| Drug General Information |
| Drug ID |
D0I4TH
|
| Former ID |
DCL001186
|
| Drug Name |
GDC-0068
|
| Synonyms |
AKT inhibitors
|
| Drug Type |
Small molecular drug
|
| Indication |
Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48]
|
Phase 1 |
[1],
[2]
|
|---|
| Company |
Genentech
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C24H32ClN5O2
|
| InChI |
InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
|
| InChIKey |
GRZXWCHAXNAUHY-NSISKUIASA-N
|
| PubChem Compound ID |
|
| PubChem Substance ID |
49713295, 56186387, 135685879, 136946576, 141467339, 144116003, 152159628, 162011956, 163321308, 163347403, 163620831, 163686159, 164193920, 172659610, 174006468, 184825151, 198969746, 223388911, 224165330, 226550983, 242585120, 247188039, 249565578, 252451740, 252553164
|
| Target and Pathway |
| Target(s) |
RAC serine/threonine-protein kinase |
Target Info |
Inhibitor |
[2]
|
|---|
|
KEGG Pathway
|
MAPK signaling pathway
|
|
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
|
|
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
|
|
Tight junction
|
|
Signaling pathways regulating pluripotency of stem cells
|
|
Platelet activation
|
|
Toll-like receptor signaling pathway
|
|
Jak-STAT signaling pathway
|
|
T cell receptor signaling pathway
|
|
B cell receptor signaling pathway
|
|
Fc epsilon RI signaling pathway
|
|
Fc gamma R-mediated phagocytosis
|
|
TNF signaling pathway
|
|
Neurotrophin signaling pathway
|
|
Cholinergic synapse
|
|
Dopaminergic synapse
|
|
Insulin signaling pathway
|
|
Progesterone-mediated oocyte maturation
|
|
Estrogen signaling pathway
|
|
Prolactin signaling pathway
|
|
Thyroid hormone signaling pathway
|
|
Adipocytokine signaling pathway
|
|
Glucagon signaling pathway
|
|
Regulation of lipolysis in adipocytes
|
|
Non-alcoholic fatty liver disease (NAFLD)
|
|
Carbohydrate digestion and absorption
|
|
Chagas disease (American trypanosomiasis)
|
|
Toxoplasmosis
|
|
Tuberculosis
|
|
Hepatitis C
|
|
Hepatitis B
|
|
Measles
|
|
Influenza A
|
|
HTLV-I infection
|
|
Epstein-Barr virus infection
|
|
Pathways in cancer
|
|
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
|
|
NetPath Pathway
|
TSH Signaling Pathway
|
|
PANTHER Pathway
|
Angiogenesis
|
|
Apoptosis signaling pathway
|
|
EGF receptor signaling pathway
|
|
Endothelin signaling pathway
|
|
FGF signaling pathway
|
|
Huntington disease
|
|
Hypoxia response via HIF activation
|
|
Inflammation mediated by chemokine and cytokine signaling pathway
|
|
Insulin/IGF pathway-protein kinase B signaling cascade
|
|
Interleukin signaling pathway
|
|
PI3 kinase pathway
|
|
T cell activation
|
|
VEGF signaling pathway
|
|
p53 pathway
|
|
Ras Pathway
|
|
p53 pathway by glucose deprivation
|
|
p53 pathway feedback loops 2
|
|
CCKR signaling map ST
|
|
Pathway Interaction Database
|
Regulation of nuclear SMAD2/3 signaling
|
|
Fc-epsilon receptor I signaling in mast cells
|
|
Endothelins
|
|
BCR signaling pathway
|
|
LPA receptor mediated events
|
|
Insulin Pathway
|
|
IL4-mediated signaling events
|
|
TCR signaling in naï
|
|
Plasma membrane estrogen receptor signaling
|
|
CD40/CD40L signaling
|
|
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
|
|
Signaling events mediated by PTP1B
|
|
S1P3 pathway
|
|
Coregulation of Androgen receptor activity
|
|
Reelin signaling pathway
|
|
Integrin-linked kinase signaling
|
|
TCR signaling in naï
|
|
Angiopoietin receptor Tie2-mediated signaling
|
|
FAS (CD95) signaling pathway
|
|
Thromboxane A2 receptor signaling
|
|
Regulation of Telomerase
|
|
FOXA2 and FOXA3 transcription factor networks
|
|
Glucocorticoid receptor regulatory network
|
|
mTOR signaling pathway
|
|
CXCR4-mediated signaling events
|
|
IGF1 pathway
|
|
FoxO family signaling
|
|
IL2 signaling events mediated by PI3K
|
|
Ceramide signaling pathway
|
|
p75(NTR)-mediated signaling
|
|
E-cadherin signaling in the nascent adherens junction
|
|
amb2 Integrin signaling
|
|
Integrins in angiogenesis
|
|
IFN-gamma pathway
|
|
ErbB1 downstream signaling
|
|
ErbB2/ErbB3 signaling events
|
|
IL6-mediated signaling events
|
|
E-cadherin signaling in keratinocytes
|
|
Nephrin/Neph1 signaling in the kidney podocyte
|
|
Retinoic acid receptors-mediated signaling
|
|
IL8- and CXCR2-mediated signaling events
|
|
Signaling events mediated by the Hedgehog family
|
|
Nongenotropic Androgen signaling
|
|
Hedgehog signaling events mediated by Gli proteins
|
|
Caspase Cascade in Apoptosis
|
|
CXCR3-mediated signaling events
|
|
VEGFR1 specific signals
|
|
Signaling events mediated by Stem cell factor receptor (c-Kit)
|
|
Signaling events mediated by VEGFR1 and VEGFR2
|
|
a6b1 and a6b4 Integrin signaling
|
|
Aurora A signaling
|
|
Insulin-mediated glucose transport
|
|
Class I PI3K signaling events mediated by Akt
|
|
IL8- and CXCR1-mediated signaling events
|
|
HIF-1-alpha transcription factor network
|
|
p53 pathway
|
|
Trk receptor signaling mediated by PI3K and PLC-gamma
|
|
VEGFR3 signaling in lymphatic endothelium
|
|
FGF signaling pathway
|
|
PathWhiz Pathway
|
Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
|
|
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
|
|
Fc Epsilon Receptor I Signaling in Mast Cells
|
|
Insulin Signalling
|
|
Leucine Stimulation on Insulin Signaling
|
|
Reactome
|
Activation of BAD and translocation to mitochondria
|
|
GPVI-mediated activation cascade
|
|
PIP3 activates AKT signaling
|
|
Translocation of GLUT4 to the plasma membrane
|
|
Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation
|
|
AKT phosphorylates targets in the cytosol
|
|
AKT phosphorylates targets in the nucleus
|
|
Negative regulation of the PI3K/AKT network
|
|
eNOS activation
|
|
AKT-mediated inactivation of FOXO1A
|
|
Integrin alphaIIb beta3 signaling
|
|
Deactivation of the beta-catenin transactivating complex
|
|
CD28 dependent PI3K/Akt signaling
|
|
CTLA4 inhibitory signaling
|
|
G beta:gamma signalling through PI3Kgamma
|
|
KSRP (KHSRP) binds and destabilizes mRNA
|
|
VEGFR2 mediated vascular permeability
|
|
TP53 Regulates Metabolic Genes
|
|
Constitutive Signaling by AKT1 E17K in Cancer
|
|
WikiPathways
|
Toll-like receptor signaling pathway
|
|
DNA Damage Response (only ATM dependent)
|
|
TCR Signaling Pathway
|
|
Notch Signaling Pathway
|
|
EPO Receptor Signaling
|
|
IL-2 Signaling Pathway
|
|
Insulin Signaling
|
|
Endochondral Ossification
|
|
EGF/EGFR Signaling Pathway
|
|
IL-4 Signaling Pathway
|
|
TGF beta Signaling Pathway
|
|
IL-6 signaling pathway
|
|
Wnt Signaling Pathway Netpath
|
|
Copper homeostasis
|
|
Extracellular vesicle-mediated signaling in recipient cells
|
|
Apoptosis-related network due to altered Notch3 in ovarian cancer
|
|
IL-3 Signaling Pathway
|
|
Cardiac Hypertrophic Response
|
|
Translocation of GLUT4 to the Plasma Membrane
|
|
Regulation of mRNA Stability by Proteins that Bind AU-rich Elements
|
|
PIP3 activates AKT signaling
|
|
Signal Transduction of S1P Receptor
|
|
T-Cell Receptor and Co-stimulatory Signaling
|
|
Primary Focal Segmental Glomerulosclerosis FSGS
|
|
Apoptosis
|
|
Alpha 6 Beta 4 signaling pathway
|
|
BDNF signaling pathway
|
|
Integrated Pancreatic Cancer Pathway
|
|
Oncostatin M Signaling Pathway
|
|
Corticotropin-releasing hormone
|
|
Interleukin-11 Signaling Pathway
|
|
AGE/RAGE pathway
|
|
TNF alpha Signaling Pathway
|
|
B Cell Receptor Signaling Pathway
|
|
Prostate Cancer
|
|
Signaling Pathways in Glioblastoma
|
|
TSLP Signaling Pathway
|
|
IL17 signaling pathway
|
|
IL-7 Signaling Pathway
|
|
Regulation of Microtubule Cytoskeleton
|
|
TWEAK Signaling Pathway
|
|
FSH signaling pathway
|
|
Leptin signaling pathway
|
|
TSH signaling pathway
|
|
RANKL/RANK Signaling Pathway
|
|
Integrated Breast Cancer Pathway
|
|
SREBP signalling
|
|
Integrated Cancer pathway
|
|
IL-1 signaling pathway
|
|
Metabolism of nitric oxide
|
|
Integrin-mediated Cell Adhesion
|
|
TFs Regulate miRNAs related to cardiac hypertrophy
|
|
MicroRNAs in cardiomyocyte hypertrophy
|
|
Angiogenesis
|
|
TOR Signaling
|
|
Regulation of toll-like receptor signaling pathway
|
|
AMPK Signaling
|
|
Androgen receptor signaling pathway
|
|
IL-5 Signaling Pathway
|
| References |
| REF 1 | (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: 7887). |
|---|
| REF 2 | Clinical pipeline report, company report or official report of Genentech (2011). |
|---|
