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2.7.1.153: phosphatidylinositol-4,5-bisphosphate 3-kinase

This is an abbreviated version!
For detailed information about phosphatidylinositol-4,5-bisphosphate 3-kinase, go to the full flat file.

Word Map on EC 2.7.1.153

Reaction

ATP
+
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
=
ADP
 +
1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate

Synonyms

class I phosphoinositide 3-kinase, class I PI3K, class IA phosphatidylinositol 3-kinase, class IA phosphatidylinositol-4,5-bisphosphate 3-kinase, CXCR2/phosphatidylinositol 3-kinase gamma, kinase (phosphorylating), phosphatidylinositol 4,5-diphosphate 3-, More, p101-PI3K, p110alpha, p110beta, p110delta, p110delta PI 3-kinase, p110gamma/p101, P120-PI3K, phosphatidyl-inositol-3-kinase, phosphatidylinositol (4,5)-bisphosphate 3-hydroxykinase, phosphatidylinositol 3'-kinase, phosphatidylinositol 3-hydroxyl kinase, phosphatidylinositol 3-kinase alpha, phosphatidylinositol 3-kinase gamma, phosphatidylinositol-4,5-bisphosphate 3-kinase, phosphoinositide 3-kinase, phosphoinositide 3-kinase p110delta, phosphoinositol 3-kinase, PI 3-K, PI 3-kinase, PI-3K, PI3-K, PI3-kinase, PI3K, PI3K p110delta, PI3Kalpha, PI3Kbeta, PI3Kdelta, PI3Kgamma, PI3Kp110delta, PIK3, PIK3CA, Pik3r1, PtdIns(4,5)P2 3-OH kinase, PtdIns-3-kinase p101, PtdIns-3-kinase p110, PtdInsP 3-OH-kinase, type I phosphoinositide 3-kinase

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.153 phosphatidylinositol-4,5-bisphosphate 3-kinase

IC50 Value

IC50 Value on EC 2.7.1.153 - phosphatidylinositol-4,5-bisphosphate 3-kinase

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000001
1-[2-methyl-3-(trifluoromethyl)benzyl]-2-methyl-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000003
1-[2-methyl-3-(trifluoromethyl)benzyl]-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000001
1-[2-methyl-3-(trifluoromethyl)benzyl]-7-[(2R)-2-methylmorpholin-2-yl]-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000024
1-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]-3-[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]urea
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000004 - 0.0013
2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.0000003 - 0.00032
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.0000006 - 0.00079
2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
0.00014 - 0.0016
3-(2-morpholino-6-(2-(pyridin-4-yl)ethylamino)pyrimidin-4-yl)phenol
0.00011 - 0.00073
3-(2-morpholino-6-(pyridin-2-ylmethoxy)pyrimidin-4-yl)phenol
0.000044 - 0.0001
3-(4-morpholino-6-(pyridin-2-yl)pyrimidin-2-yl)phenol
0.0000025 - 0.00082
3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
0.00058
3-[4-(4-morpholinyl)thieno(3,2-d)pyrimidin-2-yl]-phenol
Homo sapiens
-
versus p110alpha PI3K
0.000002 - 0.000009
4-(2-((6-methoxypyridin-3-yl)amino)-5-((4-(methylsulfonyl)piperazin-1-yl)methyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine
0.000001 - 0.000007
4-[2-[(6-methoxypyridin-3-yl)amino]-5-phenylpyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
0.000002 - 0.000005
4-[5-(3,6-dihydro-2H-pyran-4-yl)-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
0.00025
5-[2,2-difluoro-benzo(1,3)-dioxol-5-ylmethylene]-thiazolidine-2,4-dione
Homo sapiens
-
about, versus p110gamma PI3K
0.00000022 - 0.0000014
6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole
0.008
LY294002
Homo sapiens
-
inhibition of bacterial entry into macrophages
0.0000009
N-[2-(dimethylamino)ethyl]-N-methyl-4-[([4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]carbamoyl)amino]benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00004
TGX-221
Homo sapiens
-
about, versus p110beta PI3K
0.000006
TGX-221-R
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000025
Wortmannin
Homo sapiens
-
inhibition of bacterial entry into macrophages
0.000052 - 0.00035
[(4-[2-[(3-hydroxyphenyl)amino]-1H-benzimidazol-1-yl]-1,3,5-triazin-2-yl)amino]acetonitrile
0.000021
[3-[4-morpholin-4-yl-7-(pyrrolidin-1-ylmethyl)-5H-pyrrolo-[3,2-d ]pyrimidin-2-yl]phenyl]methanol
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
additional information
additional information
Homo sapiens
-
IC50 value of inhibitor 4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol is 2 nmol/l against recombinant isoform p110alpha, 3 nmol/l against recombinant isoform p110beta, 3 nmol/l against recombinant isoform p110delta, 15 nmol/l against recombinant isoform p110agamma
-