Compounds > epz005687
Page last updated: 2024-11-13

epz005687

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Description

EPZ005687: inhibits EZH2 protein; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60160561
CHEBI ID124922
SCHEMBL ID12684069
MeSH IDM0581302

Synonyms (39)

Synonym
CHEBI:124922
epz005687
HY-15555
CS-1215
S7004
1396772-26-1
ZOIBZSZLMJDVDQ-UHFFFAOYSA-N ,
cyclopentyl-n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1h-indazole-4-carboxamide
1-cyclopentyl-n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1h-indazole-4-carboxamide
1-cyclopentyl-n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
SCHEMBL12684069
epz-005687
gtpl8387
epz 005687
AC-32708
ezh2 inhibitor, epz005687
AKOS026750254
1-cyclopentyl-n-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-6-{4-[(morpholin-4-yl)methyl]phenyl}-1h-indazole-4-carboxamide
DTXSID80733849
EX-A429
mfcd25372029
NCGC00351604-09
NCGC00351604-12
epz 5687 [who-dd]
GQ4LD5KG1E ,
1h-indazole-4-carboxamide, 1-cyclopentyl-n-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-6-(4-(4-morpholinylmethyl)phenyl)-
epz-5687
epz 5687
FT-0700189
BCP07899
NCGC00351604-01
Q27077206
AS-16367
SB19050
unii-gq4ld5kg1e
CCG-269957
nsc783332
nsc-783332
WFC77226

Research Excerpts

Overview

EPZ005687 is a selective inhibiter of methyltransferase EZH2.

ExcerptReferenceRelevance
"EPZ005687 is a selective inhibiter of methyltransferase EZH2. "( EZH2 Inhibition Ameliorates Transverse Aortic Constriction-Induced Pulmonary Arterial Hypertension in Mice.
Fang, K; Li, ZH; Ren, DH; Shi, ZL; Sun, J; Zhang, JY, 2018)		1.92

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency46.61280.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency2.39190.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency35.55760.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)IC50 (µMol)8.17090.00030.50478.9000AID1199066; AID1199089; AID1729410; AID1854177; AID1868615; AID1868617; AID1882367
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)Ki0.02400.00050.03170.1940AID1199065; AID1729405
Histone-lysine N-methyltransferase EZH1Homo sapiens (human)IC50 (µMol)0.04500.00402.61658.7700AID1729409
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)EC50 (µMol)2.90000.00500.32042.9000AID1281011
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (93)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G1/S transition of mitotic cell cycleHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromatin organizationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of cell population proliferationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
regulation of gliogenesisHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
skeletal muscle satellite cell maintenance involved in skeletal muscle regenerationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
cerebellar cortex developmentHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
hippocampus developmentHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
B cell differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
keratinocyte differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of cell migrationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
regulatory ncRNA-mediated heterochromatin formationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
subtelomeric heterochromatin formationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
methylationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
response to estradiolHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of transcription elongation by RNA polymerase IIHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
cellular response to trichostatin AHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
protein modification processHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
hepatocyte homeostasisHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
regulation of circadian rhythmHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of MAP kinase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of GTPase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of keratinocyte differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of retinoic acid receptor signaling pathwayHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
rhythmic processHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
stem cell differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of striated muscle cell differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
synaptic transmission, GABAergicHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
cellular response to hydrogen peroxideHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
G1 to G0 transitionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
protein localization to chromatinHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of protein serine/threonine kinase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
regulation of kidney developmentHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
liver regenerationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
facultative heterochromatin formationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of dendrite developmentHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of cytokine production involved in inflammatory responseHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
positive regulation of cell cycle G1/S phase transitionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
response to tetrachloromethaneHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
negative regulation of stem cell differentiationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
heterochromatin formationHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
chromatin remodelingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
anatomical structure morphogenesisHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
hippocampus developmentHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
heterochromatin formationHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
subtelomeric heterochromatin formationHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
methylationHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromatin bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
transcription corepressor activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromatin DNA bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
histone methyltransferase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
ribonucleoprotein complex bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
primary miRNA bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
lncRNA bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
histone H3 methyltransferase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
histone H3K27 trimethyltransferase activityHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
promoter-specific chromatin bindingHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
DNA bindingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
histone bindingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
transcription corepressor activityHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
nucleosome bindingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
molecular condensate scaffold activityHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
histone H3K27 trimethyltransferase activityHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
chromatin bindingHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
chromosomeHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromosome, telomeric regionHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
pronucleusHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
synapseHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
chromatin silencing complexHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
pericentric heterochromatinHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
ESC/E(Z) complexHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EZH2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
chromosome, telomeric regionHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
heterochromatinHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
ESC/E(Z) complexHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EZH1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (48)

Assay IDTitleYearJournalArticle
AID1199089Inhibition of wild-type EZH2 in human OCI-LY19 cells assessed as reduction of H3K27me3 level after 96 hrs by ELISA assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199076Selectivity for human EZH2 over human SMYD22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1170578Reduction in EZH2 protein expression in human Toledo cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1199064Selectivity for human EZH2 over human G9a2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1854176Binding affinity to PRC2 (unknown origin) assessed as inhibition constant2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1868615Inhibition of EZH2 (unknown origin)2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1170581Reduction in EZH2 protein expression in human DB cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1868616Inhibition of PRC2 (unknown origin) assessed as inhibition constant2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1199083Selectivity for human EZH2 over human PRMT52015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199066Inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measured after 90 mins by flash plate assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1854177Inhibition of EZH2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1868617Inhibition of EZH2 in human OCILY19 cells assessed as reduction in H3K27me3 level treated for 96 hrs by Western blot analysis2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
AID1170579Reduction in SUZ12 protein expression in human Toledo cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1281012Clearance in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1281011Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1199088Selectivity for human EZH2 over human EZH2 A677G mutant2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1729410Inhibition of EZH2 in human PRC2 complex preincubated for 30 mins followed by histone h3 peptide (21 to 44 residues) and S-adenosylmethionine and measured after 90 mins2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
AID1199079Selectivity for human EZH2 over human MMSET2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199065Competitive inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measured after 90 mins by Michaelis-Menten plot analysis2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199077Selectivity for human EZH2 over human SMYD32015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199080Selectivity for human EZH2 over human PRMT12015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199084Selectivity for human EZH2 over human PRMT62015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1281014Volume of distribution at steady state in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1199075Selectivity for human EZH2 over human SETD72015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199078Selectivity for human EZH2 over human WHSC1L12015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199081Selectivity for human EZH2 over human PRMT32015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199082Selectivity for human EZH2 over human PRMT42015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1729423Plasma concentration in SCID mouse xenografted with human G-401 cells at 125 mg/kg, po BID administered for 21 days and measured at 3 hrs post dose on day 21 by LC-MS/MS analysis2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
AID1199086Selectivity for human EZH2 over human DOT1L2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199087Selectivity for human EZH2 over human EZH12015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1170577Reduction in EED protein expression in human Toledo cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1729409Inhibition of EZH1 in PRC2 complex (unknown origin) using biotinylated peptide as substrate in presence of S-adenosylmethionine2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
AID1281013AUC in mouse at 2 mg/kg, iv and 10 mg/kg, po by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1170580Reduction in EED protein expression in human DB cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1199063Selectivity for human EZH2 over human GLP2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1170582Reduction in SUZ12 protein expression in human DB cells at 10 uM after 72 hrs by Western blot analysis2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
AID1281015Oral bioavailability in mouse at 10 mg/kg by LC-MS/MS analysis2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
AID1729405Competitive inhibition of wild type EZH2 in human PRC2 complex using S-adenosylmethionine as substrate by Michaelis-Menten plot analysis2020Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.
AID1882367Inhibition of EZH2 (unknown origin)2022Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.
AID1199085Selectivity for human EZH2 over human PRMT82015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1854178Selectivity ratio of IC50 for EZH2 (unknown origin) to IC50 for EZH1 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346024Human enhancer of zeste 2 polycomb repressive complex 2 subunit (2.1.1.43 Histone methyltransferases (HMTs))2012Nature chemical biology, Nov, Volume: 8, Issue:11
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (63.16)24.3611
2020's7 (36.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.77

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index27.77 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index20.59 (26.88)
Search Engine Supply Index1.50 (0.95)

This Compound (27.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (21.05%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (78.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.110benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.4110aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
lysine
Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine.		2.5220aspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid		algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		4.7380indazole
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		2.1310adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
hexamidine
hexamidine : A polyether that is the bis(4-guanidinophenyl) ether of hexane-1,6-diol.		2.4110aromatic ether;
guanidines;
polyether		antimicrobial agent;
antiseptic drug
3-deazaneplanocin
3-deazaneplanocin: S-adenosylhomocysteine hydrolase antagonist		3.7120
przewaquinone d
przewaquinone D: isolated from root of Salvia przewalskii; structure given in first source; RN given refers to the trans- isomer, przewaquinone D		2.4110
nsc 663284
NSC 663284: structure in first source		2.1110quinolone
wedelolactone
wedelolactone: antihepatotoxic coumestan from Eclipta prostrata and Wedelia calendulacea (both Asteraceae); structure given in first source. wedelolactone : A member of the class of coumestans that is coumestan with hydroxy substituents as positions 1, 8 and 9 and a methoxy substituent at position 3.		4.3320aromatic ether;
coumestans;
delta-lactone;
polyphenol		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
hepatoprotective agent;
metabolite
ellagic acid
[no description available]		2.1110catechols;
cyclic ketone;
lactone;
organic heterotetracyclic compound;
polyphenol		antioxidant;
EC 1.14.18.1 (tyrosinase) inhibitor;
EC 2.3.1.5 (arylamine N-acetyltransferase) inhibitor;
EC 2.4.1.1 (glycogen phosphorylase) inhibitor;
EC 2.5.1.18 (glutathione transferase) inhibitor;
EC 2.7.1.127 (inositol-trisphosphate 3-kinase) inhibitor;
EC 2.7.1.151 (inositol-polyphosphate multikinase) inhibitor;
EC 2.7.4.6 (nucleoside-diphosphate kinase) inhibitor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
food additive;
fungal metabolite;
geroprotector;
plant metabolite;
skin lightening agent
bvt.948
[no description available]		2.1110
olaparib
[no description available]		3.5110cyclopropanes;
monofluorobenzenes;
N-acylpiperazine;
phthalazines		antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
az 505
AZ 505: an SMYD2 inhibitor; structure in first source		2.1110
bix 01294
[no description available]		3.6920piperidines
epz004777
[no description available]		2.1110N-glycosyl compound
epz-5676
[no description available]		2.11105'-deoxyribonucleoside
epz-6438
tazemetostat: a histone methyltransferase EZH2 inhibitor with antineoplastic activity		5.7670
gsk-2816126
GSK-2816126: inhibits EZH2 methyltransferase; structure in first source		5.3960piperazines;
pyridines
gsk343
GSK343: an EZH2 methyltransferase inhibitor. GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM).		4.1740aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor
(r)-pfi-2
(R)-PFI-2: a potent and selective inhibitor of SETD7 methyltransferase; structure in first source		2.1110
lly-507
LLY-507: inhibits methyltransferase SMYD2; structure in first source. LLY-507 : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl}[biphenyl]-3-carboxylic acid with the amino group of 3-(pyrrolidin-1-yl)propan-1-amine. It is a potent and selective inhibitor of SMYD2 and inhibits the ability of SMYD2 to methylate p53. It serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.		2.1110
ConditionIndicatedRelationship StrengthStudiesTrials
Germinoblastoma
[description not available]		02.4920
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		02.4920
Disease Exacerbation
[description not available]		02.110
Benign Neoplasms
[description not available]		05.2450
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		05.2450
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.6120
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Hematologic Malignancies
[description not available]		03.3310
Hematologic Neoplasms
Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES.		03.3310
Hypertrophy, Right Ventricular
Enlargement of the RIGHT VENTRICLE of the heart. This increase in ventricular mass is often attributed to PULMONARY HYPERTENSION and is a contributor to cardiovascular morbidity and mortality.		02.1710
Pulmonary Hypertension
[description not available]		02.1710
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		02.1710
Arthritis, Degenerative
[description not available]		02.1310
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		02.1310
HPV Infection
[description not available]		02.1310
Carcinoma, Epidermoid
[description not available]		02.1310
Cancer of Oropharnyx
[description not available]		02.1310
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		02.1310
Oropharyngeal Neoplasms
Tumors or cancer of the OROPHARYNX.		02.1310
Papillomavirus Infections
Neoplasms of the skin and mucous membranes caused by papillomaviruses. They are usually benign but some have a high risk for malignant progression.		02.1310