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Phosphodiesterase 6 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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▼
SildenafilIC500.5 [1], 25.0 [2], 40.0 [3]
SildenafilKi50.0 [1]
TadalafilIC50980.0 [1], 1260.0 [2], 2000.0 [3], 5200.0 [4]
VardenafilIC501.0 [1], 11.0 [2]
DipyridamoleKi125.0 [1]
ZaprinastKi400.0 [1]
N-(2-Fluoroethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]pyrrolo[3,2-b]pyridine-3-carboxamideIC509000.0 [1]
DprE1-IN-1IC506000.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-benzylpyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50249.0 [1]
4-(3-(1-Acetylpiperidine-4-yl)pyrazine-2-yloxy)phenyl(1H-benzoimidazole-2-yl)methanoneIC5030000.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-(1-benzylpiperidin-4-yl)-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC501619.0 [1]
4-[[1-(2-Chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholineIC502280.0 [1]
N-(Cyclopropylmethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]pyrrolo[3,2-b]pyridine-3-carboxamideIC503000.0 [1]
N-(2-Fluoroethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]-6-methylpyrrolo[3,2-b]pyridine-3-carboxamideIC501000.0 [1]
1-[[6-(Dimethylamino)-5-methylpyrimidin-4-yl]methyl]-N-(2-fluoroethyl)pyrrolo[3,2-b]pyridine-3-carboxamideIC50100000.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-(2-morpholin-4-ylethyl)-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC502966.0 [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-oneIC50860.0 [1]
5-Bromo-2-[5-(4-methylpiperazin-1-yl)sulfonyl-2-propoxyphenyl]-4-propan-2-yl-1H-pyrimidin-6-oneIC507.4 [1]
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-hexaeneIC50435.0 [1]
4-[(3-Chloro-4-methoxyphenyl)methylamino]-8-cyclopropyl-3-(hydroxymethyl)quinoline-6-carbonitrileIC50339.0 [1]
6-Methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazineIC501790.0 [1]
1-(2-Chlorophenyl)-6,8-Dimethoxy-3-Methylimidazo[5,1-C][1,2,4]benzotriazineIC5073.15 [1]
8-Fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC501000.0 [1]
1-(5-Butoxypyridin-3-Yl)-4-Methyl-8-(Morpholin-4-Ylmethyl)[1,2,4]triazolo[4,3-A]quinoxalineIC5010000.0 [1]
Pde2/pde10-IN-1IC5010000.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[2-(dimethylamino)ethyl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC508224.0 [1]
(7R)-7-Benzyl-2-bromo-5-ethyl-3-[(4-hydroxyphenyl)methyl]-7,8-dihydroimidazo[2,1-b]purin-4-oneIC50180.0 [1]
11-Benzyl-7,13-dimethyl-4-pyridin-3-yl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50280.0 [1]
11-Benzyl-7,13-dimethyl-4-thiophen-3-yl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC502200.0 [1]
11-Benzyl-4-(furan-3-yl)-7,13-dimethyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50330.0 [1]
11-Benzyl-7-ethyl-13-methyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50550.0 [1]
11-Benzyl-13-methyl-4-phenyl-7-propyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50610.0 [1]
11-Benzyl-13-methyl-4-phenyl-7-propan-2-yl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC5062.0 [1]
11-Benzyl-4-(4-chlorophenyl)-7,13-dimethyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC504700.0 [1]
7,11,13-Trimethyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC502600.0 [1]
11-Benzyl-13-(ethoxymethyl)-7-methyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC50330.0 [1]
11-Benzyl-13-[(dimethylamino)methyl]-7-methyl-4-phenyl-5,6,8,11,12-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,7,12-pentaen-10-oneIC501000.0 [1]
N-[3-(5-Bromo-6-oxo-4-propan-2-yl-1H-pyrimidin-2-yl)-4-propoxyphenyl]methanesulfonamideIC501600.0 [1]
(2S)-1-[3-(5-Bromo-6-oxo-4-propan-2-yl-1H-pyrimidin-2-yl)-4-propoxyphenyl]sulfonylpyrrolidine-2-carboxylic acidIC502.2 [1]
3-[(3R)-3-[(2R,8R)-2-(1,3-Benzodioxol-5-yl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-6-yl]pyrrolidin-1-yl]-N-ethylpropanamideIC50620.0 [1]
(2R,8R)-6-[(3R)-1-[3-(Azetidin-1-yl)-3-oxopropyl]pyrrolidin-3-yl]-2-(1,3-benzodioxol-5-yl)-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50846.0 [1]
3-[(3R)-3-[(2R,8R)-2-(1,3-Benzodioxol-5-yl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-6-yl]pyrrolidin-1-yl]propanamideIC501601.0 [1]
3-[(3R)-3-[(2R,8R)-2-(1,3-Benzodioxol-5-yl)-4,7-dioxo-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraen-6-yl]pyrrolidin-1-yl]-N,N-dimethylpropanamideIC50807.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-[2-(1H-imidazol-2-yl)ethyl]pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50357.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-[2-(1-methylimidazol-2-yl)ethyl]pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50494.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-pentylpyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC501770.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-propylpyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC5010.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-(2-pyridin-2-ylethyl)pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50226.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-(2-pyrazin-2-ylethyl)pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50358.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-(2-pyridin-3-ylethyl)pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC50271.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-(2-cyclopropylethyl)pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC502660.0 [1]
(2R,8R)-2-(1,3-Benzodioxol-5-yl)-6-[(3R)-1-(3-methoxypropyl)pyrrolidin-3-yl]-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dioneIC501340.0 [1]
4-(3-Chloro-4-methoxy-benzylamino)-7-trifluoromethyl-quinoline-3-carboxylic acid ethyl esterIC5020000.0 [1]
3-(4-Fluoro-2-methylphenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC501150.0 [1]
12-Methoxy-5-methyl-3-(2-methylphenyl)-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC501570.0 [1]
10-Methoxy-5-methyl-3-(2-methylpyridin-3-yl)-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(13),3,5,7,9,11-hexaeneIC505000.0 [1]
10-Methoxy-5-methyl-3-(3-methylpyridin-4-yl)-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(13),3,5,7,9,11-hexaeneIC5010000.0 [1]
6-Methoxy-3-methyl-1-(2-methylphenyl)imidazo[5,1-c][1,2,4]benzotriazineIC501980.0 [1]
6,8-Dimethoxy-3-methyl-1-(2-methylpyridin-3-yl)imidazo[5,1-c][1,2,4]benzotriazineIC50493.0 [1]
6,8-Dimethoxy-3-methyl-1-(4-methylpyridin-3-yl)imidazo[5,1-c][1,2,4]benzotriazineIC501822.0 [1]
6,8-Dimethoxy-3-methyl-1-(3-methylpyridin-4-yl)imidazo[5,1-c][1,2,4]benzotriazineIC501240.0 [1]
4-[6-Methoxy-3-methyl-1-(2-methylphenyl)imidazo[5,1-c][1,2,4]benzotriazin-8-yl]morpholineIC50693.0 [1]
1-(2-Chlorophenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC501060.0 [1]
4-[6-Methoxy-3-methyl-1-(3-methylpyridin-4-yl)imidazo[5,1-c][1,2,4]benzotriazin-8-yl]morpholineIC503120.0 [1]
3-(2,4-Dichlorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC501000.0 [1]
3-(2-Fluoro-5-methoxyphenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC50734.0 [1]
6-Fluoro-8-methoxy-1-(2-methoxyphenyl)-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC501000.0 [1]
6-Fluoro-8-methoxy-3-methyl-1-(3-methylthiophen-2-yl)imidazo[5,1-c][1,2,4]benzotriazineIC501230.0 [1]
6-Methoxy-3,8-dimethyl-N-(oxan-2-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi843.0 [1]
6-Methoxy-3,8-dimethyl-N-(morpholin-2-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi13882.0 [1]
6-Methoxy-3,8-dimethyl-N-(piperidin-4-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi14782.0 [1]
6-Methoxy-3,8-dimethyl-N-(oxan-4-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi697.0 [1]
6-Methoxy-3,8-dimethyl-N-(2-pyridin-4-ylethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi554.0 [1]
6-Methoxy-N,3,8-trimethyl-N-(oxan-4-yl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi7383.0 [1]
6-Methoxy-3,8-Dimethyl-4-(Piperazin-1-Yl)-1h-Pyrazolo[3,4-B]quinolineKi770.0 [1]
6-Methoxy-3,8-dimethyl-N-(oxan-4-yl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi278.0 [1]
4-[(3-Chloro-4-methoxyphenyl)methylamino]-8-(dimethylamino)-3-(hydroxymethyl)quinoline-6-carbonitrileIC505100.0 [1]
1-(3-Pyridyl)-8,9-dimethoxy-5,6-dihydroimidazo[5,1-a]isoquinolineKi4274.0 [1]
5-(8,9-Dimethoxy-3-methyl-5,6-dihydroimidazo[5,1-a]isoquinolin-1-yl)-1,3-thiazoleKi7100.0 [1]
1-(3-Pyridyl)-8,9-dimethoxy-3-methyl-5,6-dihydroimidazo[5,1-a]isoquinolineKi7950.0 [1]
N-Tert-butyl-5-(8,9-dimethoxy-5,6-dihydroimidazo[5,1-a]isoquinolin-1-yl)-N-methyl-1,3-thiazole-2-carboxamideKi2000.0 [1]
8,9-Dimethoxy-1-(1,3-Thiazol-5-Yl)-5,6-Dihydroimidazo[5,1-A]isoquinolineKi2000.0 [1]
6-Methoxy-3,8-dimethyl-N-(pyridin-4-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi211.0 [1]
6-Methoxy-3,8-dimethyl-N-(pyridin-2-ylmethyl)-2H-pyrazolo[3,4-b]quinolin-4-amineKi1811.0 [1]
3-(2,5-Dichlorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC50829.0 [1]
8-(Difluoromethoxy)-6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)imidazo[5,1-c][1,2,4]benzotriazineIC50909.0 [1]
6-Methoxy-3-methyl-1-(4-methylpyridin-3-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazineIC505250.0 [1]
1-(3-Fluoro-2-methylphenyl)-6-methoxy-3-methyl-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazineIC501260.0 [1]
3-(2-Chloro-4-fluorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaeneIC50462.0 [1]
8-Fluoro-6-methoxy-3-methyl-1-(3-methylthiophen-2-yl)imidazo[5,1-c][1,2,4]benzotriazineIC503270.0 [1]
8-Fluoro-6-methoxy-3-methyl-1-(1,3,5-trimethylpyrazol-4-yl)imidazo[5,1-c][1,2,4]benzotriazineIC505000.0 [1]
8-Fluoro-6-methoxy-1-(2-methoxyphenyl)-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC5010000.0 [1]
8-Fluoro-6-methoxy-3-methyl-1-(4-methylpyridin-3-yl)imidazo[5,1-c][1,2,4]benzotriazineIC5010000.0 [1]
4-[1-(2-Chlorophenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazin-8-yl]morpholineIC50276.0 [1]
8-Fluoro-6-methoxy-1-(3-methoxyphenyl)-3-methylimidazo[5,1-c][1,2,4]benzotriazineIC501000.0 [1]
5-(8-Fluoro-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazin-1-yl)-2,4-dimethyl-1,3-thiazoleIC503880.0 [1]
8-Fluoro-6-methoxy-3-methyl-1-(2-methylpyridin-3-yl)imidazo[5,1-c][1,2,4]benzotriazineIC502830.0 [1]
8-Fluoro-6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)imidazo[5,1-c][1,2,4]benzotriazineIC5010000.0 [1]
6,8-Dimethoxy-3-methyl-1-(2-methylphenyl)imidazo[5,1-c][1,2,4]benzotriazineIC50349.0 [1]
6,8-Dimethoxy-3-methyl-1-[2-(trifluoromethyl)phenyl]imidazo[5,1-c][1,2,4]benzotriazineIC501000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Phosphodiesterase 6 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/phosphodiesterase-6-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 21). Quest Database™ Phosphodiesterase 6 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/phosphodiesterase-6-inhibitors-ic50-ki.
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