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

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Target not currently curated in GtoImmuPdb

Target id: 2154

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

Abbreviated Name: PI3Kβ

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 - 1070 3q21-qter PIK3CB phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
Mouse - 1064 9 E4 Pik3cb phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
Rat - 1070 8 q31 Pik3cb phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta
Previous and Unofficial Names Click here for help
PI3Kbeta | PI3-kinase p110 subunit beta | PIK3C1 | phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | ptdIns-3-kinase p110 | p110β/PIK3CB | phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit beta | 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
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.1.153

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 8.2 pKd 11
pKd 8.2 (Kd 5.7x10-9 M) [11]
Description: Determined using an active-site dependent competition binding assay.
wortmannin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pKd 11
pKd 8.1 (Kd 7.6x10-9 M) [11]
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 8.0 pKd
pKd 8.0 (Kd 1.1x10-8 M)
IPI549 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.1 pKd 19
pKd 7.1 (Kd 8.2x10-8 M) [19]
LY 294002 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pKd 17
pKd 6.6 (Kd 2.7x10-7 M) [17]
compound 12b [PMID: 31465220] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.1 pKd 6
pKd 5.1 (Kd 7.5x10-6 M) [6]
compound 82 [PMID: 21332118] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKi 15
pKi 8.7 (Ki 2x10-9 M) [15]
taselisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 – 8.0 pKi 7,37
pKi 8.0 (Ki 9.1x10-9 M) [37]
pKi 7.3 (Ki 5.3x10-8 M) [7]
pictilisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKi 7
pKi 7.2 (Ki 7.02x10-8 M) [7]
GDC-0077 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pKi 7
pKi 7.0 (Ki 9.97x10-8 M) [7]
omipalisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pKi 29
pKi 6.9 (Ki 1.3x10-7 M) [29]
AZD8154 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pKi 42
pKi 5.9 (Ki 1.362x10-6 M) [42]
KU-0060648 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.3 pIC50 10
pIC50 9.3 (IC50 5x10-10 M) [10]
compound 15a [PMID: 32069401] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.2 pIC50 56
pIC50 9.2 (IC50 5.8x10-10 M) [56]
compound 5d [PMID: 31335136] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 33
pIC50 9.1 (IC50 7x10-10 M) [33]
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 8.5 pIC50 45
pIC50 8.5 (IC50 3x10-9 M) [45]
copanlisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 34
pIC50 8.4 (IC50 3.7x10-9 M) [34]
AZD8186 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.4 pIC50 23
pIC50 8.4 (IC50 4x10-9 M) [23]
TGX-221 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 27
pIC50 8.3 (IC50 5x10-9 M) [27]
AZD6482 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 38
pIC50 8.0 (IC50 1x10-8 M) [38]
SAR260301 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 12
pIC50 7.6 (IC50 2.3x10-8 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 7.6 pIC50 48
pIC50 7.6 (IC50 2.7x10-8 M) [48]
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 7.4 – 7.8 pIC50 53,55
pIC50 7.4 – 7.8 (IC50 4.4x10-8 – 1.7x10-8 M) [53,55]
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 7.5 pIC50 20
pIC50 7.5 (IC50 3.3x10-8 M) [20]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.3 pIC50 44
pIC50 7.3 (IC50 5.4x10-8 M) [44]
BGT-226 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pIC50 35
pIC50 7.2 (IC50 6.3x10-8 M) [35]
VS-5584 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.2 pIC50 24
pIC50 7.2 (IC50 6.8x10-8 M) [24]
samotolisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 4
pIC50 7.1 (IC50 7.8x10-8 M) [4]
compound 20f [PMID: 28520415] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.1 pIC50 43
pIC50 7.1 (IC50 7.94x10-8 M) [43]
duvelisib Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.1 pIC50 51
pIC50 7.1 (IC50 8.5x10-8 M) [51]
MEN1611 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 39
pIC50 6.9 (IC50 1.2x10-7 M) [39]
panulisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 28
pIC50 6.8 (IC50 1.76x10-7 M) [28]
Description: Using a radiometric protein kinase (33PanQinase 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 6.6 pIC50 10
pIC50 6.6 (IC50 2.7x10-7 M) [10]
PI 3-Kg inhibitor Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 9
pIC50 6.6 (IC50 2.7x10-7 M) [9]
Example 51 [WO2012135160A1] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 – 6.7 pIC50 8
pIC50 6.3 – 6.7 (IC50 5x10-7 – 2x10-7 M) [8]
Description: Binned value from patent.
pilaralisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 53
pIC50 6.4 (IC50 3.83x10-7 M) [53]
AZD8835 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 5
pIC50 6.4 (IC50 4.31x10-7 M) [5]
dezapelisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <6.3 pIC50 32
pIC50 <6.3 (IC50 >5x10-7 M) [32]
idelalisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.3 pIC50 31
pIC50 6.3 (IC50 5.65x10-7 M) [31]
puquitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 54
pIC50 6.0 (IC50 9.592x10-7 M) [54]
PIK-75 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 – 6.1 pIC50 25,30
pIC50 6.1 (IC50 8.5x10-7 M) [25]
pIC50 5.9 (IC50 1.3x10-6 M) [30]
PI-3065 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 1
pIC50 6.0 (IC50 1.078x10-6 M) [1]
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 40
pIC50 5.9 (IC50 1.2x10-6 M) [40]
alpelisib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.9 pIC50 21
pIC50 5.9 (IC50 1.2x10-6 M) [21]
PP121 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.8 pIC50 3
pIC50 5.8 (IC50 1.4x10-6 M) [3]
nemiralisib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.8 pIC50 18
pIC50 5.8 (IC50 1.584x10-6 M) [18]
Description: In a homogeneous time-resolved fluorescence (HTRF) assay
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 5.7 pIC50 26
pIC50 5.7 (IC50 1.995x10-6 M) [26]
seletalisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.7 pIC50 2
pIC50 5.7 (IC50 2.129x10-6 M) [2]
AMG319 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.6 pIC50 14
pIC50 5.6 (IC50 2.7x10-6 M) [14]
acalisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 47
pIC50 5.5 (IC50 3.377x10-6 M) [47]
Description: In an in vitro biochemical assay using recombinant enzyme.
tenalisib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <5.4 pIC50 50
pIC50 <5.4 (IC50 >4x10-6 M) [50]
Description: In a high throughput biochemical assay.
RV6153 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.3 pIC50 49
pIC50 5.3 (IC50 4.89x10-6 M) [49]
Description: In a biochemical enzyme activity 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 5.3 pIC50 36
pIC50 5.3 (IC50 5.46x10-6 M) [36]
Description: In a biochemical HTRF assay measuring generation of PIP3 via phosphorylation of PIP2, using PI3Kβ 14-603 fragment.
serabelisib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >5.0 pIC50 46
pIC50 >5.0 (IC50 <1x10-5 M) [46]
compound 15 [PMID: 29852070] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <4.5 pIC50 41
pIC50 <4.5 (IC50 >3.16x10-5 M) [41]
Description: In a biochemical enzyme activity assay.
AZ2 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 4.5 pIC50 22
pIC50 4.5 (IC50 3.162x10-5 M) [22]
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 7.6 pIC50 13
pIC50 7.6 (IC50 2.8x10-8 M) [13]
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: 16,52

Key to terms and symbols Click column headers to sort
Target used in screen: PIK3CB
Ligand Sp. Type Action Value Parameter
PI-103 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 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 6.9 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure 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
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050900 leukocyte migration TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 2 GO processes
GO:2000369 regulation of clathrin-dependent endocytosis TAS
click arrow to show/hide IEA associations
GO:0006897 endocytosis IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 4 GO processes
GO:0033031 positive regulation of neutrophil apoptotic process IMP
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050852 T cell receptor signaling pathway TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050900 leukocyte migration TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis TAS
GO:0050852 T cell receptor signaling pathway TAS

References

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2. Allen RA, Brookings DC, Powell MJ, Delgado J, Shuttleworth LK, Merriman M, Fahy IJ, Tewari R, Silva JP, Healy LJ et al.. (2017) Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3Kδ. J. Pharmacol. Exp. Ther., 361 (3): 429-440. [PMID:28442583]

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8. Brown SD, Matthews DJ. (2012) (alpha- substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5 -triazinyl benzimidazoles, pharmaceutical compositions containing them, and these compounds for use in treating proliferative diseases. Patent number: WO2012135160A1. Assignee: Pathway Therapeutics Inc.. Priority date: 28/03/2011. Publication date: 04/10/2012.

9. Camps M, Rückle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Françon B et al.. (2005) Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat. Med., 11 (9): 936-43. [PMID:16127437]

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11. Castro-Falcón G, Seiler GS, Demir Ö, Rathinaswamy MK, Hamelin D, Hoffmann RM, Makowski SL, Letzel AC, Field SJ, Burke JE et al.. (2018) Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester. J. Med. Chem., 61 (23): 10463-10472. [PMID:30380865]

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