General Information of the Protein
Protein ID
PT01368
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
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLRAICTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN
    Show/Hide
Organism
Bos taurus, Bovine
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 (PubMed:1322797, PubMed:14729945). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (By similarity). 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. 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 (By similarity). 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 (PubMed:15178440, PubMed:14729945). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).
    Show/Hide
Uniprot ID
P32871
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0869038
5-Phenyl-3-(1'-morpholinoethyl)-6-thioxo-5,6,8,9,10,10ahexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidin-1(2H)-one
   Show/Hide
C21H25N5O2S
 1
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
CP0873042
N'-[(1E)-(6-cyanoimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride
   Show/Hide
C17H15ClN6O4S
 1
1
IC50 = 0.26 nM
   TI
   LI
   LO
   TS
CP0845652
PIK-75
   Show/Hide
C16H15BrClN5O4S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0891722
5-Ethyl-3-(10-morpholinoethyl)-6-thioxo-5,6,8,9,10,10ahexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidin-1(2H)-one
   Show/Hide
C17H25N5O2S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0849535
5-Phenyl-3-(morpholinomethyl)-6-thioxo-5,6,8,9,10,10a-hexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidin-1(2H)-one
   Show/Hide
C20H23N5O2S
 1
1
IC50 = 0.5 nM
   TI
   LI
   LO
   TS
CP0946482
N'-[(1E)-(6-chloroimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride
   Show/Hide
C16H15Cl2N5O4S
 1
1
IC50 = 0.77 nM
   TI
   LI
   LO
   TS
CP0867448
5-Ethyl-3-(morpholinomethyl)-6-thioxo-5,6,8,9,10,10ahexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidin-1(2H)-one
   Show/Hide
C16H23N5O2S
 1
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0864151
3-(4-Methoxyphenyl)-5-ethyl-1-morpholino-6-thioxo-5,6,8,9,10,10a-hexahydropyrido[3,2-e]pyrrolo[1,2-c]pyrimidine-2-carbonitrile
   Show/Hide
C24H27N5O2S
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0886055
3-(3,4-Dimethoxyphenyl)-5-ethyl-1-morpholino-6-thioxo-5,6,8,9,10,10a-hexahydropyrido[3,2-e]pyrrolo[1,2-c]pyrimidine-2-carbonitrile
   Show/Hide
C25H29N5O3S
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0640938
3-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)phenol
   Show/Hide
C16H16ClN3O2S
 1
1
IC50 = 2.5 nM
   TI
   LI
   LO
   TS
CP0051080
3-{6-bromo-2-methylimidazo[1,2-a]pyridin-3-yl}-1-[(2-methyl-5-nitrobenzene)sulfonyl]-1H-pyrazole
   Show/Hide
C18H14BrN5O4S
 1
1
IC50 = 3.1 nM
   TI
   LI
   LO
   TS
CP0642162
3-(4-morpholin-4-yl-pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)-phenol
   Show/Hide
C19H17ClN4O3
 1
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
CP0382537
8-ethyl-11-(3-hydroxy-4-methoxyphenyl)-13-morpholin-4-yl-7-sulfanylidene-6,8,10-triazatricyclo[7.4.0.02,6]trideca-1(9),10,12-triene-12-carbonitrile
   Show/Hide
C24H27N5O3S
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0869037
3-(3-Methoxyphenyl)-5-ethyl-1-morpholino-6-thioxo-5,6,8,9,10,10a-hexahydropyrido[3,2-e]pyrrolo[1,2-c]pyrimidine-2-carbonitrile
   Show/Hide
C24H27N5O2S
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0949871
N'-[(1E)-(6-fluoroimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride
   Show/Hide
C16H15ClFN5O4S
 1
1
IC50 = 5.3 nM
   TI
   LI
   LO
   TS
CP0920157
N,2-dimethyl-N'-[(1E)-(6-methylimidazo[1,2-a]pyridin-3-yl)methylene]-5-nitrobenzenesulfonohydrazide hydrochloride
   Show/Hide
C17H18ClN5O4S
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0869039
3-(3-Hydroxyphenyl)-5-ethyl-1-morpholino-6-thioxo-5,6,8,9,10,10a-hexahydropyrido[3,2-e]pyrrolo[1,2-c]pyrimidine-2-carbonitrile
   Show/Hide
C23H25N5O2S
 1
1
IC50 = 7.7 nM
   TI
   LI
   LO
   TS
CP0873047
N'-[(1E)-(6-trifluoromethylimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazidehydrochloride
   Show/Hide
C17H15ClF3N5O4S
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0942058
N'-[(1E)-1-(6-bromoimidazo[1,2-a]pyridin-3-yl)ethylidene]-2-methyl-5-nitrobenzenesulfonohydrazide
   Show/Hide
C16H14BrN5O4S
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0895778
N'-[(1E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-2-methyl-5-nitrobenzenesulfonohydrazide
   Show/Hide
C15H12BrN5O4S
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0897964
N'-[(1E)-1-(6-bromoimidazo[1,2-a]pyridin-3-yl)ethylidene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
   Show/Hide
C17H16BrN5O4S
 1
1
IC50 = 81 nM
   TI
   LI
   LO
   TS
CP0942057
N'-[(1E)-1-(6-bromo-2-methylimidazo[1,2-a]pyridin-3-yl)ethylidene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
   Show/Hide
C18H18BrN5O4S
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0865022
5-Ethyl-3-(3-methoxyphenyl)-1-morpholino-8,9,10,10a-tetrahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C22H27N5O2S
 1
1
IC50 = 234 nM
   TI
   LI
   LO
   TS
CP0877558
ethyl 3-((E)-{methyl[(2-methyl-5-nitrophenyl)sulfonyl]hydrazono}methyl)imidazo[1,2-a]pyridine-6-carboxylatehydrochloride
   Show/Hide
C19H20ClN5O6S
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0865020
5-Ethyl-3-(4-methoxyphenyl)-1-morpholino-8,9,10,10a-tetrahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C22H27N5O2S
 1
1
IC50 = 387 nM
   TI
   LI
   LO
   TS
CP0949872
N'-[(1E)-1-(6-bromo-2-methylimidazo[1,2-a]pyridin-3-yl)ethylidene]-2-methyl-5-nitrobenzenesulfonohydrazide
   Show/Hide
C17H16BrN5O4S
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0002420
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
   Show/Hide
C19H17NO3
 1
1
IC50 = 630 nM
   TI
   LI
   LO
   TS
CP0051081
1-[(4-fluorobenzene)sulfonyl]-3-{2-methylimidazo[1,2-a]pyridin-3-yl}-1H-pyrazole
   Show/Hide
C17H13FN4O2S
 1
1
IC50 = 670 nM
   TI
   LI
   LO
   TS
CP0865021
3-(4-Methoxyphenyl)-1-morpholino-5-phenyl-8,9,10,10atetrahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C26H27N5O2S
 1
1
IC50 = 678 nM
   TI
   LI
   LO
   TS
CP0881577
3-(3-Methoxyphenyl)-1-morpholino-5-phenyl-8,9,10,10atetrahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C26H27N5O2S
 1
1
IC50 = 695 nM
   TI
   LI
   LO
   TS
CP0946481
3-((E)-{methyl[(2-methyl-5-nitrophenyl)sulfonyl]-hydrazono}methyl)imidazo[1,2-a]pyridine-6-carboxamidehydrochloride
   Show/Hide
C17H17ClN6O5S
 1
1
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0873711
1-Morpholino-3-(morpholinomethyl)-5-phenyl-8,9,10,10ahexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C24H30N6O2S
 1
1
IC50 = 2340 nM
   TI
   LI
   LO
   TS
CP0873710
1-Morpholino-3-(1'-morpholinoethyl)-5-phenyl-8,9,10,10ahexahydropyrimido[5,4-e]pyrrolo[1,2-c]pyrimidine-6(5H)-thione
   Show/Hide
C25H32N6O2S
 1
1
IC50 = 5490 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0051080
3-{6-bromo-2-methylimidazo[1,2-a]pyridin-3-yl}-1-[(2-methyl-5-nitrobenzene)sulfonyl]-1H-pyrazole
   Show/Hide
C18H14BrN5O4S
 1
1 IC50 = 3.1 nM
CP0002420
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
   Show/Hide
C19H17NO3
 1
1 IC50 = 630 nM
CP0051081
1-[(4-fluorobenzene)sulfonyl]-3-{2-methylimidazo[1,2-a]pyridin-3-yl}-1H-pyrazole
   Show/Hide
C17H13FN4O2S
 1
1 IC50 = 670 nM
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
PT03525 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Mus musculus, Mouse
PT07498 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Rattus norvegicus, Rat