Drug General Information |
Drug ID |
D0I6VU
|
Former ID |
DCL000109
|
Drug Name |
Enzastaurin
|
Synonyms |
LY317615; LE-0014; LY317615, Enzastaurin; 3-(1-methyl-1H-indol-3-yl)-4-{1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl}-1H-pyrrole-2,5-dione; 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
|
Drug Type |
Small molecular drug
|
Indication |
Non-hodgkin's lymphoma [ICD10:C85]
|
Phase 3 |
[1],
[2],
[3]
|
Glioblastoma multiforme [ICD9: 191; ICD10:C71]
|
Phase 2 |
[2],
[3]
|
Brain cancer; Central nervous system tumors [ICD9: 191; ICD10:C71]
|
Phase 1 |
[2],
[3]
|
Therapeutic Class |
Anticancer Agents
|
Company |
Eli Lilly
|
Structure |
|
Download
2D MOL
3D MOL
|
Formula |
C32H29N5O2
|
InChI |
InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39)
|
InChIKey |
AXRCEOKUDYDWLF-UHFFFAOYSA-N
|
CAS Number |
CAS 170364-57-5
|
PubChem Compound ID |
|
PubChem Substance ID |
10258360, 14811491, 33499842, 50653190, 57288469, 92722604, 99436960, 103240316, 104020050, 104425375, 118855345, 124756967, 125163772, 125434326, 126627253, 126666986, 131465124, 134338799, 134964387, 135237310, 135686208, 135686209, 135686224, 135686225, 136340265, 136367952, 136920322, 137248831, 137275839, 142964159, 143498272, 144115944, 144206918, 152134183, 152233034, 152258187, 152344347, 152344363, 160647023, 160814256, 162011915, 162037408, 162191234, 162801883, 163372664, 163894051, 164840960, 170465609, 172913635, 174527910
|
Target and Pathway |
Target(s) |
Protein kinase C, beta type |
Target Info |
Modulator |
[1]
|
KEGG Pathway
|
MAPK signaling pathway
|
ErbB signaling pathway
|
Ras signaling pathway
|
Rap1 signaling pathway
|
Calcium signaling pathway
|
Chemokine signaling pathway
|
NF-kappa B signaling pathway
|
HIF-1 signaling pathway
|
Phosphatidylinositol signaling system
|
Sphingolipid signaling pathway
|
mTOR signaling pathway
|
Vascular smooth muscle contraction
|
Wnt signaling pathway
|
VEGF signaling pathway
|
Focal adhesion
|
Tight junction
|
Gap junction
|
Natural killer cell mediated cytotoxicity
|
B cell receptor signaling pathway
|
Fc epsilon RI signaling pathway
|
Fc gamma R-mediated phagocytosis
|
Leukocyte transendothelial migration
|
Circadian entrainment
|
Long-term potentiation
|
Retrograde endocannabinoid signaling
|
Glutamatergic synapse
|
Cholinergic synapse
|
Serotonergic synapse
|
GABAergic synapse
|
Dopaminergic synapse
|
Long-term depression
|
Inflammatory mediator regulation of TRP channels
|
Insulin secretion
|
GnRH signaling pathway
|
Melanogenesis
|
Thyroid hormone synthesis
|
Thyroid hormone signaling pathway
|
Oxytocin signaling pathway
|
Aldosterone-regulated sodium reabsorption
|
Endocrine and other factor-regulated calcium reabsorption
|
Salivary secretion
|
Gastric acid secretion
|
Pancreatic secretion
|
Carbohydrate digestion and absorption
|
Amphetamine addiction
|
Morphine addiction
|
Vibrio cholerae infection
|
Leishmaniasis
|
African trypanosomiasis
|
Amoebiasis
|
Hepatitis B
|
Influenza A
|
Pathways in cancer
|
Proteoglycans in cancer
|
MicroRNAs in cancer
|
Glioma
|
Non-small cell lung cancer
|
Choline metabolism in cancer
|
NetPath Pathway
|
IL2 Signaling Pathway
|
PANTHER Pathway
|
Alzheimer disease-amyloid secretase pathway
|
Angiogenesis
|
Apoptosis signaling pathway
|
B cell activation
|
EGF receptor signaling pathway
|
Endothelin signaling pathway
|
FGF signaling pathway
|
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
|
Inflammation mediated by chemokine and cytokine signaling pathway
|
Metabotropic glutamate receptor group I pathway
|
Muscarinic acetylcholine receptor 1 and 3 signaling pathway
|
VEGF signaling pathway
|
Wnt signaling pathway
|
5HT2 type receptor mediated signaling pathway
|
Histamine H1 receptor mediated signaling pathway
|
Oxytocin receptor mediated signaling pathway
|
Thyrotropin-releasing hormone receptor signaling pathway
|
CCKR signaling map ST
|
Pathway Interaction Database
|
Fc-epsilon receptor I signaling in mast cells
|
TCR signaling in naï
|
TCR signaling in naï
|
IL2-mediated signaling events
|
Ras signaling in the CD4+ TCR pathway
|
JNK signaling in the CD4+ TCR pathway
|
Regulation of Ras family activation
|
Downstream signaling in naï
|
Reactome
|
Disinhibition of SNARE formation
|
Activation of NF-kappaB in B cells
|
Trafficking of GluR2-containing AMPA receptors
|
G alpha (z) signalling events
|
Depolymerisation of the Nuclear Lamina
|
WNT5A-dependent internalization of FZD4
|
VEGFR2 mediated cell proliferation
|
Response to elevated platelet cytosolic Ca2+
|
WikiPathways
|
Calcium Regulation in the Cardiac Cell
|
Insulin Signaling
|
EGF/EGFR Signaling Pathway
|
Wnt Signaling Pathway
|
Wnt Signaling Pathway and Pluripotency
|
MAPK Signaling Pathway
|
Wnt Signaling Pathway Netpath
|
G Protein Signaling Pathways
|
Kit receptor signaling pathway
|
Myometrial Relaxation and Contraction Pathways
|
Signaling by the B Cell Receptor (BCR)
|
Oncostatin M Signaling Pathway
|
Corticotropin-releasing hormone
|
AGE/RAGE pathway
|
B Cell Receptor Signaling Pathway
|
Signaling Pathways in Glioblastoma
|
miRs in Muscle Cell Differentiation
|
Response to elevated platelet cytosolic Ca2+
|
MicroRNAs in cardiomyocyte hypertrophy
|
Physiological and Pathological Hypertrophy of the Heart
|
References |
REF 1 | The oral protein-kinase C beta inhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines. Leuk Lymphoma. 2008 Jul;49(7):1374-83. |
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REF 2 | Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. |
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REF 3 | (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: 5693). |