Page last updated: 2024-11-13

1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

The compound you described, **1-[(1R)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide**, is a complex organic molecule with a specific chemical structure.

However, without additional information, it's impossible to definitively determine its importance for research. There are several reasons why a compound like this might be of interest to researchers:

* **Potential Drug Candidate:** This molecule might exhibit interesting biological activity and could be a potential candidate for drug development. It may have the ability to interact with specific proteins or enzymes involved in disease processes, potentially leading to new treatments.
* **Chemical Probe:** The compound could be used as a tool to study the mechanisms of biological processes. For example, it might bind to a particular receptor and help scientists understand how the receptor works.
* **Synthetic Chemistry Research:** The synthesis of this complex molecule could be a challenging feat in itself, requiring specialized chemical techniques. Research on its synthesis could contribute to the development of new synthetic methods and reagents.
* **Material Science:** This compound could have unique physical properties that make it interesting for materials science research. For example, it might exhibit unusual optical properties or be useful in the development of new materials.

**To understand the importance of this specific compound, you need more context:**

* **What research area is it relevant to?** For example, is it related to cancer research, neuroscience, or antimicrobial development?
* **What are the observed effects of the compound?** Does it show any biological activity?
* **What are the researchers trying to achieve with this compound?** Is it a potential therapeutic agent, a research tool, or a building block for new materials?

Once you have more information, you can better understand why this specific compound is important for research.

(R)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1H-indole-3-carboxamide: EZH2 inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71712226
CHEBI ID131155
SCHEMBL ID19890894
SCHEMBL ID22363254
SCHEMBL ID19554395

Synonyms (26)

Synonym
CHEBI:131155
S7616
CS-3174
HY-15956A
cpi-169
SCHEMBL19890894
SCHEMBL22363254
(r)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1h-indole-3-carboxamide
AKOS025404937
1802175-07-0
J-690184
(3s)-3-[3-bromo-5-(2-methyl-2-propanyl)phenyl]-3-[(n-{3-hydroxy-5-[(5-hydroxy-1,4,5,6-tetrahydro-2-pyrimidinyl)amino]benzoyl}glycyl) amino]propanoic acid
EX-A675
cpi-169 r-enantiomer
NCGC00390589-01
SCHEMBL19554395
A900618
EX-A1684
CCG-269906
Q27224940
1-[(1r)-1-(1-ethylsulfonyl-4-piperidinyl)ethyl]-n-[(4-methoxy-6-methyl-2-oxo-1h-pyridin-3-yl)methyl]-2-methyl-3-indolecarboxamide
1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1h-indole-3-carboxamide
1-[(1r)-1-(1-ethylsulfonylpiperidin-4-yl)ethyl]-n-[(4-methoxy-6-methyl-2-oxo-1h-pyridin-3-yl)methyl]-2-methylindole-3-carboxamide
cpi 169 r-enantiomer
1-[(1r)-1-[1-(ethanesulfonyl)piperidin-4-yl]ethyl]-n-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2-methyl-1h-indole-3-carboxamide
AC-35582

Research Excerpts

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

Dosage Studied

ExcerptRelevanceReference
"080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model."( Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Albrecht, BK; Audia, JE; Balasubramanian, S; Campbell, R; Cook, AS; Cummings, RT; Dakin, LA; Duplessis, M; Gagnon, A; Gehling, VS; Good, AC; Harmange, JC; Iyer, P; Lee, C; Nasveschuk, CG; Normant, E; Trojer, P; Vaswani, RG; Zhao, F, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indolecarboxamide
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency8.48660.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[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)
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)7.30000.00022.45859.9600AID1854352
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)IC50 (µMol)0.01780.00030.50478.9000AID1240270; AID1240271; AID1240272; AID1734648; AID1734649
[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)0.08000.00500.32042.9000AID1734650
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (91)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (43)

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)
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
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)
[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)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1240280Protein binding in human plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240287Time duration showing fAUC above cellular EC50 against EZH2 in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240290Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 50 to 200 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240272Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240289Inhibition of EZH2 in human KARPAS422 cells xenografted CB17 SCID mouse assessed as reduction in H3K27me3 levels at 200 mg/kg, sc BID for 17 days measured at 1 to 12 hrs post last dose by ELISA method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240279Protein binding in dog plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240286Half life in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240274Intrinsic clearance in rat liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240288AUC in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240292Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 100 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240275Intrinsic clearance in dog liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240277Protein binding in mouse plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240282Volume of distribution at steady state in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240284AUC in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1734648Inhibition of wild-type EZH2 in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins followed by addition of [3H]-SAM measured after 2 hrs by Topcount scintillation proximity assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl
AID1240271Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240285Cmax in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240291Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 50 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240293Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 200 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240295Toxicity in human KARPAS422 cells xenografted CB17 SCID mouse assessed as body weight loss at 50 to 200 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240294Toxicity in human KARPAS422 cells xenografted CB17 SCID mouse assessed as drug tolerability at 50 to 200 mg/kg, sc BID for 28 days2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240273Intrinsic clearance in mouse liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1734649Inhibition of EZH2 Y641F mutant in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins followed by addition of [3H]-SAM measured after 2 hrs by Topcount scintillation proximity assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl
AID1240270Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240276Intrinsic clearance in human liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1240281Half life in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1734650Inhibition of EZH2 in human HeLa cells assessed as inhibition of trimethylation of H3K27 after 72 hrs by AlphaLISA assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl
AID1240283Clearance in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1854352Inhibition of SARS-CoV-2 PLpro2022European journal of medicinal chemistry, Oct-05, Volume: 240Chalcone-amide, a privileged backbone for the design and development of selective SARS-CoV/SARS-CoV-2 papain-like protease inhibitors.
AID1240278Protein binding in rat plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (37.50)24.3611
2020's5 (62.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.42

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.42 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]