| Drug General Information |
| Drug ID |
D02QWY
|
| Former ID |
DNC014870
|
| Drug Name |
BMS-754807
|
| Drug Type |
Small molecular drug
|
| Indication |
Discovery agent
|
Phase 1 |
[1],
[2]
|
|---|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C23H24FN9O
|
| InChI |
InChI=1S/C23H24FN9O/c1-23(21(34)26-15-7-8-18(24)25-13-15)9-3-10-32(23)22-28-20(17-4-2-11-33(17)31-22)27-19-12-16(29-30-19)14-5-6-14/h2,4,7-8,11-14H,3,5-6,9-10H2,1H3,(H,26,34)(H2,27,28,29,30,31)/t23-/m0/s1
|
| InChIKey |
LQVXSNNAFNGRAH-QHCPKHFHSA-N
|
| PubChem Compound ID |
|
| PubChem Substance ID |
49709980, 56185670, 85852703, 103696896, 104140677, 123055432, 131480695, 134352075, 135263891, 136340299, 136367319, 137552935, 144115734, 152088813, 152255045, 152258117, 152344407, 160646956, 162011872, 162029689, 164339435, 172918698, 174006570, 174009311, 174540010, 180413428, 184816522, 198943016, 223705200, 225359828, 227985372, 244240096, 249565635, 249815170, 250184658, 251910782, 252450308, 252470843
|
| Target and Pathway |
| Target(s) |
RAC serine/threonine-protein kinase |
Target Info |
Inhibitor |
[3]
|
|---|
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KEGG Pathway
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MAPK signaling pathway
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ErbB signaling pathway
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Ras signaling pathway
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Rap1 signaling pathway
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cGMP-PKG signaling pathway
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cAMP signaling pathway
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Chemokine signaling pathway
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HIF-1 signaling pathway
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FoxO signaling pathway
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Sphingolipid signaling pathway
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mTOR signaling pathway
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PI3K-Akt signaling pathway
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AMPK signaling pathway
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Apoptosis
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Adrenergic signaling in cardiomyocytes
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VEGF signaling pathway
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Osteoclast differentiation
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Focal adhesion
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Tight junction
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Signaling pathways regulating pluripotency of stem cells
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Platelet activation
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Toll-like receptor signaling pathway
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Jak-STAT signaling pathway
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T cell receptor signaling pathway
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B cell receptor signaling pathway
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Fc epsilon RI signaling pathway
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Fc gamma R-mediated phagocytosis
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TNF signaling pathway
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Neurotrophin signaling pathway
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Cholinergic synapse
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Dopaminergic synapse
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Insulin signaling pathway
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Progesterone-mediated oocyte maturation
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Estrogen signaling pathway
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Prolactin signaling pathway
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Thyroid hormone signaling pathway
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Adipocytokine signaling pathway
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Glucagon signaling pathway
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Regulation of lipolysis in adipocytes
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Non-alcoholic fatty liver disease (NAFLD)
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Carbohydrate digestion and absorption
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Chagas disease (American trypanosomiasis)
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Toxoplasmosis
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Tuberculosis
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Hepatitis C
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Hepatitis B
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Measles
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Influenza A
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HTLV-I infection
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Epstein-Barr virus infection
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Pathways in cancer
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Proteoglycans in cancer
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Colorectal cancer
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Renal cell carcinoma
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Pancreatic cancer
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Endometrial cancer
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Glioma
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Prostate cancer
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Melanoma
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Chronic myeloid leukemia
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Acute myeloid leukemia
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Small cell lung cancer
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Non-small cell lung cancer
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Central carbon metabolism in cancer
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Choline metabolism in cancer
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NetPath Pathway
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TSH Signaling Pathway
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PANTHER Pathway
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Angiogenesis
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Apoptosis signaling pathway
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EGF receptor signaling pathway
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Endothelin signaling pathway
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FGF signaling pathway
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Huntington disease
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Hypoxia response via HIF activation
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Inflammation mediated by chemokine and cytokine signaling pathway
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Insulin/IGF pathway-protein kinase B signaling cascade
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Interleukin signaling pathway
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PI3 kinase pathway
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T cell activation
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VEGF signaling pathway
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p53 pathway
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Ras Pathway
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p53 pathway by glucose deprivation
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p53 pathway feedback loops 2
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CCKR signaling map ST
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Pathway Interaction Database
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Regulation of nuclear SMAD2/3 signaling
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Fc-epsilon receptor I signaling in mast cells
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Endothelins
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BCR signaling pathway
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LPA receptor mediated events
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Insulin Pathway
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IL4-mediated signaling events
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TCR signaling in naï
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Plasma membrane estrogen receptor signaling
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CD40/CD40L signaling
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Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
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Signaling events mediated by PTP1B
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S1P3 pathway
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Coregulation of Androgen receptor activity
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Reelin signaling pathway
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Integrin-linked kinase signaling
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TCR signaling in naï
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Angiopoietin receptor Tie2-mediated signaling
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FAS (CD95) signaling pathway
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Thromboxane A2 receptor signaling
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Regulation of Telomerase
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FOXA2 and FOXA3 transcription factor networks
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Glucocorticoid receptor regulatory network
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mTOR signaling pathway
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CXCR4-mediated signaling events
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IGF1 pathway
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FoxO family signaling
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IL2 signaling events mediated by PI3K
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Ceramide signaling pathway
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p75(NTR)-mediated signaling
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E-cadherin signaling in the nascent adherens junction
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amb2 Integrin signaling
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Integrins in angiogenesis
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IFN-gamma pathway
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ErbB1 downstream signaling
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ErbB2/ErbB3 signaling events
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IL6-mediated signaling events
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E-cadherin signaling in keratinocytes
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Nephrin/Neph1 signaling in the kidney podocyte
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Retinoic acid receptors-mediated signaling
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IL8- and CXCR2-mediated signaling events
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Signaling events mediated by the Hedgehog family
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Nongenotropic Androgen signaling
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Hedgehog signaling events mediated by Gli proteins
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Caspase Cascade in Apoptosis
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CXCR3-mediated signaling events
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VEGFR1 specific signals
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Signaling events mediated by Stem cell factor receptor (c-Kit)
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Signaling events mediated by VEGFR1 and VEGFR2
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a6b1 and a6b4 Integrin signaling
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Aurora A signaling
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Insulin-mediated glucose transport
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Class I PI3K signaling events mediated by Akt
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IL8- and CXCR1-mediated signaling events
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HIF-1-alpha transcription factor network
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p53 pathway
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Trk receptor signaling mediated by PI3K and PLC-gamma
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VEGFR3 signaling in lymphatic endothelium
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FGF signaling pathway
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PathWhiz Pathway
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Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
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Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
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Fc Epsilon Receptor I Signaling in Mast Cells
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Insulin Signalling
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Leucine Stimulation on Insulin Signaling
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Reactome
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Activation of BAD and translocation to mitochondria
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GPVI-mediated activation cascade
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PIP3 activates AKT signaling
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Translocation of GLUT4 to the plasma membrane
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Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation
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AKT phosphorylates targets in the cytosol
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AKT phosphorylates targets in the nucleus
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Negative regulation of the PI3K/AKT network
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eNOS activation
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AKT-mediated inactivation of FOXO1A
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Integrin alphaIIb beta3 signaling
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Deactivation of the beta-catenin transactivating complex
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CD28 dependent PI3K/Akt signaling
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CTLA4 inhibitory signaling
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G beta:gamma signalling through PI3Kgamma
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KSRP (KHSRP) binds and destabilizes mRNA
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VEGFR2 mediated vascular permeability
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TP53 Regulates Metabolic Genes
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Constitutive Signaling by AKT1 E17K in Cancer
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WikiPathways
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Toll-like receptor signaling pathway
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DNA Damage Response (only ATM dependent)
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TCR Signaling Pathway
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Notch Signaling Pathway
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EPO Receptor Signaling
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IL-2 Signaling Pathway
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Insulin Signaling
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Endochondral Ossification
|
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EGF/EGFR Signaling Pathway
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IL-4 Signaling Pathway
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TGF beta Signaling Pathway
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IL-6 signaling pathway
|
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Wnt Signaling Pathway Netpath
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Copper homeostasis
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Extracellular vesicle-mediated signaling in recipient cells
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Apoptosis-related network due to altered Notch3 in ovarian cancer
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IL-3 Signaling Pathway
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Cardiac Hypertrophic Response
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Translocation of GLUT4 to the Plasma Membrane
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Regulation of mRNA Stability by Proteins that Bind AU-rich Elements
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PIP3 activates AKT signaling
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Signal Transduction of S1P Receptor
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T-Cell Receptor and Co-stimulatory Signaling
|
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Primary Focal Segmental Glomerulosclerosis FSGS
|
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Apoptosis
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Alpha 6 Beta 4 signaling pathway
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BDNF signaling pathway
|
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Integrated Pancreatic Cancer Pathway
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Oncostatin M Signaling Pathway
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Corticotropin-releasing hormone
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Interleukin-11 Signaling Pathway
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AGE/RAGE pathway
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TNF alpha Signaling Pathway
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B Cell Receptor Signaling Pathway
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Prostate Cancer
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Signaling Pathways in Glioblastoma
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TSLP Signaling Pathway
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IL17 signaling pathway
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IL-7 Signaling Pathway
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Regulation of Microtubule Cytoskeleton
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TWEAK Signaling Pathway
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FSH signaling pathway
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Leptin signaling pathway
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TSH signaling pathway
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RANKL/RANK Signaling Pathway
|
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Integrated Breast Cancer Pathway
|
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SREBP signalling
|
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Integrated Cancer pathway
|
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IL-1 signaling pathway
|
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Metabolism of nitric oxide
|
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Integrin-mediated Cell Adhesion
|
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TFs Regulate miRNAs related to cardiac hypertrophy
|
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MicroRNAs in cardiomyocyte hypertrophy
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Angiogenesis
|
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TOR Signaling
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Regulation of toll-like receptor signaling pathway
|
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AMPK Signaling
|
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Androgen receptor signaling pathway
|
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IL-5 Signaling Pathway
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| References |
| REF 1 | ClinicalTrials.gov (NCT00898716) Multiple Ascending Dose Study of BMS-754807 in Patients With Solid Tumors in Japan. U.S. National Institutes of Health. |
|---|
| REF 2 | (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: 7952). |
|---|
| REF 3 | J Med Chem. 2009 Dec 10;52(23):7360-3.Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. |
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