Drug Information

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 [529450], [537114], [541035]
Glioblastoma multiforme [ICD9: 191; ICD10:C71] Phase 2 [537114], [541035]
Brain cancer; Central nervous system tumors [ICD9: 191; ICD10:C71] Phase 1 [537114], [541035]
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
176167
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 [529450]
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 na&#xef
TCR signaling in na&#xef
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 na&#xef
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 529450The 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.
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 541035(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).
Ref 529450The 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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