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Tclin
PIK3CA
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

Protein Summary
Description
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) 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. 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. Regul ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000263967
  • ENSP00000263967
  • ENSG00000121879

Symbol
  • MCM
  • CWS5
  • MCAP
  • PI3K
  • CLAPO
  • CLOVE
  • MCMTC
  • PI3K-alpha
  • p110-alpha
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
biological term
1
hub protein
1
molecular function
1
protein domain
1
biological process
0.99


IDG Development Level Summary
Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1249.2   (req: < 5)
Gene RIFs: 1152   (req: <= 3)
Antibodies: 649   (req: <= 50)
Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1249.2   (req: >= 5)
Gene RIFs: 1152   (req: > 3)
Antibodies: 649   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 53
Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 1418
Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4
Active Ligands (1418)
1 – 10 of 1418
CHEMBL573339,CHEMBL538346
chemical structure image
CHEMBL521851
chemical structure image
CHEMBL428496
chemical structure image
CHEMBL1081312
chemical structure image
CHEMBL586702
chemical structure image
CHEMBL1879463
chemical structure image
CHEMBL3622533
chemical structure image
CHEMBL1922094
chemical structure image
CHEMBL1615189
chemical structure image
CHEMBL393525
chemical structure image
Protein Data Bank (44)
1 – 5 of 44
PDB Structure Id
Ligand
Method
Resolution (Å)
M.W. (kDa)
Pub Year
Title
PDB Structure Id
M.W.
Resolution
Pub Year
Pathways (381)
Activated NTRK2 signals through PI3K (R-HSA-9028335)

Click on a row in the table to change the structure displayed.

Items per page:
1 – 5 of 109
Data Source
Name
Explore in Pharos
Explore in Source
Reactome
Activated NTRK2 signals through PI3K
Reactome
Activated NTRK3 signals through PI3K
Reactome
Adaptive Immune System
Reactome
Axon guidance
Reactome
CD28 co-stimulation
Name
Explore in Pharos
Explore in Source
Activated NTRK2 signals through PI3K
Activated NTRK3 signals through PI3K
Adaptive Immune System
Axon guidance
CD28 co-stimulation
Gene Ontology Terms (60)
Items per page:
10
1 – 9 of 9
GO Term
Evidence
Assigned by
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Direct Assay (IDA)
MGI
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Sequence or structural Similarity (ISS)
BHF-UCL
Inferred from Electronic Annotation (IEA)
UniProtKB-KW
Inferred from Electronic Annotation (IEA)
Ensembl
Inferred from Electronic Annotation (IEA)
Ensembl
Inferred from Electronic Annotation (IEA)
UniProtKB-KW
Protein-Protein Interactions (767)
1 – 10 of 767
PIK3R3
Tbio
Family: Enzyme
Novelty: 0.02218437
p_int: 0.999991998
p_ni: 0.000008002
Score: 0.997
Data Source: BioPlex,Reactome,STRINGDB
PCBP1
Tbio
Novelty: 0.01171416
p_int: 0.999983432
p_ni: 0.000016567
Score: 0.278
Data Source: BioPlex,STRINGDB
GRB2
Tchem
Novelty: 0.00060543
p_int: 0.999769808
p_ni: 0.000230192
Score: 0.965
Data Source: BioPlex,Reactome,STRINGDB
HAVCR2
Tbio
Novelty: 0.00217571
p_int: 0.998423595
p_ni: 0.001576405
Data Source: BioPlex
FLRT1
Tdark
Novelty: 0.3774664
p_int: 0.998205284
p_ni: 0.001794713
p_wrong: 2e-9
Score: 0.318
Data Source: BioPlex,STRINGDB
BTN3A1
Tbio
Novelty: 0.03350752
p_int: 0.997026348
p_ni: 0.002963375
p_wrong: 0.000010277
Data Source: BioPlex
IL20RA
Tbio
Novelty: 0.03295383
p_int: 0.995638023
p_ni: 0.004361975
p_wrong: 2e-9
Data Source: BioPlex
ABCB9
Tbio
Family: Transporter
Novelty: 0.01804769
p_int: 0.993960824
p_ni: 0.006037693
p_wrong: 0.000001484
Data Source: BioPlex
SUN2
Tbio
Novelty: 0.01877097
p_int: 0.992856423
p_ni: 0.007143545
p_wrong: 3.2e-8
Score: 0.217
Data Source: BioPlex,STRINGDB
TMEM52B
Tdark
Novelty: 1
p_int: 0.991942501
p_ni: 0.008053341
p_wrong: 0.000004159
Data Source: BioPlex
Publication Statistics
PubMed Score  1249.20

PubMed score by year
PubTator Score  1569.79

PubTator score by year
Patents
Amino Acid Sequence
Residue Counts
Sequence
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIF
1-70
VSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFR
70-140
RNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLK
140-210
INHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLG
210-280
RMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRD
280-350
IDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHC
350-420
PLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMS
420-490
VIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVT
490-560
IPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQ
560-630
YLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLK
630-700
HLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECR
700-770
IMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLS
770-840
IGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFI
840-910
LGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERF
910-980
QEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGG
980-1050
WTTKMDWIFHTIKQHALN
1050-1068
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN