General Information of the Protein
Protein ID
PT07498
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Secondarily
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha
Phosphoinositide-3-kinase catalytic alpha polypeptide
Serine/threonine protein kinase PIK3CA
Gene Name
PIK3CA
Sequence
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLVTIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFVIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPIDSFTMPSYSRRISTATPYMNGETATKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHTGLSNRLARDNELRENDKEQLRALCTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRSFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRQPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQEYTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFTKQMNDAHHGGWTTKMDWIFHTIKQHALN
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Organism
Rattus norvegicus, Rat
Protein Classification
Enzyme
>
Transferase
Function
Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides. Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins (PubMed:20236230). Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. In addition to its lipid kinase activity, it displays a serine-protein kinase activity that results in the autophosphorylation of the p85alpha regulatory subunit as well as phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor and possibly others (By similarity). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).
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Uniprot ID
A0A0G2K344
Ensembl ID
ENSG00000121879
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000019 , Rat1
Compound ID Compound Name Compound Formula
CP0001158
US9284315, BEZ-235
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C30H23N5O
 1
1
IC50 = 5.3 nM
   TI
   LI
   LO
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CP0579027
(4S,5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0576748
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 42 nM
   TI
   LI
   LO
   TS
CP0576744
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-methyl-1,3-oxazolidin-2-one
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C17H18F3N7O3
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0007893
4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine
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C23H27N7O3S2
 1
1
IC50 = 52 nM
   TI
   LI
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   TS
CP0125999
2-amino-5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-1H-pyrimidin-6-one
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C16H21N7O3
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0545315
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0548467
(4S,5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 94 nM
   TI
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   LO
   TS
CP0577684
5-[6-(7-methoxy-2,3-dihydro-1,4-benzoxazin-4-yl)-2-morpholin-4-ylpyrimidin-4-yl]pyrimidin-2-amine
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C21H23N7O3
 1
1
IC50 = 108 nM
   TI
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CP0573794
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-[(1S)-1-hydroxyethyl]-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 109 nM
   TI
   LI
   LO
   TS
CP0545313
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 116 nM
   TI
   LI
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   TS
CP0001930
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
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C18H21F3N6O2
 1
1
IC50 = 117 nM
   TI
   LI
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   TS
CP0188346
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyrimidin-2-amine
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C17H20F3N7O2
 1
1
IC50 = 130 nM
   TI
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CP0545312
(4S)-3-[4-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-methyl-1,3-oxazolidin-2-one
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C18H19F3N6O3
 1
1
IC50 = 130 nM
   TI
   LI
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CP0543347
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-5,5-dimethyl-1,3-oxazolidin-2-one
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C19H22F3N7O4
 1
1
IC50 = 134 nM
   TI
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CP0576745
(5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 158 nM
   TI
   LI
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CP0577015
(3aS,6aS)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]oxazol-2-one
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C18H18F3N7O4
 1
1
IC50 = 214 nM
   TI
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CP0568134
(4S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one
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C18H20F3N7O4
 1
1
IC50 = 215 nM
   TI
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CP0574438
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-dimethylurea
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C17H20F3N7O2
 1
1
IC50 = 249 nM
   TI
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CP0543348
(4R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-4-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 256 nM
   TI
   LI
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CP0576740
3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazolidin-2-one
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C16H16F3N7O3
 1
1
IC50 = 256 nM
   TI
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CP0546964
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]pyrrolidin-2-one
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C18H19F3N6O2
 1
1
IC50 = 258 nM
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CP0579376
3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazinan-2-one
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C17H18F3N7O3
 1
1
IC50 = 264 nM
   TI
   LI
   LO
   TS
CP0576741
(5S)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
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C17H18F3N7O4
 1
1
IC50 = 277 nM
   TI
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CP0552713
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]piperidin-2-one
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C19H21F3N6O2
 1
1
IC50 = 369 nM
   TI
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CP0548095
2-[(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-methyl-2-oxo-1,3-oxazolidin-4-yl]acetonitrile
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C19H19F3N8O3
 1
1
IC50 = 376 nM
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CP0576738
2-amino-5-[6-[2-(2-hydroxyethyl)morpholin-4-yl]-2-morpholin-4-ylpyrimidin-4-yl]pyridine-4-carbonitrile
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C20H25N7O3
 1
1
IC50 = 476 nM
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CP0577685
3-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1,3-oxazolidin-2-one
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C17H17F3N6O3
 1
1
IC50 = 484 nM
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CP0568135
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]imidazolidin-2-one
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C17H18F3N7O2
 1
1
IC50 = 558 nM
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CP0579116
[(3R)-4-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]morpholin-3-yl]methanol
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C19H23F3N6O3
 1
1
IC50 = 601 nM
   TI
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CP0579375
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-3-phenylimidazolidin-2-one
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C23H22F3N7O2
 1
1
IC50 = 606 nM
   TI
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CP0576737
5-(2,6-dimorpholin-4-ylpyridin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
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C19H22F3N5O2
 1
1
IC50 = 739 nM
   TI
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CP0574436
5-[2-morpholin-4-yl-6-(2-phenylmorpholin-4-yl)pyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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C24H25F3N6O2
 1
1
IC50 = 1247 nM
   TI
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CP0552712
5-[6-(1,1-dioxo-1,4-thiazinan-4-yl)-2-morpholin-4-ylpyrimidin-4-yl]-4-(trifluoromethyl)pyridin-2-amine
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C18H21F3N6O3S
 1
1
IC50 = 1770 nM
   TI
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CP0568133
1-[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]-1-(2-hydroxyethyl)-3-methylurea
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C18H22F3N7O3
 1
1
IC50 = 3060 nM
   TI
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CP0545314
(4S,5R)-3-[4-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-6-morpholin-4-ylpyrimidin-2-yl]-5-methyl-4-[(1-oxo-1,4-thiazinan-4-yl)methyl]-1,3-oxazolidin-2-one
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C22H27F3N8O4S
 1
1
IC50 = 4600 nM
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CP0574440
2-[[6-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-2-morpholin-4-ylpyrimidin-4-yl]amino]-3-phenylpropan-1-ol
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C23H25F3N6O2
 1
1
IC50 = 6185 nM
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Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01045 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Homo sapiens, Human
PT01368 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Bos taurus, Bovine
PT03525 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Mus musculus, Mouse