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

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Immunopharmacology Ligand 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

Gene and Protein Information Click here for help
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-4,5-bisphosphate 3-kinase catalytic subunit alpha
Rat - 1068 2 q25 Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha
Previous and Unofficial Names Click here for help
caPI3K | PI3K | PI3Kalpha | PtdIns-3-kinase subunit alpha | p110α/PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha | phosphatidylinositol-4
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
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:  51
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 Click here for help
EC Number: 2.7.1.153
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
neolymphostin A Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pKd 13
pKd 9.1 (Kd 8.8x10-10 M) [13]
Description: Determined using an active-site dependent competition binding assay.
bimiralisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.8 pKd
pKd 8.8 (Kd 1.5x10-9 M)
wortmannin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pKd 13
pKd 8.3 (Kd 5.4x10-9 M) [13]
IPI549 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.8 pKd 23
pKd 7.8 (Kd 1.7x10-8 M) [23]
quinostatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pKd 73
pKd 6.2 (Kd 6x10-7 M) [73]
Description: In vitro binding affinity to recombinant complex of PI3K alpha regulatory and catalytic subunits.
PQR620 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pKd 60
pKd 6.0 (Kd 1x10-6 M) [60]
compound 12b [PMID: 31465220] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pKd 6
pKd 5.8 (Kd 1.6x10-6 M) [6]
GDC-0077 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 10.5 pKi 7
pKi 10.5 (Ki 3.4x10-11 M) [7]
taselisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.5 – 10.1 pKi 7,52
pKi 10.1 (Ki 9x10-11 M) [7]
pKi 9.5 (Ki 2.9x10-10 M) [52]
PF-04691502 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.2 pKi 45
pKi 9.2 (Ki 5.7x10-10 M) [45]
compound 82 [PMID: 21332118] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pKi 20
pKi 8.9 (Ki 1.2x10-9 M) [20]
pictilisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pKi 7
pKi 8.6 (Ki 2.56x10-9 M) [7]
omipalisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.7 pKi 40
pKi 7.7 (Ki 1.9x10-8 M) [40]
wortmannin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pKi 30
pKi 6.9 (Ki 1.2x10-7 M) [30]
compound 22 [PMID: 24754609] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pKi 17
pKi 6.9 (Ki 1.32x10-7 M) [17]
PQR620 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.4 pKi 60
pKi 5.4 (Ki 4.203x10-6 M) [60]
compound 15a [PMID: 32069401] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.7 pIC50 74
pIC50 9.7 (IC50 2x10-10 M) [74]
gedatolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.4 pIC50 67
pIC50 9.4 (IC50 4x10-10 M) [67]
copanlisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 pIC50 46
pIC50 9.3 (IC50 5x10-10 M) [46]
HS-173 Small molecule or natural product Hs Inhibition 9.1 pIC50 38
pIC50 9.1 (IC50 8x10-10 M) [38]
compound 5d [PMID: 31335136] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 44
pIC50 9.1 (IC50 8.7x10-10 M) [44]
PIK-75 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 – 9.5 pIC50 33,41
pIC50 9.5 (IC50 3x10-10 M) [33]
pIC50 8.2 (IC50 5.8x10-9 M) [41]
PI-103 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 61
pIC50 8.7 (IC50 2x10-9 M) [61]
GSK1059615 Small molecule or natural product Primary target of this compound Hs Inhibition 8.7 pIC50 40
pIC50 8.7 (IC50 2x10-9 M) [40]
paxalisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 34
pIC50 8.7 (IC50 2x10-9 M) [34]
panulisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 37
pIC50 8.7 (IC50 2.2x10-9 M) [37]
Description: Using a radiometric protein kinase (33PanQinase activity) assay.
pictilisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 24
pIC50 8.5 (IC50 3x10-9 M) [24]
dactolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 48
pIC50 8.4 (IC50 4x10-9 M) [48]
BGT-226 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 49
pIC50 8.4 (IC50 4x10-9 M) [49]
KU-0060648 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 12
pIC50 8.4 (IC50 4x10-9 M) [12]
apitolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 64
pIC50 8.3 (IC50 4.8x10-9 M) [64]
alpelisib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 26
pIC50 8.3 (IC50 5x10-9 M) [26]
AZD8835 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 6.2x10-9 M) [4]
samotolisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.1x10-9 M) [3]
MEN1611 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 54
pIC50 7.8 (IC50 1.4x10-8 M) [54]
ZSTK474 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 71
pIC50 7.8 (IC50 1.6x10-8 M) [71]
VS-5584 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.8 pIC50 32
pIC50 7.8 (IC50 1.6x10-8 M) [32]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.7 pIC50 59
pIC50 7.7 (IC50 1.9x10-8 M) [59]
buparlisib Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.5 pIC50 9
pIC50 7.5 (IC50 3x10-8 M) [9]
AZD8186 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 31
pIC50 7.5 (IC50 3.5x10-8 M) [31]
pilaralisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pIC50 71
pIC50 7.4 (IC50 3.9x10-8 M) [71]
PP121 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5.2x10-8 M) [2]
AZD8154 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.3 pIC50 57
pIC50 7.3 (IC50 5.5x10-8 M) [57]
PI 3-Kg inhibitor Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 10
pIC50 7.2 (IC50 6x10-8 M) [10]
compound 11j [PMID: 23021994] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 29
pIC50 7.0 (IC50 9.2x10-8 M) [29]
serabelisib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition >7.0 pIC50 62
pIC50 >7.0 (IC50 <1x10-7 M) [62]
AZD7648 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 28
pIC50 7.0 (IC50 1x10-7 M) [28]
RV1729 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 39
pIC50 6.7 (IC50 1.93x10-7 M) [39]
Description: In a biochemical enzyme activity assay.
LY 294002 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 12,16
pIC50 6.7 (IC50 3x10-7 – 2x10-7 M) [12,16]
sapanisertib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 36
pIC50 6.7 (IC50 2.19x10-7 M) [36]
leniolisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.6 pIC50 18
pIC50 6.6 (IC50 2.62x10-7 M) [18]
Description: In vitro enzyme assay
compound 2q [PMID: 30986068] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.6 pIC50 50
pIC50 6.6 (IC50 2.7x10-7 M) [50]
Description: In a biochemical HTRF assay measuring generation of PIP3 via phosphorylation of PIP2, using PI3Kα 14-602 fragment.
dezapelisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <6.3 pIC50 43
pIC50 <6.3 (IC50 >5x10-7 M) [43]
Example 51 [WO2012135160A1] Small molecule or natural product Click here for species-specific activity table Hs Inhibition <6.3 pIC50 8
pIC50 <6.3 (IC50 >5x10-7 M) [8]
idelalisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 42
pIC50 6.1 (IC50 8.2x10-7 M) [42]
AZD6482 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 53
pIC50 6.1 (IC50 8.7x10-7 M) [53]
AS-252424 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 58
pIC50 6.0 (IC50 9.35x10-7 M) [58]
eCF309 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 25
pIC50 6.0 (IC50 9.81x10-7 M) [25]
Description: In a biochemical assay.
puquitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 72
pIC50 6.0 (IC50 9.928x10-7 M) [72]
compound 52 [PMID: 28541707] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pIC50 47
pIC50 5.9 (IC50 1.19x10-6 M) [47]
Description: Calculated based on 700-fold lower than affinity for PI3Kδ.
TG-100-115 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pIC50 55
pIC50 5.9 (IC50 1.3x10-6 M) [55]
SAR260301 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.8 pIC50 14
pIC50 5.8 (IC50 1.539x10-6 M) [14]
duvelisib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.8 pIC50 69
pIC50 5.8 (IC50 1.602x10-6 M) [69]
compound 41 [PMID: 31855425] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.8 pIC50 35
pIC50 5.8 (IC50 1.585x10-6 M) [35]
compound 7 [PMID: 31955578] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pIC50 5
pIC50 5.7 (IC50 2.2x10-6 M) [5]
seletalisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.4 pIC50 1
pIC50 5.4 (IC50 3.638x10-6 M) [1]
AZ2 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.4 pIC50 27
pIC50 5.4 (IC50 3.981x10-6 M) [27]
PI 3-Kg inhibitor II Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.3 pIC50 10
pIC50 5.3 (IC50 4.5x10-6 M) [10]
nemiralisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.3 pIC50 22
pIC50 5.3 (IC50 5.011x10-6 M) [22]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
acalisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pIC50 63
pIC50 5.3 (IC50 5.441x10-6 M) [63]
Description: In an in vitro biochemical assay using recombinant enzyme.
compound 15 [PMID: 29852070] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.1 pIC50 56
pIC50 5.1 (IC50 7.943x10-6 M) [56]
Description: In a biochemical enzyme activity assay.
tenalisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <5.0 pIC50 66
pIC50 <5.0 (IC50 >1x10-5 M) [66]
Description: In a high throughput biochemical assay.
RV6153 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <4.9 pIC50 65
pIC50 <4.9 (IC50 >1.39x10-5 M) [65]
Description: In a biochemical enzyme activity assay.
quinostatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.8 pIC50 73
pIC50 4.8 (IC50 1.5x10-5 M) [73]
Description: Inhibition of lipid-kinase activity in vitro.
AMG319 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 4.5 pIC50 19
pIC50 4.5 (IC50 3.3x10-5 M) [19]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PIK-108 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Negative <5.0 pIC50 15
pIC50 <5.0 (IC50 >1x10-5 M) [15]
DiscoveRx KINOMEscan® screen Click here for help
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: 21,70

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CA
Ligand Sp. Type Action Value Parameter
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(C420R)
Ligand Sp. Type Action Value Parameter
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E542K)
Ligand Sp. Type Action Value Parameter
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E545A)
Ligand Sp. Type Action Value Parameter
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(E545K)
Ligand Sp. Type Action Value Parameter
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Target used in screen: PIK3CA(H1047L)
Ligand Sp. Type Action Value Parameter
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.3 pKd
TG-100-115 Small molecule or natural product