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Phosphodiesterase 8A 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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SildenafilIC5010000.0 [1], 100000.0 [2]
2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazineIC505000.0 [1]
TadalafilIC5010000.0 [1]
RolipramIC5016000.0 [1]
(2S,3R)-3-(6-Amino-9H-purin-9-yl)nonan-2-olIC5016000.0 [1]
8-[(4-Chlorophenyl)methyl]-10-thia-3,5,6,8-tetrazatetracyclo[7.7.0.02,6.011,16]hexadeca-1(9),2,4,11(16)-tetraen-7-oneIC5010000.0 [1]
4-(4-((8-(3-(Difluoromethoxy)phenyl)quinolin-6-yl)methoxy)phenyl)-2-methylbutan-2-olIC5029000.0 [1]
3-[4-(2-Hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
3-[(4-Hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
7-(6-Methoxypyridin-3-yl)-3-(2-morpholin-4-ylethylamino)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2-oneIC502000.0 [1]
CID 46239428Ki10000.0 [1]
N-[(1S)-1-[3-Fluoro-4-(trifluoromethoxy)phenyl]-2-methoxyethyl]-7-methoxy-2-oxo-1,3-dihydropyrido[2,3-b]pyrazine-4-carboxamideIC5030000.0 [1]
N-(12-Methoxy-5-methyl-3-propyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-7-yl)methanesulfonamideIC501000.0 [1]
6,8-Dimethoxy-3,4-dimethyl-1-(3-methylpyridin-4-yl)imidazo[1,5-a]quinoxalineIC5010000.0 [1]
6-Methoxy-3,8-Dimethyl-4-(Morpholin-4-Ylmethyl)-1h-Pyrazolo[3,4-B]quinolineKi10000.0 [1]
[1-(3-{[1-(Quinolin-2-Yl)azetidin-3-Yl]oxy}pyrazin-2-Yl)piperidin-4-Yl]methanolIC5030000.0 [1]
(11R,15S)-5-Anilino-4-[[4-(6-fluoropyridin-2-yl)phenyl]methyl]-8-methyl-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-one;phosphoric acidKi3000.0 [1]
5-Methyl-6-oxo-N-(1,3,4-thiadiazol-2-yl)-7H-furo[2,3-f]indole-7-carboxamideIC5016000.0 [1]
2-Oxo-N-[1-[4-(trifluoromethoxy)phenyl]propyl]-1,3-dihydropyrido[2,3-b]pyrazine-4-carboxamideIC5010000.0 [1]
(3-Bromo-4-fluorophenyl)-[(5S)-3,3-difluoro-5-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperidin-1-yl]methanoneIC5010000.0 [1]
(11R,15S)-5-Anilino-8-methyl-4-[(4-pyridin-2-ylphenyl)methyl]-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-oneKi8200.0 [1]
(11R,15S)-5-Anilino-8-methyl-4-[(4-phenylphenyl)methyl]-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-oneKi33000.0 [1]
(11R,15S)-5-Anilino-8-methyl-4-[[4-(trifluoromethyl)phenyl]methyl]-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-oneKi54000.0 [1]
(11R,15S)-5-Anilino-8-methyl-4-[[6-(trifluoromethyl)pyridin-3-yl]methyl]-1,3,4,8,10-pentazatetracyclo[7.6.0.02,6.011,15]pentadeca-2,5,9-trien-7-oneKi100000.0 [1]
3-Cyclopentyloxy-4-(difluoromethoxy)-N-[(4-methoxyphenyl)methyl]benzamideIC50100000.0 [1]
8-Bromo-1-(6-fluoropyridin-3-yl)-6-methoxy-3,4-dimethylimidazo[1,5-a]quinoxalineIC501000.0 [1]
1,8-Bis(6-fluoropyridin-3-yl)-6-methoxy-3,4-dimethylimidazo[1,5-a]quinoxalineIC501000.0 [1]
8-Bromo-1-(2-fluoropyridin-3-yl)-6-methoxy-3,4-dimethylimidazo[1,5-a]quinoxalineIC501000.0 [1]
6-Methoxy-3,4-dimethyl-1,8-dipyridin-3-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
8-(6-Fluoropyridin-3-yl)-6-methoxy-3,4-dimethyl-1-pyridin-4-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
8-(6-Fluoropyridin-3-yl)-6-methoxy-3,4-dimethyl-1-pyridin-3-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
1-(6-Fluoropyridin-3-yl)-6-methoxy-3,4-dimethyl-8-pyridin-4-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
1-(6-Fluoropyridin-3-yl)-6-methoxy-3,4-dimethyl-8-pyridin-3-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
1-(2-Fluoropyridin-3-yl)-6-methoxy-3,4-dimethyl-8-pyridin-3-ylimidazo[1,5-a]quinoxalineIC501000.0 [1]
PDE5 Inhibitor C2IC506223.0 [1]
N-(2-Chlorophenyl)-3-cyclopentyloxy-4-(difluoromethoxy)benzamideIC50100000.0 [1]
3-Cyclopentyloxy-4-(difluoromethoxy)-N-pyridin-3-ylbenzamideIC50100000.0 [1]
3-(Cyclopropylmethoxy)-4-(difluoromethoxy)-N-pyridin-3-ylbenzamideIC50100000.0 [1]
N-(2-Chlorophenyl)-3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzamideIC50100000.0 [1]
3-Isopropyl-5-(2-(2-morpholinoethoxy)benzyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-oneIC5010000.0 [1]
5,6-Diethyl-2-{5-[(4-Methylpiperazin-1-Yl)sulfonyl]-2-Propoxyphenyl}pyrimidin-4(3h)-OneIC5010000.0 [1]
(2R)-2-[(1-Cyclopentyl-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl)amino]-N-(4-methoxyphenyl)propanamideIC50100000.0 [1]
3-Propan-2-yl-5-[[(1S,2R)-2-(pyrimidin-2-ylamino)cyclohexyl]methyl]-2,6-dihydropyrazolo[4,3-d]pyrimidin-7-oneIC5010000.0 [1]
2-[[(1R,2S)-2-[(7-Oxo-3-propan-2-yl-2,6-dihydropyrazolo[4,3-d]pyrimidin-5-yl)methyl]cyclohexyl]amino]-4-(trifluoromethyl)pyrimidine-5-carboxylic acidIC501000.0 [1]
(2S)-2-[(1-Cyclopentyl-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl)amino]-N-(4-methoxyphenyl)propanamideIC50100000.0 [1]
(2R)-2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamideIC50100000.0 [1]
(2S)-2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamideIC50100000.0 [1]
4-Ethoxy-N-(6-hydroxyhexyl)-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)benzenesulfonamideIC5010000.0 [1]
2-[[1-(2-Chlorophenyl)-4-oxo-5H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N-(4-methoxyphenyl)propanamideIC50100000.0 [1]
6-Methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamideIC5010000.0 [1]
Pde5-IN-2IC5032000.0 [1]
(2S,8R)-2-(5-Ethylthiophen-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC504000.0 [1]
(10S,15S)-13-Ethyl-10-(5-ethylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dioneIC503000.0 [1]
Methyl 7-cyclopentyloxy-6-methoxy-2-[4-(trifluoromethoxy)benzoyl]-3,4-dihydro-1H-isoquinoline-3-carboxylateIC50100000.0 [1]
N-[4-[(7-Cyclopentyloxy-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl)sulfonyl]phenyl]acetamideIC50100000.0 [1]
(R)-2-(4-Fluorophenoxy)-N-(1-(thiophen-2-yl)ethyl)nicotinamideIC5016000.0 [1]
2-Methoxy-6,7-Dimethyl-9-(4-Methylpyridin-3-Yl)imidazo[1,5-A]pyrido[3,2-E]pyrazineIC5010000.0 [1]
3-(2,5-Dichlorophenyl)-12-methoxy-5,7-dimethyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC501000.0 [1]
12-Methoxy-5,7-dimethyl-3-(2-methylphenyl)-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC5010000.0 [1]
3-(12-Methoxy-5,7-dimethyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)benzamideIC5010000.0 [1]
12-Methoxy-5,7-dimethyl-3-(3-methylthiophen-2-yl)-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC5010000.0 [1]
8-Fluoro-6-Methoxy-3,4-Dimethyl-1-(3-Methylpyridin-4-Yl)imidazo[1,5-A]quinoxalineIC5010000.0 [1]
8-Fluoro-6-methoxy-3,4-dimethyl-1-(2-methylpyridin-3-yl)imidazo[1,5-a]quinoxalineIC5010000.0 [1]
6,8-Dimethoxy-3,4-dimethyl-1-(4-methylpyridin-3-yl)imidazo[1,5-a]quinoxalineIC5010000.0 [1]
6,8-Dimethoxy-3,4-dimethyl-1-(2-methylpyridin-3-yl)imidazo[1,5-a]quinoxalineIC5010000.0 [1]
(3R)-1-[(6-Methoxy-3,8-dimethyl-2H-pyrazolo[3,4-b]quinolin-4-yl)methyl]pyrrolidin-3-olKi10000.0 [1]
4-[(6-Methoxy-3,8-dimethyl-2H-pyrazolo[3,4-b]quinolin-4-yl)methyl]-2-methylmorpholineKi10000.0 [1]
6-Chloro-3,4-Dimethyl-1-(3-Methylpyridin-4-Yl)-8-(Trifluoromethyl)imidazo[1,5-A]quinoxalineIC501000.0 [1]
6-Methoxy-3,4-dimethyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[1,5-a]quinoxalineIC50500.0 [1]
6-Chloro-8-methoxy-3,4-dimethyl-1-(3-methylpyridin-4-yl)imidazo[1,5-a]quinoxalineIC501000.0 [1]
5-Methyl-3-[[(2R)-4-(1,3-thiazol-2-ylmethyl)morpholin-2-yl]methyl]triazolo[4,5-d]pyrimidin-7-amineIC501.9 [1]
1-[(5-Methyl-2-phenyl-1,3-oxazol-4-yl)methyl]-N-[(6-methylpyridin-2-yl)methyl]piperidine-3-carboxamideIC501.8 [1]
(3R,5R)-5-Ethyl-1-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methyl]-N-[(6-methylpyridin-2-yl)methyl]piperidine-3-carboxamideIC501.8 [1]
2-[(5-Methyl-2-phenyl-1,3-oxazol-4-yl)methyl]-N-[(6-methylpyridin-2-yl)methyl]-3,4-dihydro-1H-isoquinoline-4-carboxamideIC501.8 [1]
1-[4-[3-(1-Quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]piperidin-1-yl]ethanoneIC5030000.0 [1]
6-[3-(1-Quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]quinazolin-2-amineIC5030000.0 [1]
3-(2-Chloro-4-fluorophenyl)-12-methoxy-5,7-dimethyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC501000.0 [1]
12-Methoxy-5,7-dimethyl-3-(1,3,5-trimethylpyrazol-4-yl)-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC5010000.0 [1]
5-(12-Methoxy-5,7-dimethyl-2,4,8,13-tetrazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaen-3-yl)-2,4-dimethyl-1,3-thiazoleIC5010000.0 [1]
3,4-Dimethyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethoxy)imidazo[1,5-a]quinoxalineIC5010000.0 [1]
3,4-Dimethyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[1,5-a]quinoxalineIC505000.0 [1]
1-(Cyclopropylmethyl)-5-[2-(1,2-dihydroimidazo[1,2-a]benzimidazol-3-yl)ethoxy]-3-(2-phenylpyrazol-3-yl)pyridazin-4-oneIC5010000.0 [1]
1-[(2-Chloro-6-fluorophenyl)methyl]-N-[4-(diethylamino)phenyl]-4,6-dioxo-5H-1,5-naphthyridine-3-carboxamideIC505000.0 [1]
1-[(2-Chloro-6-fluorophenyl)methyl]-N-(4-morpholin-4-ylphenyl)-4,6-dioxo-5H-1,5-naphthyridine-3-carboxamideIC501000.0 [1]
8-[(4-Hydroxycyclohexyl)amino]-3-(6-methoxypyridin-3-yl)-5-(2-propoxyethyl)pyrimido[5,4-c]pyridazin-6-oneIC502000.0 [1]
4-[(3,8-Dimethyl-6-propan-2-yloxy-2H-pyrazolo[3,4-b]quinolin-4-yl)methyl]-1,4-oxazepaneKi10000.0 [1]
4-[[6-(2-Methoxyethoxy)-3,8-dimethyl-2H-pyrazolo[3,4-b]quinolin-4-yl]methyl]-1,4-oxazepaneKi10000.0 [1]
3,8-Dimethyl-4-(1,4-oxazepan-4-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-6-olKi10000.0 [1]
[1-[4-(1-Quinolin-2-ylazetidin-3-yl)oxypyridin-3-yl]piperidin-4-yl]methanolIC5030000.0 [1]
1-[4-(3-{[1-(Quinolin-2-Yl)azetidin-3-Yl]oxy}quinoxalin-2-Yl)piperidin-1-Yl]ethanoneIC5030000.0 [1]
[1-[3-(1-Quinolin-2-ylpiperidin-4-yl)oxypyrazin-2-yl]piperidin-4-yl]methanolIC5030000.0 [1]
[1-[3-(1-Quinolin-2-ylazetidin-3-yl)oxyquinoxalin-2-yl]piperidin-4-yl]methanolIC5030000.0 [1]
[(1S)-1-[3-(Cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-2-(3,5-dichloro-1-oxidopyridin-1-ium-4-yl)ethyl] (2S)-3-[3-(dimethylcarbamoyl)phenyl]sulfonyl-1,3-thiazolidine-2-carboxylateIC503560.0 [1]
[(1S)-1-[3-(Cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-2-(3,5-dichloro-1-oxidopyridin-1-ium-4-yl)ethyl] (2S)-1-[3-(dimethylcarbamoyl)phenyl]sulfonylpyrrolidine-2-carboxylateIC5017000.0 [1]
2-Ethyl-2-{[4-(Methylamino)-6-(1h-1,2,4-Triazol-1-Yl)-1,3,5-Triazin-2-Yl]amino}butanenitrileIC501000.0 [1]
8-[(2-Fluoro-4-methoxyphenyl)methyl]-13-(oxan-4-ylmethyl)-10-thia-3,5,6,8,13-pentazatetracyclo[7.7.0.02,6.011,16]hexadeca-1(9),2,4,11(16)-tetraen-7-oneIC508400.0 [1]
4-[6-(1,3-Difluoropropan-2-yloxy)-3-[(3,4-dimethoxyphenyl)methyl]-2,4-dioxoquinazolin-1-yl]piperidine-1-carbaldehydeIC50140.0 [1]
4-[6-(1,3-Difluoropropan-2-yloxy)-3-[[3-methoxy-4-(2-oxo-2-piperidin-1-ylethoxy)phenyl]methyl]-2,4-dioxoquinazolin-1-yl]piperidine-1-carbaldehydeIC50390.0 [1]
5-[[6-(1,3-Difluoropropan-2-yloxy)-1-(1-formylpiperidin-4-yl)-2,4-dioxoquinazolin-3-yl]methyl]-2-phenylbenzonitrileIC5015.0 [1]
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References

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MLA

"Quest Database™ Phosphodiesterase 8A Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/phosphodiesterase-8a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 9). Quest Database™ Phosphodiesterase 8A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/phosphodiesterase-8a-inhibitors-ic50-ki.
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