Drug Information

Drug General Information
Drug ID
D0G3MN
Former ID
DNCL002436
Drug Name
GSK2636771
Drug Type
Small molecular drug
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Phase 1 [523668], [542883]
Company
GlaxoSmithKline
Structure
Download
2D MOL

3D MOL
Formula
C22H22F3N3O3
InChI
InChI=1S/C22H22F3N3O3/c1-13-15(4-3-5-18(13)22(23,24)25)12-28-14(2)26-20-17(21(29)30)10-16(11-19(20)28)27-6-8-31-9-7-27/h3-5,10-11H,6-9,12H2,1-2H3,(H,29,30)
InChIKey
XTKLTGBKIDQGQL-UHFFFAOYSA-N
PubChem Compound ID
56949517
PubChem Substance ID
135656208, 144116031, 152258656, 160647492, 161005251, 162011756, 162109068, 164045113, 174006492, 185970629, 198947436, 208265522, 223705202, 224580193, 225848211, 227506784, 242591564, 249565650, 251963087, 252215511, 252237587, 252451673, 252471900
Target and Pathway
Target(s) PI3K beta Target Info Inhibitor [542883]
BioCyc Pathway Superpathway of inositol phosphate compounds
3-phosphoinositide biosynthesis
KEGG Pathway Inositol phosphate metabolism
ErbB signaling pathway
Ras signaling pathway
Rap1 signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
HIF-1 signaling pathway
FoxO signaling pathway
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK signaling pathway
Apoptosis
Adrenergic signaling in cardiomyocytes
VEGF signaling pathway
Osteoclast differentiation
Focal adhesion
Signaling pathways regulating pluripotency of stem cells
Platelet activation
Toll-like receptor signaling pathway
Jak-STAT signaling pathway
Natural killer cell mediated cytotoxicity
T cell receptor signaling pathway
B cell receptor signaling pathway
Fc epsilon RI signaling pathway
Fc gamma R-mediated phagocytosis
TNF signaling pathway
Leukocyte transendothelial migration
Neurotrophin signaling pathway
Cholinergic synapse
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Regulation of lipolysis in adipocytes
Type II diabetes mellitus
Non-alcoholic fatty liver disease (NAFLD)
Aldosterone-regulated sodium reabsorption
Carbohydrate digestion and absorption
Bacterial invasion of epithelial cells
Chagas disease (American trypanosomiasis)
Toxoplasmosis
Amoebiasis
Hepatitis C
Hepatitis B
Measles
Influenza A
HTLV-I infection
Epstein-Barr virus infection
Pathways in cancer
Viral carcinogenesis
Proteoglycans in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Melanoma
Chronic myeloid leukemia
Acute myeloid leukemia
Small cell lung cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
Choline metabolism in cancer
PANTHER Pathway Angiogenesis
Apoptosis signaling pathway
Axon guidance mediated by netrin
B cell activation
EGF receptor signaling pathway
Endothelin signaling pathway
FGF signaling pathway
Hypoxia response via HIF activation
Inflammation mediated by chemokine and cytokine signaling pathway
Insulin/IGF pathway-protein kinase B signaling cascade
Integrin signalling pathway
Interleukin signaling pathway
PDGF signaling pathway
PI3 kinase pathway
T cell activation
VEGF signaling pathway
p53 pathway
Ras Pathway
p53 pathway feedback loops 2
CCKR signaling map ST
Pathway Interaction Database ErbB4 signaling events
LPA receptor mediated events
TRAIL signaling pathway
Signaling events mediated by TCPTP
FAS (CD95) signaling pathway
CXCR4-mediated signaling events
EGF receptor (ErbB1) signaling pathway
Class I PI3K signaling events
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
PDGFR-beta signaling pathway
Nephrin/Neph1 signaling in the kidney podocyte
Internalization of ErbB1
CXCR3-mediated signaling events
Reactome PI3K Cascade
GPVI-mediated activation cascade
PIP3 activates AKT signaling
PI3K/AKT activation
Role of phospholipids in phagocytosis
Tie2 Signaling
Constitutive Signaling by Aberrant PI3K in Cancer
DAP12 signaling
Role of LAT2/NTAL/LAB on calcium mobilization
Nephrin interactions
G beta:gamma signalling through PI3Kgamma
VEGFA-VEGFR2 Pathway
Interleukin-3, 5 and GM-CSF signaling
Interleukin receptor SHC signaling
Regulation of signaling by CBL
WikiPathways Toll-like receptor signaling pathway
DNA Damage Response (only ATM dependent)
G13 Signaling Pathway
Regulation of Actin Cytoskeleton
Insulin Signaling
Fc epsilon receptor (FCERI) signaling
PI Metabolism
Interleukin-2 signaling
Fcgamma receptor (FCGR) dependent phagocytosis
DAP12 interactions
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
PIP3 activates AKT signaling
Signaling Pathways in Glioblastoma
TCR signaling
Signaling by PDGF
Signaling by Insulin receptor
NGF signalling via TRKA from the plasma membrane
Nephrin interactions
Interleukin-3, 5 and GM-CSF signaling
GPVI-mediated activation cascade
Cell surface interactions at the vascular wall
MicroRNAs in cardiomyocyte hypertrophy
Regulation of toll-like receptor signaling pathway
AMPK Signaling
References
Ref 523668ClinicalTrials.gov (NCT01458067) A Phase I/IIa, First Time in Human, Study of GSK2636771 in Subjects With Advanced Solid Tumors With Phosphatase and Tensin Homolog (PTEN) Deficiency. U.S. National Institutes of Health.
Ref 542883(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7967).
Ref 542883(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7967).

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