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PI3-kinase p110-alpha/p85-alpha 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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DactolisibIC504.0 [1], 16.4 [2], 35.15 [3], 49.0 [4], 89.0 [5]
CID 46927938IC502.3 [1]
CID 46927938Ki2.3 [1], 2.34 [2]
[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl] N-methylsulfamateKi0.08 [1], 0.23 [2]
4-[4-(2-Aminopyrimidin-5-yl)-7-[3-[methyl(methylsulfamoyl)amino]cyclobutyl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-2-yl]morpholineKi0.19 [1], 0.32 [2], 0.41 [3], 0.47 [4]
WortmanninIC501.2 [1], 11.9 [2], 1610.0 [3]
IdelalisibIC50825.0 [1], 2000.0 [2], 7500.0 [3]
PictilisibIC504.8 [1], 18.0 [2], 19.0 [3]
BuparlisibIC5011.0 [1], 29.0 [2], 40.0 [3]
PI-103IC502.0 [1], 8.0 [2], 40.0 [3]
pi3K/Mtor Inhibitor-1IC5010.0 [1], 11.0 [2]
N-[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]methanesulfonamideKi0.16 [1], 0.28 [2], 1.39 [3]
DuvelisibIC50400.0 [1], 10000.0 [2]
FimepinostatIC5019.0 [1]
4-[2-[(5-Fluoro-6-methoxypyridin-3-yl)amino]-5-[(1R)-1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amineKi4.0 [1]
N-[3-(Dimethylamino)propyl]-6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideIC5035.0 [1]
N-[3-(Dimethylamino)propyl]-6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideKi44.0 [1]
12-(2-Aminopyrimidin-5-yl)-N-[(4-fluorophenyl)methyl]-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraene-5-carboxamideIC501.2 [1]
12-(2-Aminopyrimidin-5-yl)-N-[(4-fluorophenyl)methyl]-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraene-5-carboxamideKi9.2 [1]
5-[4-(4-Fluorophenyl)sulfonyl-10-morpholin-4-yl-1,4,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineIC501.1 [1]
5-[4-(4-Fluorophenyl)sulfonyl-10-morpholin-4-yl-1,4,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineKi2.55 [1]
5-[5-[2-(4-Fluorophenyl)ethyl]-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineIC508.0 [1]
5-[5-[2-(4-Fluorophenyl)ethyl]-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineKi5.9 [1]
5-[5-(4-Fluorophenyl)-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineIC500.5 [1]
5-[5-(4-Fluorophenyl)-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl]pyrimidin-2-amineKi3.3 [1]
12-(2-Aminopyrimidin-5-yl)-N-cyclohexyl-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraene-5-carboxamideIC509.6 [1]
12-(2-Aminopyrimidin-5-yl)-N-cyclohexyl-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraene-5-carboxamideKi3.1 [1]
N-[4-[[4-[2-(Difluoromethyl)-4-methoxybenzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]amino]cyclohexyl]methanesulfonamideIC506.1 [1], 8.0 [2]
5-(4-Cyclopropylsulfonyl-10-morpholin-4-yl-1,4,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl)pyrimidin-2-amineIC5026.1 [1]
5-(4-Cyclopropylsulfonyl-10-morpholin-4-yl-1,4,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl)pyrimidin-2-amineKi7.65 [1]
N-[2-[12-(2-Aminopyrimidin-5-yl)-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-5-yl]ethyl]methanesulfonamideIC508.1 [1]
N-[2-[12-(2-Aminopyrimidin-5-yl)-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-5-yl]ethyl]methanesulfonamideKi9.9 [1]
5-(5-Methylsulfonyl-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl)pyrimidin-2-amineIC5029.3 [1]
5-(5-Methylsulfonyl-10-morpholin-4-yl-1,5,8,11-tetrazatricyclo[7.4.0.02,7]trideca-2(7),8,10,12-tetraen-12-yl)pyrimidin-2-amineKi3.11 [1]
4-[6-(1H-Indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineIC5095.0 [1]
4-[6-(1H-Indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineKi181.0 [1]
6-(1H-Indazol-4-yl)-N-methyl-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideIC50110.0 [1]
6-(1H-Indazol-4-yl)-N-methyl-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideKi102.0 [1]
6-(1H-Indazol-4-yl)-N-(3-methoxypropyl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideIC5031.0 [1]
6-(1H-Indazol-4-yl)-N-(3-methoxypropyl)-8-morpholin-4-ylimidazo[1,2-a]pyrazine-2-carboxamideKi60.0 [1]
4-[5-Chloro-6-(1H-indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineIC50145.0 [1]
4-[5-Chloro-6-(1H-indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineKi210.0 [1]
4-[3-Bromo-6-(1H-indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineIC5047.0 [1]
4-[3-Bromo-6-(1H-indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]imidazo[1,2-a]pyrazin-8-yl]morpholineKi86.0 [1]
6-(1H-Indazol-4-yl)-8-morpholin-4-yl-N-(2-morpholin-4-ylethyl)imidazo[1,2-a]pyrazine-2-carboxamideIC5038.0 [1]
6-(1H-Indazol-4-yl)-8-morpholin-4-yl-N-(2-morpholin-4-ylethyl)imidazo[1,2-a]pyrazine-2-carboxamideKi65.0 [1]
6-(1H-Indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazine-5-carbonitrileIC50194.0 [1]
6-(1H-Indazol-4-yl)-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazine-5-carbonitrileKi410.0 [1]
5-[7-(3-Aminocyclobutyl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.94 [1], 1.35 [2]
5-[2-[(3S)-3-Methylmorpholin-4-yl]-7-(1-propan-2-ylsulfonylazetidin-3-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.23 [1], 2.3 [2]
5-[7-[3-(Methylamino)cyclobutyl]-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.99 [1], 2.12 [2]
5-[7-(3,3-Difluorocyclobutyl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.21 [1], 0.31 [2]
N-[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]-N-methylmethanesulfonamideKi0.23 [1], 0.72 [2]
5-[7-[(3S)-1-Methylsulfonylpyrrolidin-3-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.15 [1], 1.25 [2]
N-[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]-N-methylacetamideKi5.39 [1], 9.03 [2]
5-[7-[(1S)-3,3-Difluorocyclopentyl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.31 [1], 0.39 [2]
5-[7-[(1R)-3,3-Difluorocyclopentyl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.31 [1], 0.39 [2]
N-[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]acetamideKi5.83 [1], 9.7 [2]
(3S)-3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-N-methylpyrrolidine-1-sulfonamideKi0.12 [1], 0.79 [2]
3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-1-methylcyclobutan-1-olKi0.74 [1], 1.97 [2]
N-[3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-2,2,4,4-tetramethylcyclobutyl]acetamideKi1.14 [1], 7.68 [2]
Methyl 3-[4-(2-aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]azetidine-1-carboxylateKi0.23 [1]
3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutane-1-carbonitrileKi0.12 [1], 0.23 [2]
5-[7-(3-Fluorocyclobutyl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.23 [1], 0.51 [2]
5-[2-[(3S)-3-Methylmorpholin-4-yl]-7-[(3S)-1-methylsulfonylpyrrolidin-3-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.23 [1], 0.26 [2]
1-[(3S,4R)-3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-4-fluoropyrrolidin-1-yl]ethanoneKi2.44 [1], 5.08 [2]
5-[7-(1-Methylsulfonylazetidin-3-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.3 [1], 0.35 [2]
3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]azetidine-1-sulfonamideKi0.13 [1], 0.23 [2]
(3S)-3-[4-(2-Aminopyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-N,N-dimethylpyrrolidine-1-sulfonamideKi0.1 [1], 0.24 [2]
5-[7-[(3R)-1-Methylsulfonylpiperidin-3-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.51 [1], 0.6 [2]
(3R)-3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-N-methylpyrrolidine-1-sulfonamideKi0.47 [1], 3.25 [2]
Tert-butyl (3S)-3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]pyrrolidine-1-carboxylateKi0.18 [1], 0.36 [2]
(3S)-3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]pyrrolidine-1-sulfonamideKi0.13 [1], 0.23 [2]
5-[7-[(3S)-1-Ethylsulfonylpyrrolidin-3-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.09 [1], 0.49 [2]
5-[7-[(3S)-1-Cyclopropylsulfonylpyrrolidin-3-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.07 [1], 0.23 [2]
5-[2-Morpholin-4-yl-7-[(3S)-1-propan-2-ylsulfonylpyrrolidin-3-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.15 [1], 0.23 [2]
5-[7-(1-Ethylsulfonylazetidin-3-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.12 [1], 0.23 [2]
5-[2-Morpholin-4-yl-7-[(3R)-1-propan-2-ylsulfonylpyrrolidin-3-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.15 [1], 0.23 [2]
5-[7-(1-Cyclopropylsulfonylazetidin-3-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.12 [1], 0.23 [2]
5-[7-[(3S)-1-Ethylsulfonylpyrrolidin-3-yl]-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.06 [1], 0.23 [2]
5-[2-[(3S)-3-Methylmorpholin-4-yl]-7-(1-methylsulfonylazetidin-3-yl)-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.23 [1], 0.29 [2]
3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-N,N-dimethylazetidine-1-sulfonamideKi0.03 [1], 0.23 [2]
5-[7-[(3S)-1-Cyclopropylsulfonylpyrrolidin-3-yl]-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.06 [1], 0.23 [2]
5-[7-(1-Ethylsulfonylazetidin-3-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.1 [1], 0.23 [2]
(3R,4R)-3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-4-methoxy-N-methylpyrrolidine-1-sulfonamideKi0.18 [1], 0.26 [2]
Ethyl (3S)-3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]pyrrolidine-1-carboxylateKi0.09 [1], 0.23 [2]
5-[7-(1-Cyclopropylsulfonylazetidin-3-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.03 [1], 0.23 [2]
(3R,4R)-3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-4-hydroxy-N-methylpyrrolidine-1-sulfonamideKi0.13 [1], 0.23 [2]
3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]-N-methylazetidine-1-sulfonamideKi0.06 [1], 0.23 [2]
3-[4-(2-Aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]azetidine-1-sulfonamideKi0.22 [1], 0.23 [2]
Methyl (3S)-3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]pyrrolidine-1-carboxylateKi0.07 [1], 0.23 [2]
5-[2-[(3S)-3-Methylmorpholin-4-yl]-7-[(3S)-1-propan-2-ylsulfonylpyrrolidin-3-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.04 [1], 0.23 [2]
5-(7-Tert-butyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amineKi0.15 [1], 0.23 [2]
(1-Acetylazetidin-3-yl) (3R)-3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]pyrrolidine-1-carboxylateKi0.1 [1], 0.23 [2]
5-[7-(3-Methyl-1-methylsulfonylpyrrolidin-3-yl)-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl]pyrimidin-2-amineKi0.01 [1], 0.23 [2]
Tert-butyl N-[3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]carbamateKi0.43 [1], 0.64 [2]
Tert-butyl N-[3-[4-(2-aminopyrimidin-5-yl)-2-[(3S)-3-methylmorpholin-4-yl]-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]-N-methylcarbamateKi0.29 [1], 0.69 [2]
VorinostatIC5010000.0 [1]
[5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanolIC505577.0 [1]
Torin 1IC50250.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ PI3-kinase p110-alpha/p85-alpha Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/pi3-kinase-p110-alpha-p85-alpha-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ PI3-kinase p110-alpha/p85-alpha Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/pi3-kinase-p110-alpha-p85-alpha-inhibitors-ic50-ki.
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