ChEMBL logo

ChEMBL

spacer
ChEMBL Statistics
  Loading Statistics...
spacer

Target Report Card

Target Name and Classification

Target ID CHEMBL4005
Target Type SINGLE PROTEIN
Preferred Name PI3-kinase p110-alpha subunit
Synonyms PI3-kinase subunit alpha | PI3K-alpha | PI3Kalpha | PIK3CA | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Phosphoinositide-3-kinase catalytic alpha polypeptide | PtdIns-3-kinase subunit alpha | PtdIns-3-kinase subunit p110-alpha | Serine/threonine protein kinase PIK3CA | p110alpha
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme

Target Components

Component Description Relationship Accession
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform SINGLE PROTEIN P42336

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3559703 PI3-kinase class I PROTEIN COMPLEX GROUP
CHEMBL2111367 PI3-kinase p110-alpha/p85-alpha PROTEIN COMPLEX

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL2396661 ALPELISIB PI3-kinase p110-alpha subunit inhibitor 3 PubMed PubMed
CHEMBL3545052 CUDC-907 PI3-kinase p110-alpha subunit inhibitor 2 Other PubMed
CHEMBL3545379 MLN-1117 PI3-kinase p110-alpha subunit inhibitor 2 PubMed PubMed
CHEMBL1258517 PKI-179 PI3-kinase p110-alpha subunit inhibitor 1 PubMed
CHEMBL3545055 INK-1117 PI3-kinase p110-alpha subunit inhibitor 1
CHEMBL3545245 BAY-1082439 PI3-kinase p110-alpha subunit inhibitor 1 Other
CHEMBL3545323 PWT-33579 PI3-kinase p110-alpha subunit inhibitor 1

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000121879
Ensembl ENSG00000121879
GO Cellular Component GO:0005622 (intracellular)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005942 (phosphatidylinositol 3-kinase complex)
GO:0005943 (phosphatidylinositol 3-kinase complex, class IA)
GO:0030027 (lamellipodium)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016303 (1-phosphatidylinositol-3-kinase activity)
GO:0016740 (transferase activity)
GO:0030295 (protein kinase activator activity)
GO:0035004 (phosphatidylinositol 3-kinase activity)
GO:0035005 (1-phosphatidylinositol-4-phosphate 3-kinase activity)
GO:0043560 (insulin receptor substrate binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO Biological Process GO:0001525 (angiogenesis)
GO:0001889 (liver development)
GO:0001944 (vasculature development)
GO:0006006 (glucose metabolic process)
GO:0006468 (protein phosphorylation)
GO:0006661 (phosphatidylinositol biosynthetic process)
GO:0006909 (phagocytosis)
GO:0007173 (epidermal growth factor receptor signaling pathway)
GO:0010468 (regulation of gene expression)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0030168 (platelet activation)
GO:0031295 (T cell costimulation)
GO:0032147 (activation of protein kinase activity)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0036092 (phosphatidylinositol-3-phosphate biosynthetic process)
GO:0038028 (insulin receptor signaling pathway via phosphatidylinositol 3-kinase)
GO:0038095 (Fc-epsilon receptor signaling pathway)
GO:0038096 (Fc-gamma receptor signaling pathway involved in phagocytosis)
GO:0038128 (ERBB2 signaling pathway)
GO:0040014 (regulation of multicellular organism growth)
GO:0043457 (regulation of cellular respiration)
GO:0043491 (protein kinase B signaling)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0043542 (endothelial cell migration)
GO:0044029 (hypomethylation of CpG island)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048010 (vascular endothelial growth factor receptor signaling pathway)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0050852 (T cell receptor signaling pathway)
GO:0050900 (leukocyte migration)
GO:0060048 (cardiac muscle contraction)
GO:0060612 (adipose tissue development)
GO:0071333 (cellular response to glucose stimulus)
GO:0097009 (energy homeostasis)
GO:0098779 (mitophagy in response to mitochondrial depolarization)
GO:2000270 (negative regulation of fibroblast apoptotic process)
GO:2000653 (regulation of genetic imprinting)
GO:2000811 (negative regulation of anoikis)
Wikipedia P110%CE%B1

Target Cross References - Protein

canSAR P42336
CGD Cowden syndrome 5
Human Protein Atlas ENSG00000121879
IntAct P42336
Guide to Pharmacology 2153
Open Targets ENSG00000121879
PharmGKB PA33308
Pharos P42336 (Tchem)
Reactome R-HSA-109704 (PI3K Cascade.)
R-HSA-114604 (GPVI-mediated activation cascade.)
R-HSA-1236382 (Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants.)
R-HSA-1250342 (PI3K events in ERBB4 signaling.)
R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-1433557 (Signaling by SCF-KIT.)
R-HSA-1660499 (Synthesis of PIPs at the plasma membrane.)
R-HSA-180292 (GAB1 signalosome.)
R-HSA-1839117 (Signaling by cytosolic FGFR1 fusion mutants.)
R-HSA-186763 (Downstream signal transduction.)
R-HSA-1963642 (PI3K events in ERBB2 signaling.)
R-HSA-198203 (PI3K/AKT activation.)
R-HSA-202424 (Downstream TCR signaling.)
R-HSA-2029485 (Role of phospholipids in phagocytosis.)
R-HSA-210993 (Tie2 Signaling.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-2424491 (DAP12 signaling.)
R-HSA-2730905 (Role of LAT2/NTAL/LAB on calcium mobilization.)
R-HSA-373753 (Nephrin interactions.)
R-HSA-388841 (Costimulation by the CD28 family.)
R-HSA-389357 (CD28 dependent PI3K/Akt signaling.)
R-HSA-392451 (G beta:gamma signalling through PI3Kgamma.)
R-HSA-416476 (G alpha (q) signalling events.)
R-HSA-416482 (G alpha (12/13) signalling events.)
R-HSA-4420097 (VEGFA-VEGFR2 Pathway.)
R-HSA-512988 (Interleukin-3, 5 and GM-CSF signaling.)
R-HSA-5637810 (Constitutive Signaling by EGFRvIII.)
R-HSA-5654689 (PI-3K cascade:FGFR1.)
R-HSA-5654695 (PI-3K cascade:FGFR2.)
R-HSA-5654710 (PI-3K cascade:FGFR3.)
R-HSA-5654720 (PI-3K cascade:FGFR4.)
R-HSA-5655253 (Signaling by FGFR2 in disease.)
R-HSA-5655291 (Signaling by FGFR4 in disease.)
R-HSA-5655302 (Signaling by FGFR1 in disease.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8851907 (MET activates PI3K/AKT signaling.)
R-HSA-8853334 (Signaling by FGFR3 fusions in cancer.)
R-HSA-8853338 (Signaling by FGFR3 point mutants in cancer.)
R-HSA-8853659 (RET signaling.)
R-HSA-912526 (Interleukin receptor SHC signaling.)
R-HSA-912631 (Regulation of signaling by CBL.)
UniProt P42336 Q14CW1 Q99762

Target Cross References - Domain

InterPro IPR000008 (C2_dom.)
IPR000341 (PI3K_Ras-bd_dom.)
IPR000403 (PI3/4_kinase_cat_dom.)
IPR001263 (PInositide-3_kin_accessory_dom.)
IPR002420 (PI3K_C2_dom.)
IPR003113 (PI3K_adapt-bd_dom.)
IPR011009 (Kinase-like_dom.)
IPR015433 (PI_Kinase.)
IPR016024 (ARM-type_fold.)
IPR018936 (PI3/4_kinase_CS.)
IPR029071 (Ubiquitin-rel_dom.)
Pfam PF00454 (PI3_PI4_kinase)
PF00613 (PI3Ka)
PF00792 (PI3K_C2)
PF00794 (PI3K_rbd)
PF02192 (PI3K_p85B)

Target Cross References - Structure

PDBe 2RD0 3HHM 3HIZ 3ZIM 4JPS 4L1B 4L23 4L2Y 4OVU 4OVV 4TUU 4TV3 4WAF 4YKN 4ZOP 5DXH 5DXT 5FI4 5ITD
CREDO 2RD0 3HHM 3HIZ 3ZIM 4JPS 4L1B 4L23 4L2Y 4OVU 4OVV 4TUU 4TV3 4WAF 4YKN 4ZOP 5DXH 5DXT 5FI4 5ITD
spacer
spacer