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gsk-2816126

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Description

GSK-2816126: inhibits EZH2 methyltransferase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68210102
CHEMBL ID3287735
CHEBI ID124921
SCHEMBL ID12180401
MeSH IDM0580964

Synonyms (45)

Synonym
CHEBI:124921
FKSFKBQGSFSOSM-QFIPXVFZSA-N ,
n-[(4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-[(1s)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1h-indole-4-carboxamide
bdbm50017293
chembl3287735 ,
SCHEMBL12180401
gsk126
CS-1401
NCGC00347286-01
S7061
1-[(2s)-butan-2-yl]-n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
gtpl7012
gsk 126
gsk2816126
gsk-126
HY-13470
smr004701327
MLS006010251
1346574-57-9
ezh2 inhibitor
(s)-1-(sec-butyl)-n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1h-indole-4-carboxamide
1h-indole-4-carboxamide, n-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-3-methyl-1-((1s)-1-methylpropyl)-6-(6-(1-piperazinyl)-3-pyridinyl)-
gsk-2816126
(s)-1-sec-butyl-n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1h-indole-4-carboxamide
n-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-3-methyl-1-((1s)-1-methylpropyl)-6-(6-(1-piperazinyl)-3-pyridinyl)-1h-indole-4-carboxamide
W4OGW9QZ97 ,
gsk 2816126 [who-dd]
gsk-2816126a
EX-A499
AKOS027322309
unii-w4ogw9qz97
BCP06129
Q27077865
AS-16379
1-[(2s)-butan-2-yl]-n-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1h-indole-4-carboxamide
a9g ,
n-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1s)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1h-indole-4-carboxamide
CCG-269895
nsc780041
nsc-789702
gsk126 hcl
nsc789702
gsk-126 hcl
nsc-780041
DTXSID301025739

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
"The MTD of GSK2816126 was established at 2,400 mg, but the dosing method and relatively short half-life limited effective exposure, and modest anticancer activity was observed at tolerable doses."( Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors.
Carver, J; Creasy, CL; Dhar, A; Frey, S; Giulino-Roth, L; Horner, T; Johnson, PWM; Khaled, A; Leonard, JP; Longley, J; Lopez, J; McCabe, MT; Michot, JM; Oh, C; Pene Dumitrescu, T; Ribrag, V; Stern, M; Wang, X; Winter, JN; Yap, TA, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
piperazines
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency20.86900.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
[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)
Polycomb protein EEDHomo sapiens (human)IC50 (µMol)0.01600.00201.21958.9000AID1151968
Polycomb protein SUZ12Homo sapiens (human)IC50 (µMol)0.01600.00401.61908.9000AID1151968
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)IC50 (µMol)0.03500.00030.50478.9000AID1151968; AID1240270; AID1240271; AID1240272; AID1774253; AID1774254; AID1816403; AID1854177; AID1868625; AID1882367
Histone-lysine N-methyltransferase EZH2Homo sapiens (human)Ki0.00050.00050.03170.1940AID1199092; AID1199093; AID1199094; AID1199095; AID1199096; AID1199097; AID1199098; AID1199151
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
spinal cord developmentPolycomb protein EEDHomo sapiens (human)
negative regulation of DNA-templated transcriptionPolycomb protein EEDHomo sapiens (human)
heterochromatin formationPolycomb protein EEDHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolycomb protein EEDHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolycomb protein SUZ12Homo sapiens (human)
cell population proliferationPolycomb protein SUZ12Homo sapiens (human)
positive regulation of cell population proliferationPolycomb protein SUZ12Homo sapiens (human)
negative regulation of cell differentiationPolycomb protein SUZ12Homo sapiens (human)
oligodendrocyte differentiationPolycomb protein SUZ12Homo sapiens (human)
random inactivation of X chromosomePolycomb protein SUZ12Homo sapiens (human)
facultative heterochromatin formationPolycomb protein SUZ12Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
transcription corepressor bindingPolycomb protein EEDHomo sapiens (human)
protein bindingPolycomb protein EEDHomo sapiens (human)
enzyme activator activityPolycomb protein EEDHomo sapiens (human)
histone methyltransferase activityPolycomb protein EEDHomo sapiens (human)
identical protein bindingPolycomb protein EEDHomo sapiens (human)
nucleosome bindingPolycomb protein EEDHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPolycomb protein SUZ12Homo sapiens (human)
transcription corepressor bindingPolycomb protein SUZ12Homo sapiens (human)
protein bindingPolycomb protein SUZ12Homo sapiens (human)
enzyme activator activityPolycomb protein SUZ12Homo sapiens (human)
methylated histone bindingPolycomb protein SUZ12Homo sapiens (human)
histone methyltransferase activityPolycomb protein SUZ12Homo sapiens (human)
metal ion bindingPolycomb protein SUZ12Homo sapiens (human)
lncRNA bindingPolycomb protein SUZ12Homo sapiens (human)
promoter-specific chromatin bindingPolycomb protein SUZ12Homo sapiens (human)
chromatin DNA bindingPolycomb protein SUZ12Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleusPolycomb protein EEDHomo sapiens (human)
nucleoplasmPolycomb protein EEDHomo sapiens (human)
chromosomePolycomb protein EEDHomo sapiens (human)
cytosolPolycomb protein EEDHomo sapiens (human)
ESC/E(Z) complexPolycomb protein EEDHomo sapiens (human)
nucleusPolycomb protein SUZ12Homo sapiens (human)
nucleoplasmPolycomb protein SUZ12Homo sapiens (human)
nucleolusPolycomb protein SUZ12Homo sapiens (human)
nuclear bodyPolycomb protein SUZ12Homo sapiens (human)
sex chromatinPolycomb protein SUZ12Homo sapiens (human)
chromatin silencing complexPolycomb protein SUZ12Homo sapiens (human)
ESC/E(Z) complexPolycomb protein SUZ12Homo sapiens (human)
ribonucleoprotein complexPolycomb protein SUZ12Homo sapiens (human)
RSC-type complexPolycomb protein SUZ12Homo sapiens (human)
nucleusPolycomb protein SUZ12Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (139)

Assay IDTitleYearJournalArticle
AID1199107Selectivity ratio of IC50 for human SETD7 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199108Selectivity ratio of IC50 for human SMYD2 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816530Downregulation of CENPK mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816512Downregulation of CHEK1 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816400PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as reduction in H3K27me3 level at up to 10 uM incubated for 72 hrs by Western blot analysis
AID1860974Binding affinity to recombinant PRC2 complex (unknown origin) assessed as association rate constant by surface plasmon resonance assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1872379Antitumor activity against human DLBCL pfeiffer cells xenografted in mouse assessed as tumor growth inhibition at 50 mg/kg, ip administered once daily for 36 days relative to control2022European journal of medicinal chemistry, Mar-05, Volume: 231Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs.
AID1199151Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816510Downregulation of ARL6IP mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199097Inhibition of human EZH2 Y641N mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1860968Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1318898Binding affinity to EZH2 (unknown origin) expressed in baculovirus infected SF9 cells co-expressing SUZ12/EED/RbAp48 complex assessed as binding off-rate at 0.4 uM incubated for 20 mins by Q-TOF mass spectrometry2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
AID1816403Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA immunodetection assay
AID1816499Downregulation of ARL6IP mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1151977Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1199116Selectivity ratio of IC50 for human DOT1L to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1854193Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1199098Inhibition of human EZH2 Y641C mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816391PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of SUZ12 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1860967Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1199093Inhibition of human EZH2 A677G mutant assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1860970Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816407Antiproliferative activity against human WSUDLCL2 cells harboring EZH2-Y641F mutant assessed as inhibition of cell growth at 10 uM incubated for 9 days by optical microscopic analysis
AID1240276Intrinsic clearance in human liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816506Downregulation of CEP76 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816390PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of RbAp48 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1199109Selectivity ratio of IC50 for human MMSET to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199112Selectivity ratio of IC50 for human PRMT3 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1774254Inhibition of EZH2 Y641F mutant (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1151976Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1860969Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1774255Antiproliferative activity against human WSUDLCL2 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1816513Downregulation of TACC3 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199105Selectivity ratio of IC50 for human MLL4 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816502Downregulation of CHEK1 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1868625Inhibition of wild-type 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.
AID1854177Inhibition of EZH2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1199113Selectivity ratio of IC50 for human PRMT4 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1240274Intrinsic clearance in rat liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
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.
AID1816500Downregulation of CEP76 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1151974Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1199115Selectivity ratio of IC50 for human PRMT6 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1151973Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase 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.
AID1199102Selectivity ratio of IC50 for human MLL1 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816392PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EED degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1860966Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816399PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EED degradation at up to 10 uM incubated for 72 hrs by Western blot analysis
AID1774253Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
AID1199101Selectivity ratio of IC50 for human SUV39H2 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1860971Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1199095Inhibition of human EZH2 Y641F mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
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.
AID1199099Selectivity ratio of IC50 for human G9a to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816498Downregulation of BRIC5 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199094Inhibition of human EZH2 A677G mutant assessed as H3K27me1 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199092Inhibition of human wild-type EZH2 assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816516Antiproliferative activity against human A549 cells harboring SWI/SNF mutant assessed as inhibition of cell growth at 10 uM treated for 9 days by optical microscopic analysis
AID1816511Downregulation of CEP76 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1240279Protein binding in dog plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816517Antiproliferative activity against human NCI-H1299 cells harboring SWI/SNF mutant assessed as inhibition of cell growth at 10 uM treated for 9 days by optical microscopic analysis
AID1199119Selectivity ratio of Ki(app) for human EZH1 to Ki(app) for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1860975Binding affinity to recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant by surface plasmon resonance assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1199117Selectivity ratio of IC50 for human DNMT3a to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1860973Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816507Downregulation of CHEK1 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1816397PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EZH2 degradation at up to 10 uM incubated for 72 hrs by Western blot analysis
AID1240275Intrinsic clearance in dog liver microsomes2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1860965Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1860976Binding affinity to recombinant PRC2 complex (unknown origin) assessed as Equilibrium dissociation constant by surface plasmon resonance assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816504Downregulation of BRIC5 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1151975Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1151978Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1240278Protein binding in rat plasma2015Bioorganic & 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.
AID1199104Selectivity ratio of IC50 for human MLL3 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199096Inhibition of human EZH2 Y641H mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199118Selectivity ratio of IC50 for human DNMT3b to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1199106Selectivity ratio of IC50 for human SETD8 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1151968Inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED protein complex (unknown origin) using histone H3 peptide/S-adenosylmethionine as substrate after 2 hrs by TR-FRET assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1199110Selectivity ratio of IC50 for human SETMAR to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
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.
AID1816393PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of EZH2 degradation at 1 uM incubated for 48 hrs by Western blot analysis
AID1199103Selectivity ratio of IC50 for human MLL2 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816501Downregulation of CENPK mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1854194Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Targeting EZH2 for cancer therapy: From current progress to novel strategies.
AID1151972Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay2014Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
AID1816508Downregulation of TACC3 mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1860972Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of precision targeting EZH2 degraders for triple-negative breast cancer.
AID1816404Downregulation of CENPK mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199111Selectivity ratio of IC50 for human PRMT1 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1240277Protein binding in mouse plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816505Downregulation of ARL6IP mRNA expression in human NCI-H1299 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1240280Protein binding in human plasma2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
AID1816503Downregulation of TACC3 mRNA expression in human A549 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199100Selectivity ratio of IC50 for human SUV39H1 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1816398PROTAC activity at CRBN E3 ligase/EZH2 in PRC2 complex in human WSUDLCL2 cells assessed as induction of SUZ12 degradation at up to 10 uM incubated for 72 hrs by Western blot analysis
AID1816509Downregulation of BRIC5 mRNA expression in human MDA-MB-468 cells at 10 uM incubated for 48 hrs by qRT-PCR analysis
AID1199114Selectivity ratio of IC50 for human PRMT5 to IC50 for human wild-type EZH22015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Selective inhibitors of protein methyltransferases.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID1347149Furin counterscreen 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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347168HepG2 cells viability 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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347152Confirmatory screen NINDS AMC 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.
AID1347154Primary screen GU AMC 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.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347161Confirmatory 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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347153Confirmatory screen GU AMC 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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347167Vero cells viability 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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346024Human enhancer of zeste 2 polycomb repressive complex 2 subunit (2.1.1.43 Histone methyltransferases (HMTs))2012Nature, Dec-06, Volume: 492, Issue:7427
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
AID1346024Human enhancer of zeste 2 polycomb repressive complex 2 subunit (2.1.1.43 Histone methyltransferases (HMTs))2012Journal of biomolecular screening, Dec, Volume: 17, Issue:10
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.
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 (98)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's59 (60.20)24.3611
2020's39 (39.80)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.02%)5.53%
Reviews6 (6.12%)6.00%
Case Studies0 (0.00%)4.05%
Observational1 (1.02%)0.25%
Other90 (91.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]