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Phosphodiesterase 10A Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
PapaverineIC5040.0 [1]
MardepodectIC501.34 [1]
2-[[4-[4-Pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinolineIC500.3 [1], 1.0 [2], 1.41 [3]
2-Methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazineIC507.0 [1], 7.28 [2], 7.3 [3], 32.0 [4]
SildenafilIC503100.0 [1], 5400.0 [2], 6800.0 [3], 10000.0 [4]
6,7-Dimethoxy-4-[(3R)-3-(quinoxalin-2-yloxy)pyrrolidin-1-yl]quinazolineIC5016.0 [1], 64.0 [2]
6,7-Dimethoxy-4-[(3R)-3-(quinoxalin-2-yloxy)pyrrolidin-1-yl]quinazolineKi3981071.71 [1]
TadalafilIC5010000.0 [1]
(2R)-2-[[3-Cyano-2-[4-(2-ethoxyphenyl)phenyl]-6-fluoroquinolin-4-yl]amino]propanoic acidIC506.0 [1], 8.0 [2]
1H-Isoindole-1,3(2H)-dione, 2-((3,4-dihydro-3-(4-methoxyphenyl)-4-oxo-2-quinazolinyl)methyl)-Ki1000.0 [1], 1900.0 [2]
4-Methoxy-2-[2-[3-(4-methoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]isoindole-1,3-dioneKi2.0 [1]
5,8-Dimethyl-2-(2-phenylimidazo[1,2-a]pyridin-7-yl)-[1,2,4]triazolo[1,5-a]pyrazineIC500.1 [1], 37.0 [2]
N-[cis-3-(2-Methoxy-3h-Imidazo[4,5-B]pyridin-3-Yl)cyclobutyl]-1,3-Benzothiazol-2-AmineIC500.8 [1], 2.2 [2], 3.4 [3]
VardenafilIC50790.0 [1], 880.0 [2]
5-(6,7-Dimethoxycinnolin-4-yl)-3-methyl-N-propan-2-ylpyridin-2-amineIC501.9 [1], 2.0 [2]
CID 46239428Ki5.0 [1]
5-(1h-Benzimidazol-2-Ylmethylsulfanyl)-2-Methyl-[1,2,4]triazolo[1,5-C]quinazolineIC5012.0 [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)methanesulfonamideIC507.0 [1], 7.16 [2]
3-(2-Chlorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC5013.1 [1], 21.0 [2]
1h-Benzimidazol-2-Yl(4-{[3-(Morpholin-4-Yl)pyrazin-2-Yl]oxy}phenyl)methanoneIC504.5 [1]
1-[4-[3-[4-(1H-Benzimidazole-2-carbonyl)phenoxy]pyrazin-2-yl]piperazin-1-yl]ethanoneIC505.1 [1]
N-[4-(3-Morpholin-4-ylpyrazin-2-yl)oxyphenyl]-1H-benzimidazol-2-amineIC501.1 [1], 25.0 [2]
[1-[3-[4-(1,3-Benzothiazol-2-ylamino)phenoxy]pyrazin-2-yl]piperidin-4-yl]methanolIC500.2 [1], 200.0 [2]
4-[5-(8,9-Dimethoxy-5,6-dihydroimidazo[5,1-a]isoquinolin-1-yl)-1,3-thiazol-2-yl]morpholineIC5010.0 [1]
4-[5-(8,9-Dimethoxy-5,6-dihydroimidazo[5,1-a]isoquinolin-1-yl)-1,3-thiazol-2-yl]morpholineKi26.0 [1]
2-Methyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)-ethyl)pyrazolo[1,5-c]quinazolineIC5050.0 [1]
2-(2'-Ethoxybiphenyl-4-Yl)-4-Hydroxy-1,6-Naphthyridine-3-CarbonitrileIC5012.0 [1]
N-Methyl-N-[4-(quinolin-2-ylmethoxy)phenyl]-1,3-benzothiazole-6-carboxamideIC5031.0 [1]
N-Methyl-N-[4-(quinolin-2-ylmethoxy)phenyl]pyridine-4-carboxamideIC50250.0 [1]
N-Methyl-3-pyridin-2-yl-N-[4-(quinolin-2-ylmethoxy)phenyl]-1H-pyrazole-5-carboxamideIC5012.0 [1]
6-Chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-(3-quinolin-2-ylpropoxy)pyrimidin-4-amineKi0.01 [1]
[1-(3-{[1-(Quinolin-2-Yl)azetidin-3-Yl]oxy}pyrazin-2-Yl)piperidin-4-Yl]methanolIC502.4 [1], 2400.0 [2]
6-Methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazineIC501.48 [1]
1-(2-Chlorophenyl)-6,8-Dimethoxy-3-Methylimidazo[5,1-C][1,2,4]benzotriazineIC500.28 [1]
8-Fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC503.55 [1]
N-Methyl-3-phenyl-N-[4-(quinolin-2-ylmethoxy)phenyl]-1H-pyrazole-5-carboxamideIC5024.0 [1]
2-{2-[3-(4-Methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]ethyl}-1H-isoindole-1,3(2H)-dioneKi87.0 [1]
5,8-Dimethyl-2-[2-(1-methyl-4-phenylimidazol-2-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyrazineIC501.8 [1], 7.2 [2]
5,7-Dimethyl-2-[2-(1-methyl-4-phenylimidazol-2-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyridineIC500.32 [1], 17.0 [2]
Unii-ND06tnj6W7IC500.32 [1]
5,7-Dimethyl-2-[2-(1-methyl-4-phenylimidazol-2-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyrimidineIC5012.0 [1], 67.0 [2]
5,8-Dimethyl-2-[2-(1-methyl-4-phenylimidazol-2-yl)ethyl]-[1,2,4]triazolo[1,5-c]pyrimidineIC507.2 [1]
2-[2-[3-(4-Methoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]-4-methylisoindole-1,3-dioneKi6.1 [1], 61.0 [2]
4-Hydroxy-2-[2-[3-(4-methoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]isoindole-1,3-dioneKi20.0 [1], 22.0 [2]
2-[3-[3-(4-Methoxyphenyl)-4-oxoquinazolin-2-yl]propyl]isoindole-1,3-dioneKi219.0 [1]
2-[2-[3-(4-Methoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]-4-pyridin-4-ylisoindole-1,3-dioneKi0.07 [1]
2-[2-[3-(4-Methoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-propan-2-yloxyisoindole-1,3-dioneKi0.37 [1], 0.56 [2]
2-(6-Chloropyridin-3-yl)-N-(1-methylpyrazol-4-yl)-4-propan-2-yloxy-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxamideKi0.9 [1]
2-[2-[3-(4-Methoxyphenyl)-4-oxoquinazolin-2-yl]ethyl]-4-propan-2-yloxyisoindole-1,3-dioneKi0.15 [1]
2-(6-Chloropyridin-3-yl)-4-propan-2-yloxy-6-pyridin-3-ylsulfonyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidineKi0.63 [1]
[2-(6-Chloropyridin-3-yl)-4-(2-methoxyethoxy)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-pyrazolo[1,5-a]pyridin-3-ylmethanoneKi0.92 [1], 0.93 [2]
[2-(6-Chloropyridin-3-yl)-4-(2-methoxyethoxy)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-imidazo[1,5-a]pyridin-1-ylmethanoneKi0.99 [1], 1.0 [2]
N-(3-Ethylphenyl)-4-(1-methylpiperidin-4-yl)oxy-2-pyridin-3-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxamideKi14.0 [1]
1-[4-[Benzyl(methyl)amino]-2-[5-(1H-pyrazol-4-yl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-3-methylbutan-1-oneKi15.0 [1]
N-Phenyl-2-pyridin-4-yl-4-(2-pyridin-2-ylethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxamideKi47.9 [1]
5,8-Dimethyl-2-[2-(1-methyl-2-thiophen-2-ylimidazol-4-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyrazineIC501.0 [1]
6-Cyclopropyl-N-(2-methyl-5-quinolin-2-ylpyrazol-3-yl)-3-(pyrimidin-5-ylamino)pyridine-2-carboxamideIC501.0 [1]
6-Cyclopropyl-N-(2-pyridin-2-yl-1,3-thiazol-5-yl)-3-(pyrimidin-5-ylamino)pyridine-2-carboxamideIC502.0 [1]
1-[4-[3-(1-Quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]piperidin-1-yl]ethanoneIC5029.0 [1], 29000.0 [2]
6-[3-(1-Quinolin-2-ylazetidin-3-yl)oxypyrazin-2-yl]quinazolin-2-amineIC506.8 [1], 6800.0 [2]
(1H-Benzoimidazol-2-yl)-[3-(3-phenyl-pyridin-2-yl)-azetidin-1-yl]-methanoneIC5021.9 [1]
6-Cyclopropyl-N-[4-(methylcarbamoyl)pyridin-3-yl]-3-(pyrimidin-5-ylamino)pyridine-2-carboxamideIC5013.7 [1]
2-[3-(1H-Benzimidazol-2-yl)propoxy]-6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methylpyrimidin-4-amineKi0.02 [1]
6-Chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-[2-(1,8-naphthyridin-2-yloxy)ethoxy]pyrimidin-4-amineKi0.04 [1]
5-Cyclopropyl-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]pyrazolo[1,5-a]pyrimidin-7-amineKi9.2 [1]
6-Cyclopropyl-N-[2-(2-methoxyethyl)-5-pyridin-2-ylpyrazol-3-yl]-3-(pyrimidin-5-ylamino)pyridine-2-carboxamideIC501.0 [1]
[1-[4-(1-Quinolin-2-ylazetidin-3-yl)oxypyridin-3-yl]piperidin-4-yl]methanolIC504.7 [1], 4700.0 [2]
[1-[3-(1-Quinolin-2-ylpiperidin-4-yl)oxypyrazin-2-yl]piperidin-4-yl]methanolIC506.5 [1], 6500.0 [2]
[1-[3-(1-Quinolin-2-ylazetidin-3-yl)oxyquinoxalin-2-yl]piperidin-4-yl]methanolIC506.8 [1], 6800.0 [2]
6-Cyclopropyl-N-[2-(dimethylcarbamoyl)-3-methoxyphenyl]-3-(pyrimidin-5-ylamino)pyrazine-2-carboxamideIC5012.0 [1], 12.2 [2]
6-Cyclopropyl-N-[3-(dimethylcarbamoyl)-1-methylpyrazol-4-yl]-3-(pyrimidin-5-ylamino)pyridine-2-carboxamideIC5031.5 [1]
1h-Benzimidazol-2-Yl(4-{[3-(Tetrahydro-2h-Pyran-4-Yl)pyridin-2-Yl]oxy}phenyl)methanoneIC500.1 [1], 0.17 [2]
1-[4-[2-[4-(1H-Benzimidazole-2-carbonyl)phenoxy]pyridin-3-yl]piperidin-1-yl]ethanoneIC500.1 [1], 0.16 [2]
N-[4-(3-Morpholin-4-ylpyridin-2-yl)oxyphenyl]-1,3-benzothiazol-2-amineIC500.96 [1]
2-[2-[2-(Furan-3-yl)-1H-imidazol-5-yl]ethyl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazineIC500.27 [1]
2-[2-[3-[(3S)-3-Fluoropyrrolidin-1-yl]phenyl]imidazo[1,2-a]pyridin-7-yl]-5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazineIC500.16 [1]
5,8-Dimethyl-2-(2-pyridin-2-ylimidazo[1,2-a]pyridin-7-yl)-[1,2,4]triazolo[1,5-a]pyrazineIC500.16 [1]
5,8-Dimethyl-2-[2-(2-thiophen-2-yl-1H-imidazol-5-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyrazineIC500.34 [1], 0.4 [2]
N-[(1-Methylpyrazol-4-yl)methyl]-5-[[(1S,2S)-2-pyridin-2-ylcyclopropyl]methoxy]pyrazolo[1,5-a]pyrimidin-7-amineKi0.23 [1], 0.32 [2]
6-Chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-[[(1S,2S)-2-pyridin-2-ylcyclopropyl]methoxy]pyrimidin-4-amineKi0.02 [1], 0.07 [2]
6-Chloro-5-methyl-N-[(1-methylpyrazol-4-yl)methyl]-2-[[(1S,2S)-2-pyridin-2-ylcyclopropyl]methoxy]pyrimidin-4-amineKi0.44 [1]
4-[8-Morpholin-4-yl-2-(3-quinolin-2-ylcyclobutyl)imidazo[1,2-b]pyridazin-3-yl]benzoic acidIC501.0 [1], 13.0 [2]
1-[4-[8-Morpholin-4-yl-2-(3-quinolin-2-ylcyclobutyl)imidazo[1,2-b]pyridazin-3-yl]phenyl]piperidine-4-carboxylic acidIC502.0 [1], 93.0 [2]
4,7-Diacetyl-N-[4-(2-hydroxypropan-2-yl)quinolin-2-yl]-3-methyl-1-benzothiophene-2-carboxamideIC502.6 [1], 5.1 [2]
7-Acetyl-N-[5-(3-methoxyazetidine-1-carbonyl)quinolin-2-yl]-4-(methoxymethyl)-3-methyl-1-benzothiophene-2-carboxamideIC500.22 [1], 0.73 [2]
7-Acetyl-N-[4-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]quinolin-2-yl]-4-(methoxymethyl)-3-methyl-1-benzothiophene-2-carboxamideIC500.15 [1], 1.3 [2]
[2-[[7-Acetyl-4-(methoxymethyl)-3-methyl-1-benzothiophene-2-carbonyl]amino]quinolin-5-yl]methyl dihydrogen phosphateIC500.6 [1], 0.99 [2]
7-Acetyl-N-[4-[[(3S)-3-hydroxypyrrolidin-1-yl]methyl]quinolin-2-yl]-4-(methoxymethyl)-3-methyl-1-benzothiophene-2-carboxamideIC500.23 [1], 0.42 [2]
1-[5-(4-Chloro-3,5-dimethoxyphenyl)furan-2-yl]-2-ethoxy-2-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]ethanoneIC500.62 [1]
N-[3-[3-(Oxan-4-yl)pyridin-2-yl]oxycyclobutyl]-1,3-benzothiazol-2-amineIC500.75 [1], 3.19 [2]
5-Methyl-N-[3-[3-(oxan-4-yl)pyridin-2-yl]oxycyclobutyl]pyridin-2-amineIC508.25 [1], 17.63 [2]
N-[3-[3-(Oxan-4-yl)pyridin-2-yl]oxycyclobutyl]-1H-benzimidazol-2-amineIC501.53 [1], 2.63 [2]
1-[4-[3-[3-(Quinolin-2-ylamino)cyclobutyl]oxypyrazin-2-yl]piperidin-1-yl]ethanoneIC504.93 [1], 15.82 [2]
1-[4-[3-[3-[(5-Methylpyridin-2-yl)amino]cyclobutyl]oxypyrazin-2-yl]piperidin-1-yl]ethanoneIC5066.06 [1], 84.55 [2]
N-[3-[3-(Oxan-4-yl)pyridin-2-yl]oxycyclobutyl]-5-(trifluoromethyl)pyridin-2-amineIC50106.0 [1], 865.0 [2]
6-[[3-[3-(Oxan-4-yl)pyridin-2-yl]oxycyclobutyl]amino]pyridine-3-carbonitrileIC50590.0 [1], 865.0 [2]
5-Chloro-N-[3-[3-(oxan-4-yl)pyridin-2-yl]oxycyclobutyl]pyridin-2-amineIC5083.7 [1], 865.0 [2]
2-[3-[3-(3-Azabicyclo[3.2.2]nonan-3-yl)pyrazin-2-yl]azetidin-1-yl]quinolineIC5035.0 [1]
4-[3-(1-Quinolin-2-ylazetidin-3-yl)pyrazin-2-yl]benzamideIC501.3 [1]
2-Fluoro-4-[3-(1-quinolin-2-ylazetidin-3-yl)pyrazin-2-yl]benzamideIC502.0 [1], 2.6 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Phosphodiesterase 10A Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/phosphodiesterase-10a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Phosphodiesterase 10A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/phosphodiesterase-10a-inhibitors-ic50-ki.
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