phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha | Phosphatidylinositol-4,5-bisphosphate 3-kinase family | IUPHAR/BPS Guide to PHARMACOLOGY

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phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

target has curated data in GtoImmuPdb

Target id: 2153

Nomenclature: phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

Abbreviated Name: PI3Kα

Family: Phosphatidylinositol-4,5-bisphosphate 3-kinase family, Phosphatidylinositol kinases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1068 3q26.3 PIK3CA phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Mouse - 1068 3 B Pik3ca phosphatidylinositol-4
Rat - 1068 2 q25 Pik3ca phosphatidylinositol-4
Previous and Unofficial Names
caPI3K | PI3K | PI3Kalpha | PtdIns-3-kinase subunit alpha | p110α/PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | phosphatidylinositol-4
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kalpha
PDB Id:  3ZIM
Resolution:  2.85Å
Species:  Human
References:  42
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of the C2 domain from human PI3-kinase p110 subunit alpha
PDB Id:  2ENQ
Resolution:  0.0Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.1.153
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
neolymphostin A Hs Inhibition 9.1 pKd 9
pKd 9.1 (Kd 8.8x10-10 M) [9]
Description: Determined using an active-site dependent competition binding assay.
bimiralisib Hs Inhibition 8.8 pKd
pKd 8.8 (Kd 1.5x10-9 M)
wortmannin Hs Inhibition 8.3 pKd 9
pKd 8.3 (Kd 5.4x10-9 M) [9]
IPI549 Hs Inhibition 7.8 pKd 19
pKd 7.8 (Kd 1.7x10-8 M) [19]
quinostatin Hs Inhibition 6.2 pKd 61
pKd 6.2 (Kd 6x10-7 M) [61]
Description: In vitro binding affinity to recombinant complex of PI3K alpha regulatory and catalytic subunits.
PQR620 Hs Inhibition 6.0 pKd 49
pKd 6.0 (Kd 1x10-6 M) [49]
GDC-0077 Hs Inhibition 10.5 pKi 5
pKi 10.5 (Ki 3.4x10-11 M) [5]
taselisib Hs Inhibition 9.5 – 10.1 pKi 5,43
pKi 10.1 (Ki 9x10-11 M) [5]
pKi 9.5 (Ki 2.9x10-10 M) [43]
PF-04691502 Hs Inhibition 9.2 pKi 38
pKi 9.2 (Ki 5.7x10-10 M) [38]
compound 82 [PMID: 21332118] Hs Inhibition 8.9 pKi 16
pKi 8.9 (Ki 1.2x10-9 M) [16]
pictilisib Hs Inhibition 8.6 pKi 5
pKi 8.6 (Ki 2.56x10-9 M) [5]
omipalisib Hs Inhibition 7.7 pKi 34
pKi 7.7 (Ki 1.9x10-8 M) [34]
wortmannin Hs Inhibition 6.9 pKi 25
pKi 6.9 (Ki 1.2x10-7 M) [25]
compound 22 [PMID: 24754609] Hs Inhibition 6.9 pKi 13
pKi 6.9 (Ki 1.32x10-7 M) [13]
PQR620 Hs Inhibition 5.4 pKi 49
pKi 5.4 (Ki 4.203x10-6 M) [49]
gedatolisib Hs Inhibition 9.4 pIC50 56
pIC50 9.4 (IC50 4x10-10 M) [56]
HS-173 Hs Inhibition 9.1 pIC50 32
pIC50 9.1 (IC50 8x10-10 M) [32]
PIK-75 Hs Inhibition 8.2 – 9.5 pIC50 28,35
pIC50 9.5 (IC50 3x10-10 M) [28]
pIC50 8.2 (IC50 5.8x10-9 M) [35]
PI-103 Hs Inhibition 8.7 pIC50 50
pIC50 8.7 (IC50 2x10-9 M) [50]
GSK1059615 Hs Inhibition 8.7 pIC50 34
pIC50 8.7 (IC50 2x10-9 M) [34]
GDC0084 Hs Inhibition 8.7 pIC50 29
pIC50 8.7 (IC50 2x10-9 M) [29]
panulisib Hs Inhibition 8.7 pIC50 31
pIC50 8.7 (IC50 2.2x10-9 M) [31]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
pictilisib Hs Inhibition 8.5 pIC50 20
pIC50 8.5 (IC50 3x10-9 M) [20]
dactolisib Hs Inhibition 8.4 pIC50 40
pIC50 8.4 (IC50 4x10-9 M) [40]
BGT-226 Hs Inhibition 8.4 pIC50 41
pIC50 8.4 (IC50 4x10-9 M) [41]
KU-0060648 Hs Inhibition 8.4 pIC50 8
pIC50 8.4 (IC50 4x10-9 M) [8]
apitolisib Hs Inhibition 8.3 pIC50 53
pIC50 8.3 (IC50 4.8x10-9 M) [53]
alpelisib Hs Inhibition 8.3 pIC50 22
pIC50 8.3 (IC50 5x10-9 M) [22]
AZD8835 Hs Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 6.2x10-9 M) [4]
LY3023414 Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.1x10-9 M) [3]
MEN1611 Hs Inhibition 7.8 pIC50 45
pIC50 7.8 (IC50 1.4x10-8 M) [45]
ZSTK474 Hs Inhibition 7.8 pIC50 59
pIC50 7.8 (IC50 1.6x10-8 M) [59]
VS-5584 Hs Inhibition 7.8 pIC50 27
pIC50 7.8 (IC50 1.6x10-8 M) [27]
fimepinostat Hs Inhibition 7.7 pIC50 48
pIC50 7.7 (IC50 1.9x10-8 M) [48]
buparlisib Hs Inhibition 7.5 pIC50 6
pIC50 7.5 (IC50 3x10-8 M) [6]
AZD8186 Hs Inhibition 7.5 pIC50 26
pIC50 7.5 (IC50 3.5x10-8 M) [26]
pilaralisib Hs Inhibition 7.4 pIC50 59
pIC50 7.4 (IC50 3.9x10-8 M) [59]
PP121 Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5.2x10-8 M) [2]
PI 3-Kg inhibitor Hs Inhibition 7.2 pIC50 7
pIC50 7.2 (IC50 6x10-8 M) [7]
compound 11j [PMID: 23021994] Hs Inhibition 7.0 pIC50 24
pIC50 7.0 (IC50 9.2x10-8 M) [24]
serabelisib Hs Inhibition >7.0 pIC50 51
pIC50 >7.0 (IC50 <1x10-7 M) [51]
RV1729 Hs Inhibition 6.7 pIC50 33
pIC50 6.7 (IC50 1.93x10-7 M) [33]
Description: In a biochemical enzyme activity assay.
LY 294002 Hs Inhibition 6.7 pIC50 8,12
pIC50 6.7 (IC50 3x10-7 – 2x10-7 M) [8,12]
sapanisertib Hs Inhibition 6.7 pIC50 30
pIC50 6.7 (IC50 2.19x10-7 M) [30]
leniolisib Hs Inhibition 6.6 pIC50 14
pIC50 6.6 (IC50 2.62x10-7 M) [14]
Description: In vitro enzyme assay
dezapelisib Hs Inhibition <6.3 pIC50 37
pIC50 <6.3 (IC50 >5x10-7 M) [37]
idelalisib Hs Inhibition 6.1 pIC50 36
pIC50 6.1 (IC50 8.2x10-7 M) [36]
AZD6482 Hs Inhibition 6.1 pIC50 44
pIC50 6.1 (IC50 8.7x10-7 M) [44]
eCF309 Hs Inhibition 6.0 pIC50 21
pIC50 6.0 (IC50 9.81x10-7 M) [21]
Description: In a biochemical assay.
puquitinib Hs Inhibition 6.0 pIC50 60
pIC50 6.0 (IC50 9.928x10-7 M) [60]
compound 52 [PMID: 28541707] Hs Inhibition 5.9 pIC50 39
pIC50 5.9 (IC50 1.19x10-6 M) [39]
Description: Calculated based on 700-fold lower than affinity for PI3Kδ.
TG-100-115 Hs Inhibition 5.9 pIC50 46
pIC50 5.9 (IC50 1.3x10-6 M) [46]
SAR260301 Hs Inhibition 5.8 pIC50 10
pIC50 5.8 (IC50 1.539x10-6 M) [10]
duvelisib Hs Inhibition 5.8 pIC50 57
pIC50 5.8 (IC50 1.602x10-6 M) [57]
seletalisib Hs Inhibition 5.4 pIC50 1
pIC50 5.4 (IC50 3.638x10-6 M) [1]
AZ2 Hs Inhibition 5.4 pIC50 23
pIC50 5.4 (IC50 3.981x10-6 M) [23]
PI 3-Kg inhibitor II Hs Inhibition 5.3 pIC50 7
pIC50 5.3 (IC50 4.5x10-6 M) [7]
nemiralisib Hs Inhibition 5.3 pIC50 18
pIC50 5.3 (IC50 5.011x10-6 M) [18]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
acalisib Hs Inhibition 5.3 pIC50 52
pIC50 5.3 (IC50 5.441x10-6 M) [52]
Description: In an in vitro biochemical assay using recombinant enzyme.
compound 15 [PMID: 29852070] Hs Inhibition 5.1 pIC50 47
pIC50 5.1 (IC50 7.943x10-6 M) [47]
Description: In a biochemical enzyme activity assay.
tenalisib Hs Inhibition <5.0 pIC50 55
pIC50 <5.0 (IC50 >1x10-5 M) [55]
Description: In a high throughput biochemical assay.
RV6153 Hs Inhibition <4.9 pIC50 54
pIC50 <4.9 (IC50 >1.39x10-5 M) [54]
Description: In a biochemical enzyme activity assay.
quinostatin Hs Inhibition 4.8 pIC50 61
pIC50 4.8 (IC50 1.5x10-5 M) [61]
Description: Inhibition of lipid-kinase activity in vitro.
AMG319 Hs Inhibition 4.5 pIC50 15
pIC50 4.5 (IC50 3.3x10-5 M) [15]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
PIK-108 Hs Negative <5.0 pIC50 11
pIC50 <5.0 (IC50 >1x10-5 M) [11]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 17,58

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CA
Ligand Sp. Type Action Affinity Parameter
pictilisib Hs Inhibitor Inhibition 9.0 pKd
PI-103 Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.2 pKd
PP-242 Hs Inhibitor Inhibition 6.8 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(C420R)
Ligand Sp. Type Action Affinity Parameter
PI-103 Hs Inhibitor Inhibition 8.9 pKd
pictilisib Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.0 pKd
PP-242 Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E542K)
Ligand Sp. Type Action Affinity Parameter
PI-103 Hs Inhibitor Inhibition 8.9 pKd
pictilisib Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.1 pKd
PP-242 Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E545A)
Ligand Sp. Type Action Affinity Parameter
pictilisib Hs Inhibitor Inhibition 9.1 pKd
PI-103 Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.1 pKd
PP-242 Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E545K)
Ligand Sp. Type Action Affinity Parameter
pictilisib Hs Inhibitor Inhibition 8.9 pKd
PI-103 Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Hs Inhibitor Inhibition 7.1 pKd
PP-242 Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(H1047L)
Ligand Sp. Type Action Affinity Parameter
PI-103 Hs Inhibitor Inhibition 8.5 pKd
pictilisib Hs Inhibitor Inhibition 8.4 pKd
lestaurtinib Hs Inhibitor Inhibition 7.3 pKd
TG-100-115 Hs Inhibitor Inhibition 6.5 pKd
PP-242 Hs Inhibitor Inhibition 6.4 pKd
staurosporine Hs Inhibitor Inhibition 6.4 pKd
midostaurin Hs Inhibitor Inhibition 6.0 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(H1047Y)
Ligand Sp. Type Action Affinity Parameter
PI-103 Hs Inhibitor Inhibition 8.5 pKd
pictilisib Hs Inhibitor Inhibition 8.4 pKd
TG-100-115 Hs Inhibitor Inhibition 6.8 pKd
PP-242 Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.2 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd