Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(-)-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
-