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(2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
(5Z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione
1,2-bis-(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
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i.e. BAPTA-AM, a cell-penetrating Ca2+-chelator
2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid
2-amino-N-[(1S)-1-[8-[(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(morpholin-4-yl)-1H-benzimidazole-4-carboxylic acid
3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide
3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol
4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one
5-[2,6-bis(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
6-[5-(2,2-dimethylpropane-1-sulfonyl)pyridin-3-yl]-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-2-amine
8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-(morpholin-4-yl)-4-oxo-4H-1-benzopyran-6-carboxamide
calpeptin
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inhibits proteolytic activation of enzyme form PI3K C2beta in brush border plasma membranes
Isoflurane
ISO, inhibits KCl-stimulated PI3K-C2alpha membrane translocation
Mn2+
3.5 mM, instead of Mg2+, almost complete inhibition
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide
N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide
N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide
Nonidet P-40
0.5%, almost complete inhibition
sevoflurane
SEVO, inhibits KCl-stimulated PI3K-C2alpha membrane translocation
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Triton X-100
0.5%, almost complete inhibition
[6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](morpholin-4-yl)methanone
(2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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(2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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(5Z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione
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(5Z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione
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2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid
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2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid
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2-amino-N-[(1S)-1-[8-[(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
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2-amino-N-[(1S)-1-[8-[(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
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2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(morpholin-4-yl)-1H-benzimidazole-4-carboxylic acid
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2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(morpholin-4-yl)-1H-benzimidazole-4-carboxylic acid
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3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide
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3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide
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3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol
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3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol
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4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one
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4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one
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5-[2,6-bis(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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5-[2,6-bis(morpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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6-[5-(2,2-dimethylpropane-1-sulfonyl)pyridin-3-yl]-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-2-amine
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6-[5-(2,2-dimethylpropane-1-sulfonyl)pyridin-3-yl]-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-2-amine
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8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-(morpholin-4-yl)-4-oxo-4H-1-benzopyran-6-carboxamide
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8-[(1R)-1-(3,5-difluoroanilino)ethyl]-N,N-dimethyl-2-(morpholin-4-yl)-4-oxo-4H-1-benzopyran-6-carboxamide
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adipokines
block insulin signalling via PI3K isozymes
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adipokines
block insulin signalling via PI3K isozymes
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Caffeine
might inhibit the enzyme
Caffeine
might inhibit the enzyme
ceramide
selective inhibition of PI3KC2beta
ceramide
selective inhibition of PI3KC2beta
cytokines
block insulin signalling via PI3K isozymes
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cytokines
block insulin signalling via PI3K isozymes
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dactolisib
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duvelisib
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GDC-0941
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LY294002
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IC50: 0.019 mM, maximal inhibition at 1 mM
LY294002
a PI3K inhibitor, inhibits KCl-elicited rapid and sustained contraction of rat aortic smooth muscle
N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
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N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide
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N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide
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N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide
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N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide
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N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide
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N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide
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N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide
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naringenin
might inhibit the enzyme
naringenin
might inhibit the enzyme
Wortmannin
IC50: 11 nM
Wortmannin
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IC50: 420 nM, maximal inhibition at 10 mM
Wortmannin
class I isozyme inhibitor, isozyme PI3K-C2alpha is resistant to inhibition
Wortmannin
low inhibition
Wortmannin
class I isozyme inhibitor, isozyme PI3K-C2alpha is resistant to inhibition
Wortmannin
low inhibition
Wortmannin
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phosphoinositide 3-kinase C2beta
Wortmannin
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a pan-PI3K inhibitor
ZSTK474
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[6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](morpholin-4-yl)methanone
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[6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](morpholin-4-yl)methanone
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additional information
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introduction of phosphatidylserine, produces an 8fold decrease in Vmax for ATP using phosphatidylinositol. Without phosphatidylserine, phosphatidylinositol 4-phosphate produces non-linear enzyme kinetics
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additional information
enzyme is regulated by several feedback inhibition possibilities in the insulin signalling pathway, overview
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD 3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by NVP-BYL719/buparlisib, 5-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]propyl]quinazolin-4(3H)-one, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD 3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by NVP-BYL719/buparlisib, 5-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]propyl]quinazolin-4(3H)-one, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD 3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by NVP-BYL719/buparlisib, 5-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]propyl]quinazolin-4(3H)-one, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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additional information
enzyme is regulated by several feedback inhibition possibilities in the insulin signalling pathway, overview
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by buparlisib, idelalisib, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by buparlisib, idelalisib, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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additional information
no or poor inhibition by buparlisib, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, and N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide; no or poor inhibition by buparlisib, idelalisib, 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol, (8S)-2-[(3R)-3-methylmorpholin-4-yl]-9-(3-methyl-2-oxobutyl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, 3-amino-N-[3-(3,5-dimethoxyanilino)pyrazin-2-yl]benzene-1-sulfonamide, N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide; no or poor inhibition by GDC-0941, (2S)-N1-[4-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide, 2-([(1R)-1-[7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino)benzoic acid, idelalisib, N-(7,8-dimethoxy-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyridine-3-carboxamide, N-(5-[4-chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methyl-1,3-thiazol-2-yl)acetamide, 4-[(3-chloro-4-fluorophenyl)methyl]-6-[(Z)-(4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]-2H-1,4-benzoxazin-3(4H)-one, dactolisib, ZSTK474, AZD3147, 5-[4-[(methanesulfonyl)methyl]-6-(morpholin-4-yl)pyrimidin-2-yl]-1H-indole, gedatolisib, 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)[4,5'-bipyrimidine]-2,2'-diamine, 1-([2-[(2-chloropyridin-4-yl)amino]-4'-(cyclopropylmethyl)[4,5'-bipyrimidin]-2'-yl]amino)-2-methylpropan-2-ol, SAR405, (2S)-2-amino-1-(4-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)-1,3,5-triazin-2-yl]piperazin-1-yl)-3-phenylpropan-1-one, N-[4-(morpholin-4-yl)-2-[3-[(naphthalene-2-sulfonyl)amino]phenyl]quinazolin-6-yl]acetamide, N-[2-[3-[(benzenesulfonyl)amino]phenyl]-4-(morpholin-4-yl)quinazolin-6-yl]acetamide, N-(3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl)-2-methylalaninamide, N-[3-(3,5-dimethoxyanilino)quinoxalin-2-yl]-4-fluorobenzene-1-sulfonamide, and N-[3-(2-chloro-5-hydroxyanilino)pyrazin-2-yl]benzenesulfonamide
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