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.0000067
tadalafil
Homo sapiens
mutant V782A, pH 7.5, 30°C
0.0000091
tadalafil
Homo sapiens
mutant L765A, pH 7.5, 30°C
0.0000094
tadalafil
Homo sapiens
-
IC50: 9.4 nM, PDE5
0.0000375
tadalafil
Homo sapiens
mutant F786A, pH 7.5, 30°C
0.000081
tadalafil
Homo sapiens
mutant H613A, pH 7.5, 30°C
0.000112
tadalafil
Homo sapiens
mutant Y612A, pH 7.5, 30°C
0.00021
tadalafil
Homo sapiens
mutant Q817A, pH 7.5, 30°C
0.000301
tadalafil
Homo sapiens
mutant F820A, pH 7.5, 30°C
0.01
tadalafil
Homo sapiens
-
IC50: above 10000 nM, PDE9
0.00000006
vardenafil
Homo sapiens
mutant Y612F, pH 7.5, 30°C
0.000000091
vardenafil
Bos taurus
-
IC50: 0.091 nM
0.00000012
vardenafil
Homo sapiens
wild-type, pH 7.5, 30°C
0.0000003
vardenafil
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.00000049
vardenafil
Homo sapiens
mutant L765A, pH 7.5, 30°C
0.00000078
vardenafil
Homo sapiens
mutant H613A, pH 7.5, 30°C
0.00000083
vardenafil
Homo sapiens
mutant F786A, pH 7.5, 30°C
0.00000089
vardenafil
Homo sapiens
-
IC50: 0.89 nM, PDE5
0.000011
vardenafil
Bos taurus
-
IC50: 11 nM, PDE6
0.0000147
vardenafil
Homo sapiens
mutant Y612A, pH 7.5, 30°C
0.0000275
vardenafil
Homo sapiens
mutant V782A, pH 7.5, 30°C
0.0000537
vardenafil
Homo sapiens
mutant F820A, pH 7.5, 30°C
0.0000613
vardenafil
Homo sapiens
mutant Q817A, pH 7.5, 30°C
0.000091
vardenafil
Homo sapiens
-
IC50: 0.091 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication
0.00337
vardenafil
Homo sapiens
-
IC50: 3370 nM, PDE9
0.0000088
zaprinast
Homo sapiens
-
bladder homogenate, 30°C, pH 7.0
0.00013
zaprinast
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00065
zaprinast
Drosophila melanogaster
-
IC50: 0.00065 mM
0.0023
zaprinast
Cavia porcellus
-
PDE5
0.0038
zaprinast
Plasmodium falciparum
Q2V2M6
IC50: 0.0038 mM for wild-type enzyme and 0.0056 for mutant enzyme G788A
0.24
zaprinast
Strongylocentrotus purpuratus
-
IC50: 0.24 mM
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