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Phosphodiesterase 5A Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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SildenafilIC503.6 [1]
SildenafilKi1.6 [1], 1.87 [2], 1.91 [3], 10.0 [4]
TadalafilIC504.0 [1]
TadalafilKi5.2 [1], 10.0 [2]
ZaprinastIC501000.0 [1]
ZaprinastKi130.0 [1]
VardenafilIC500.7 [1]
VardenafilKi0.7 [1], 1.0 [2]
RolipramIC5016000.0 [1]
RolipramKi200000.0 [1]
5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-oneIC5026.92 [1], 27.0 [2], 40.0 [3]
1-(1,3-Benzodioxol-5-yl)-2-[5-(3,4-dimethoxyphenyl)pyrimidin-2-yl]-3,9-dihydro-1H-pyrido[3,4-b]indol-4-oneKi8.0 [1], 8.86 [2]
Sildenafil citrateIC502.2 [1], 3.5 [2], 5.1 [3]
MilrinoneIC50740.0 [1], 100000.0 [2], 110000.0 [3]
1-(3-Chlorophenylamino)-4-phenylphthalazineIC50500.0 [1], 1800.0 [2], 5000.0 [3]
(11R,15S)-4-Benzyl-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC5019.0 [1], 39.0 [2]
(10S,15R)-13-Butyl-10-(4-methoxyphenyl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dioneIC505.0 [1], 5.01 [2]
1-(2,3-Dihydro-1-benzofuran-5-yl)-2-(5-pyridin-2-ylpyridin-2-yl)-1,3,4,9-tetrahydropyrido[3,4-b]indoleKi4.0 [1]
2-(2-Ethoxyphenyl)-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-oneIC505.0 [1], 5.01 [2]
N-DesmethylvardenafilIC500.6 [1], 2.0 [2]
11-Benzyl-7,13-dimethyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50160.0 [1]
5-(2-Ethoxyphenyl)-1,3-dimethyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-oneIC50316.23 [1], 330.0 [2], 331.13 [3]
4-[4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]-N-hydroxycyclohexane-1-carboxamideIC5053.0 [1], 146.0 [2], 190.0 [3]
3-[[4-Ethoxy-3-(3-ethyl-1-methyl-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxycyclobutane-1-carboxamideIC5034.0 [1], 45.0 [2], 60.0 [3]
DipyridamoleIC50520.0 [1], 574.0 [2]
HydroxyhomosildenafilIC501.91 [1], 19.0 [2]
DesmethylsildenafilIC505.7 [1], 5.75 [2]
AvanafilIC506.99 [1]
AvanafilKi5.0 [1]
Sodium;1-[4-(1,3-benzodioxol-5-ylmethylamino)-6-chloroquinazolin-2-yl]piperidine-4-carboxylateIC503.7 [1], 8.6 [2]
PerlolyrineIC509300.0 [1]
CipamfyllineIC5071000.0 [1]
CipamfyllineKi7500.0 [1]
6H-Purin-6-one, 1,7-dihydro-2-(2-propoxyphenyl)-IC5080.0 [1], 1000.0 [2]
2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazineIC50919.0 [1], 920.0 [2]
3-[4-(2-Hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC500.2 [1]
(7R,8S)-2-Benzyl-5-methyl-7,8-propano-7,8-dihydro-3H-imidazo[2,1-b]purin-4(5H)-oneIC5080.0 [1]
3-(4-Hydroxybenzyl)-1-(Thiophen-2-Yl)chromeno[2,3-C]pyrrol-9(2h)-OneIC5017.0 [1]
3-[(4-Hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC500.05 [1]
7-(6-Methoxypyridin-3-yl)-3-(2-morpholin-4-ylethylamino)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC500.07 [1]
(11R,15S)-5-[(3-Bromo-4-hydroxyphenyl)methyl]-8-ethyl-4-methoxy-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC501.58 [1], 1.6 [2]
(7R)-7-Benzyl-3-[(3-chloro-4-hydroxyphenyl)methyl]-5-ethyl-2-phenylmethoxy-7,8-dihydroimidazo[2,1-b]purin-4-oneIC502.09 [1], 2.1 [2]
(7R)-7-Benzyl-3-[(3-chloro-4-hydroxyphenyl)methyl]-5-ethyl-2-methoxy-7,8-dihydroimidazo[2,1-b]purin-4-oneIC501.9 [1], 1.91 [2]
5-[[(7R)-7-Benzyl-5-ethyl-2-methoxy-4-oxo-7,8-dihydroimidazo[2,1-b]purin-3-yl]methyl]-2-methoxybenzonitrileIC5010.96 [1], 11.0 [2]
(7R)-7-Benzyl-3-[(3-bromo-4-hydroxyphenyl)methyl]-5-ethyl-2-methoxy-7,8-dihydroimidazo[2,1-b]purin-4-oneIC501.29 [1], 1.3 [2]
1-(2-Ethoxyethyl)-3-ethyl-5-(piperazin-1-yl)-N-(pyridin-2-yl)-1H-pyrazolo[4,3-d]pyrimidin-7-amineIC500.4 [1]
11-Benzyl-13-methyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50180.0 [1]
3-[2-(2-Hydroxyethylamino)ethylamino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC501.1 [1], 1.12 [2]
7-(6-Methoxypyridin-3-yl)-3-(2-morpholin-4-ylethylamino)-1-(2-propoxyethyl)pyrido[2,3-b]pyrazin-2-oneIC500.34 [1]
1-(4-Fluorobenzyl)-6-(3-carbamoyl-6-propoxyphenyl)-1H-imidazo[4,5-g]quinazoline-8(7H)-oneIC500.48 [1]
3-Ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-(2-methoxyethoxy)pyridin-3-yl]-2-(pyridin-2-ylmethyl)-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC501.3 [1]
1-Benzyl-6-[3-(4-methylpiperazinosulfonyl)-6-propoxyphenyl]-1H-imidazo[4,5-g]quinazoline-8(7H)-oneIC505.3 [1]
Ethoxy-[[1-[3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperidin-4-yl]methyl]phosphinic acidIC500.17 [1], 5888436553555.88 [2]
5-(2-Ethoxyphenyl)-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-oneIC5050.0 [1], 82.0 [2]
2-(5-(4-Methylpiperazin-1-ylsulfonyl)-2-propoxyphenyl)-9-propyl-1H-purin-6(9H)-oneIC5010.0 [1]
5-[5-[4-(Diethoxyphosphorylmethyl)piperazin-1-yl]sulfonyl-2-propoxyphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC500.58 [1], 1737800828749.38 [2]
3-Ethyl-5-[5-(4-ethylpiperazin-1-yl)sulfonyl-2-propoxypyridin-3-yl]-2-(pyridin-2-ylmethyl)-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC501.1 [1]
2-(2-Propoxyphenyl)-9-propyl-1H-purin-6(9H)-oneIC5010.0 [1]
Ethoxy-[[4-[3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperazin-1-yl]methyl]phosphinic acidIC500.18 [1], 5495408738576.25 [2]
Ethoxy-[2-[4-[3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperazin-1-yl]ethyl]phosphinic acidIC500.28 [1], 3548133892335.76 [2]
Ethoxy-[1-[3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperidin-4-yl]phosphinic acidIC500.3 [1], 3311311214825.91 [2]
5-[5-[4-(2-Diethoxyphosphorylethyl)piperazin-1-yl]sulfonyl-2-propoxyphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC501.05 [1], 954992586021.44 [2]
5-[5-(4-Diethoxyphosphorylpiperidin-1-yl)sulfonyl-2-propoxyphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC500.41 [1], 2454708915685.03 [2]
5-[5-[4-(Diethoxyphosphorylmethyl)piperidin-1-yl]sulfonyl-2-propoxyphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-oneIC500.34 [1], 2951209226666.39 [2]
2-[4-[3-(1-Methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperazin-1-yl]ethylphosphonic acidIC500.94 [1], 1071519305237.6 [2]
[1-[3-(1-Methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperidin-4-yl]phosphonic acidIC500.7 [1], 1412537544622.76 [2]
[1-[3-(1-Methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenyl]sulfonylpiperidin-4-yl]methylphosphonic acidIC500.32 [1], 3090295432513.59 [2]
5-[[4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxythiophene-2-carboxamideIC5011.0 [1]
5-[[4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxyfuran-2-carboxamideIC503.0 [1]
5-[[4-Ethoxy-3-(5-methyl-4-oxo-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-2-yl)phenyl]methyl]-N-hydroxythiophene-2-carboxamideIC503.0 [1]
3-(5-Ethylfuran-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-oneIC500.53 [1], 0.54 [2]
3-(5-Ethylthiophen-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-oneIC500.6 [1]
4-(1,3-Benzodioxol-5-ylmethoxy)-6,7,8-trimethoxy-quinazolineIC501000.0 [1]
6-(6-Methoxypyridin-3-yl)-2-(2-morpholin-4-ylethylamino)-4-(2-propoxyethyl)pyrido[2,3-b]pyrazin-3-oneIC502.4 [1], 2.9 [2]
(11R,15S)-4-Benzyl-8-ethyl-5-[(4-hydroxyphenyl)methyl]-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC503.89 [1], 3.9 [2]
(11R,15S)-5-[(3-Bromo-4-methoxyphenyl)methyl]-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC506.46 [1], 6.5 [2]
(11R,15S)-4-Ethoxy-8-ethyl-5-[(4-hydroxyphenyl)methyl]-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC500.89 [1], 0.9 [2]
(11R,15S)-5-[(3-Chloro-4-hydroxyphenyl)methyl]-8-ethyl-4-methoxy-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC502.0 [1]
(11R,15S)-5-[(3-Chloro-4-methoxyphenyl)methyl]-8-ethyl-4-methoxy-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC505.0 [1], 5.01 [2]
(7R)-7-Benzyl-3-[(3-chloro-4-methoxyphenyl)methyl]-5-ethyl-4-oxo-7,8-dihydroimidazo[2,1-b]purine-2-carboxamideIC502.8 [1], 2.82 [2]
3-Benzo[1,3]dioxol-5-ylmethyl-6,7,8-trimethoxy-3H-quinazolin-4-oneIC50530.0 [1]
3-(1,3-Benzodioxol-5-yl)-2-benzoyl-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-oneKi2.49 [1]
(11R,15S)-8-Ethyl-5-[(4-methoxyphenyl)methyl]-7-oxo-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-triene-4-carboxamideIC503.98 [1], 4.0 [2]
(11R,15S)-5-[(3-Chloro-4-hydroxyphenyl)methyl]-8-ethyl-N-methyl-7-oxo-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-triene-4-carboxamideIC501.29 [1], 1.3 [2]
5-[[(7R)-7-Benzyl-5-ethyl-2-methoxy-4-oxo-7,8-dihydroimidazo[2,1-b]purin-3-yl]methyl]-2-hydroxybenzonitrileIC5042.66 [1], 43.0 [2]
(7R)-7-Benzyl-3-[(3-bromo-4-methoxyphenyl)methyl]-5-ethyl-2-methoxy-7,8-dihydroimidazo[2,1-b]purin-4-oneIC502.19 [1], 2.2 [2]
(11R,15S)-5-[(3-Bromo-4-methoxyphenyl)methyl]-8-ethyl-4-methoxy-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC502.8 [1], 2.82 [2]
(11R,15S)-5-[(3-Chloro-4-hydroxyphenyl)methyl]-4-ethoxy-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC502.09 [1], 2.1 [2]
(11R,15S)-5-[(3-Chloro-4-methoxyphenyl)methyl]-4-ethoxy-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC506.46 [1], 6.5 [2]
(11R,15S)-5-[(3-Bromo-4-methoxyphenyl)methyl]-4-ethoxy-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC505.37 [1], 5.4 [2]
(7R)-2,7-Dibenzyl-5-ethyl-7,8-dihydro-3H-imidazo[2,1-b]purin-4-oneIC504.5 [1]
(11R,15S)-5-[(4-Chlorophenyl)methyl]-8-ethyl-4-(2-phenylethynyl)-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC505.0 [1], 5.01 [2]
(11R,15S)-5-(1,3-Benzodioxol-5-ylmethyl)-4-benzyl-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC5045.71 [1], 46.0 [2]
(11R,15S)-4-Benzyl-5-[(3-chloro-4-methoxyphenyl)methyl]-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC5057.54 [1], 58.0 [2]
(11R,15S)-5-[(4-Aminophenyl)methyl]-4-benzyl-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC50549.54 [1], 550.0 [2]
(11R,15S)-4-Benzyl-8-ethyl-5-[(4-methoxyphenyl)methyl]-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC5019.95 [1], 20.0 [2]
(11R,15S)-4-Benzyl-5-[(4-chlorophenyl)methyl]-8-ethyl-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC50158.49 [1], 160.0 [2]
(11R,15S)-4-Benzyl-8-ethyl-5-[(4-methylphenyl)methyl]-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC5039.81 [1], 40.0 [2]
(11R,15S)-8-Ethyl-4-ethylsulfanyl-5-[(4-hydroxyphenyl)methyl]-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-trien-7-oneIC501.8 [1], 1.82 [2]
(11R,15S)-8-Ethyl-5-[(4-hydroxyphenyl)methyl]-7-oxo-1,3,5,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2(6),3,9-triene-4-carboxamideIC502.09 [1], 2.1 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Phosphodiesterase 5A Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Nov. 2024, https://www.aatbio.com/data-sets/phosphodiesterase-5a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 20). Quest Database™ Phosphodiesterase 5A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/phosphodiesterase-5a-inhibitors-ic50-ki.
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