Page last updated: 2024-12-06

sinefungin

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

Sinefungin is a nucleoside antibiotic produced by Streptomyces griseolus. It is a potent inhibitor of S-adenosylmethionine (SAM)-dependent methyltransferases, including DNA methyltransferases and histone methyltransferases. Sinefungin has been shown to have a wide range of biological activities, including antitumor, antiviral, and antifungal activity. Its mechanism of action is based on its ability to bind to the active site of SAM-dependent methyltransferases, preventing the transfer of methyl groups from SAM to target molecules. Sinefungin has been studied extensively for its potential therapeutic applications in various diseases, including cancer, viral infections, and fungal infections. Its unique chemical structure and biological activity make it a valuable tool for investigating the role of methylation in cellular processes. Furthermore, sinefungin has been used as a probe to study the structure and function of SAM-dependent methyltransferases. Its synthesis involves a complex series of reactions, including the use of a variety of reagents and catalysts. '

Cross-References

ID SourceID
PubMed CID65482
CHEMBL ID1214186
CHEBI ID45453
SCHEMBL ID167609
MeSH IDM0048573

Synonyms (68)

Synonym
lilly 57926
ly-57926
CHEMBL1214186
chebi:45453 ,
antibiotic a 9145
sinefungine [inn-french]
brn 3574678
a 9145
compound 57926
d-glycero-alpha-l-talo-decofuranuronic acid, 6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-
sinefunginum [inn-latin]
ly 57926
rp 32232
sinefungin [usan:inn]
sinefungina [inn-spanish]
decofuranuronic acid, 6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-, (beta-d-ribo)-
antibiotic 32232 rp
decofuranuronic acid, 6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-
SFG ,
sinefungin ,
58944-73-3
sinefungin (usan/inn)
D05846
adenosyl-ornithine
sinefungin, 95% (hplc), powder
(2s,5s)-2,5-diamino-6-[(2r,3s,r,5r)-5-(6-amino-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]hexanoic acid
6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxydecofuranuronic acid
1QAQ
2H2J
DB01910
6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-beta-d-ribo-decofuranuronic acid
1AQJ
(2s,5s)-2,5-diamino-6-[(2r,3s,4r,5r)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]hexanoic acid
sinefungine
w2u467ciil ,
sinefunginum
sinefungina
unii-w2u467ciil
(5s)-5-amino-6-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]-l-norleucine
bdbm50378739
sinefungin [mi]
sinefungin [mart.]
6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-.beta.-d-ribo-decofuranuronic acid
decofuranuronic acid, 6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-, (.beta.-d-ribo)-
sinefungin [inn]
sinefungin [usan]
CCG-208696
LMXOHSDXUQEUSF-YECHIGJVSA-N
SCHEMBL167609
(2s,5s)-2,5-diamino-6-((2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)hexanoic acid
DTXSID10207689
AKOS027327588
6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-d-glycero-alpha-l-talo-decofuranuronic acid
(2s,5s)-2,5-diamino-6-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-3,4-dihydroxy-2-tetrahydrofuryl]hexanoic acid
(2s,5s)-2,5-diamino-6-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]hexanoic acid (non-preferred name)
NCGC00263619-03
NCGC00263619-01
Q27093021
HY-101938
BRD-K91100918-001-01-2
BCP28648
CS-0022195
tca-o-pcp?trichloroacetic acid pentachlorophenyl ester
(2s,5s)-5-(5'-adenosyl)-2,5-diaminopentanoic acid
A869317
AS-77750
6,9-diamino-1-(6-amino-9h-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-d-glycero-a-l-talo-decofuranuronic acid
BS162746

Research Excerpts

Overview

Sinefungin (SFG) is an antifungal and antiparasitic nucleoside antibiotic composed by ornithine and adenosine moieties both having the potential to bind copper(II) Sinefungan is an antibiotic possessing a strong anti-leishmanial activity.

ExcerptReferenceRelevance
"Sinefungin (SFG) is an antifungal and antiparasitic nucleoside antibiotic composed by ornithine and adenosine moieties both having the potential to bind copper(II). "( 1H and 13C NMR study of the complex formed by copper(II) with the nucleoside antibiotic sinefungin.
Cappannelli, M; Gaggelli, E; Jezowska-Bojczuk, M; Molteni, E; Mucha, A; Porciatti, E; Valensin, D; Valensin, G, 2007
)
2
"Sinefungin is an antibiotic possessing a strong anti-leishmanial activity. "( Sinefungin and taxol effects on cell cycle and cytoskeleton of Leishmania donovani promastigotes.
Brown, S; Gendron, MC; Moulay, L; Robert-Gero, M; Tournier, F, 1996
)
3.18
"Sinefungin is an antibiotic structurally related to S-adenosylmethionine. "( The effect of sinefungin and synthetic analogues on RNA and DNA methyltransferases from Streptomyces.
Barbes, C; Hardisson, C; Martin, CG; Sanchez, J; Yebra, MJ, 1991
)
2.08
"Sinefungin is a naturally occurring nucleoside isolated from cultures of Streptomyces griseolus and S. "( Effects of sinefungin and S-adenosylhomocysteine on DNA and protein methyltransferases from Streptomyces and other bacteria.
Barbés, C; Hardisson, C; Robert-Geró, M; Sánchez, J; Yebra, MJ, 1990
)
2.11

Effects

Sinefungin has been shown to inhibit the development of various fungi and viruses. Its major attraction to date resides in its potent antiparasitic activity.

ExcerptReferenceRelevance
"Sinefungin has the same effects on Leishmania tropica promastigotes."( Leishmania donovani: enhanced expression of soluble acid phosphatase in the presence of sinefungin, an antiparasitic agent.
Moulay, L; Robert-Gero, M, 1995
)
1.23
"Sinefungin has been shown to inhibit the development of various fungi and viruses, but its major attraction to date resides in its potent antiparasitic activity."( Molecular target of the antileishmanial action of sinefungin.
Nolan, LL, 1987
)
1.25

Bioavailability

ExcerptReferenceRelevance
" Peritoneal equilibration tests showed that sinefungin attenuated the urea nitrogen transport rate from plasma and the glucose absorption rate from the dialysate."( Inhibition of the H3K4 methyltransferase SET7/9 ameliorates peritoneal fibrosis.
Doi, S; Maeda, K; Masaki, T; Nakashima, A; Sasaki, K; Tamura, R; Ueno, T, 2018
)
0.74

Dosage Studied

ExcerptRelevanceReference
"8% following dosage at concentrations of 10 micrograms/ml and 30 micrograms/ml, respectively."( Determination of sinefungin in rat plasma by high-performance liquid chromatography.
Brasseur, P; Favennec, L; Marchand, J; Tharasse-Bloch, C, 1995
)
0.63
" Insights to the intracellular action of sinefungin stem from the finding that increased gene dosage of yeast AdoMet synthase plus cap guanine-N7 methyltransferase afforded greater resistance to sinefungin than either enzyme alone."( Sinefungin resistance of Saccharomyces cerevisiae arising from Sam3 mutations that inactivate the AdoMet transporter or from increased expression of AdoMet synthase plus mRNA cap guanine-N7 methyltransferase.
Schwer, B; Shuman, S; Zheng, S, 2007
)
2.05
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antifungal agentAn antimicrobial agent that destroys fungi by suppressing their ability to grow or reproduce.
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
[role 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]

Drug Classes (2)

ClassDescription
adenosinesAny purine ribonucleoside that is a derivative of adenosine.
non-proteinogenic alpha-amino acidAny alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
[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]

Pathways (4)

PathwayProteinsCompounds
L-methionine salvage cycle II (plants)829
L-methionine salvage cycle I (bacteria and plants)232
S-methyl-5'-thioadenosine degradation I214
Creatine pathway116

Protein Targets (28)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ermc' MethyltransferaseBacillus subtilisKi18.000018.000025.500033.0000AID977610
Chain A, Ermc' Rrna MethyltransferaseBacillus subtilisKi18.000018.000025.500033.0000AID977610
NS5 Zika virusIC50 (µMol)1.40001.18001.38671.6200AID1558311; AID1558312
Protein arginine N-methyltransferase 5Homo sapiens (human)IC50 (µMol)8.60000.00900.69158.6000AID1530641
mRNA cap guanine-N7 methyltransferaseHomo sapiens (human)IC50 (µMol)0.03350.00050.03350.0500AID1718108; AID1718112; AID1739792
Indolethylamine N-methyltransferaseHomo sapiens (human)IC50 (µMol)4.00004.00004.00004.0000AID1885879
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC50 (µMol)0.31900.00402.92669.9600AID1806268
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)0.30720.00022.45859.9600AID1806268; AID1893717; AID1908792; AID1908796
Nicotinamide N-methyltransferaseHomo sapiens (human)IC50 (µMol)39.23673.62004.41005.2000AID1510774; AID1885881; AID1885883
Histone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)IC50 (µMol)33.71000.00010.51357.0000AID1390742
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC50 (µMol)2.50000.00202.52666.0800AID476874
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC50 (µMol)179.73330.00251.14809.2000AID1137572; AID1461879; AID1461884
Protein arginine N-methyltransferase 1Homo sapiens (human)IC50 (µMol)1.00000.25003.61679.4000AID476872
RNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)IC50 (µMol)0.31900.27800.31900.3600AID1806268
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC50 (µMol)180.50000.01300.79954.9000AID1137571; AID1461878; AID1461885
Non-structural protein 1 Dengue virusIC50 (µMol)0.04100.04101.32592.3000AID1631411
[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)
Chain A, ADENINE-N6-DNA-METHYLTRANSFERASE TAQIThermus aquaticusKd0.34000.34001.37002.4000AID977611
Chain A, Adenine-n6-dna-methyltransferase TaqiThermus aquaticusKd0.34000.34001.37002.4000AID977611
Chain B, ADENINE-N6-DNA-METHYLTRANSFERASE TAQIThermus aquaticusKd0.34000.34001.37002.4000AID977611
Chain A, Ribulose-1,5 bisphosphate carboxylase/oxygenasePisum sativum (garden pea)Kd4.20004.2000341.80001,000.0000AID977611
Chain A, Ribulose-1,5 bisphosphate carboxylase/oxygenase large subunit N-methyltransferasePisum sativum (garden pea)Kd4.20004.2000341.80001,000.0000AID977611
Chain A, Ribulose-1,5 bisphosphate carboxylase/oxygenase large subunit N-methyltransferasePisum sativum (garden pea)Kd4.20004.2000341.80001,000.0000AID977611
Chain A, Ribulose-1,5 bisphosphate carboxylase/oxygenase large subunit N-methyltransferasePisum sativum (garden pea)Kd4.20004.2000341.80001,000.0000AID977611
tRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)Kd7.50007.50007.50007.5000AID1881233
Thiopurine S-methyltransferaseHomo sapiens (human)Kd10.000010.000010.000010.0000AID1179566
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interferon gamma precursorHomo sapiens (human)AC501.14350.128015.173038.6100AID1259418; AID1259420
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (106)

Processvia Protein(s)Taxonomy
tRNA methylationtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
response to amphetaminetRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
tRNA modificationtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
tRNA stabilizationtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
peptidyl-arginine N-methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
spliceosomal snRNP assemblyProtein arginine N-methyltransferase 5Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 5Homo sapiens (human)
DNA-templated transcription terminationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of mitotic nuclear divisionProtein arginine N-methyltransferase 5Homo sapiens (human)
peptidyl-arginine methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
circadian regulation of gene expressionProtein arginine N-methyltransferase 5Homo sapiens (human)
endothelial cell activationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of cell differentiationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of mRNA splicing, via spliceosomeProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of oligodendrocyte differentiationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of ERK1 and ERK2 cascadeProtein arginine N-methyltransferase 5Homo sapiens (human)
Golgi ribbon formationProtein arginine N-methyltransferase 5Homo sapiens (human)
liver regenerationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of signal transduction by p53 class mediatorProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting dopamine receptor signaling pathwayProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of DNA-templated transcriptionProtein arginine N-methyltransferase 5Homo sapiens (human)
7-methylguanosine mRNA cappingmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
RNA 5'-cap (guanine-N7)-methylationmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
cellular response to leukemia inhibitory factormRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
amine metabolic processIndolethylamine N-methyltransferaseHomo sapiens (human)
response to toxic substanceIndolethylamine N-methyltransferaseHomo sapiens (human)
methylationIndolethylamine N-methyltransferaseHomo sapiens (human)
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
protein methylationProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
protein repairProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
nicotinamide metabolic processNicotinamide N-methyltransferaseHomo sapiens (human)
response to xenobiotic stimulusNicotinamide N-methyltransferaseHomo sapiens (human)
response to organonitrogen compoundNicotinamide N-methyltransferaseHomo sapiens (human)
animal organ regenerationNicotinamide N-methyltransferaseHomo sapiens (human)
methylationNicotinamide N-methyltransferaseHomo sapiens (human)
NAD biosynthesis via nicotinamide riboside salvage pathwayNicotinamide N-methyltransferaseHomo sapiens (human)
positive regulation of gluconeogenesisNicotinamide N-methyltransferaseHomo sapiens (human)
positive regulation of protein deacetylationNicotinamide N-methyltransferaseHomo sapiens (human)
nucleobase-containing compound metabolic processThiopurine S-methyltransferaseHomo sapiens (human)
xenobiotic metabolic processThiopurine S-methyltransferaseHomo sapiens (human)
methylationThiopurine S-methyltransferaseHomo sapiens (human)
xenobiotic catabolic processThiopurine S-methyltransferaseHomo sapiens (human)
glycogen metabolic processGlycine N-methyltransferaseHomo sapiens (human)
methionine metabolic processGlycine N-methyltransferaseHomo sapiens (human)
methylationGlycine N-methyltransferaseHomo sapiens (human)
protein modification processGlycine N-methyltransferaseHomo sapiens (human)
S-adenosylmethionine metabolic processGlycine N-methyltransferaseHomo sapiens (human)
protein homotetramerizationGlycine N-methyltransferaseHomo sapiens (human)
S-adenosylhomocysteine metabolic processGlycine N-methyltransferaseHomo sapiens (human)
sarcosine metabolic processGlycine N-methyltransferaseHomo sapiens (human)
one-carbon metabolic processGlycine N-methyltransferaseHomo sapiens (human)
regulation of gluconeogenesisGlycine N-methyltransferaseHomo sapiens (human)
positive regulation of cell population proliferationHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
gene expressionHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
heterochromatin formationHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
telomere organizationHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
methylationHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
regulation of receptor signaling pathway via JAK-STATHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
regulation of transcription regulatory region DNA bindingHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
DNA repairHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
DNA damage checkpoint signalingHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
DNA damage responseHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
heterochromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin remodelingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
peptidyl-lysine monomethylationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
response to ethanolHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
heterochromatin organizationHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to starvationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of DNA replicationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
synaptonemal complex assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
spermatid developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
long-term memoryHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
fertilizationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
regulation of protein modification processHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
organ growthHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
phenotypic switchingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to ethanolHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
behavioral response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
oocyte developmentHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
neuron fate specificationHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
response to fungicideHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to cocaineHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
cellular response to xenobiotic stimulusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of autophagosome assemblyHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
in utero embryonic developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
protein methylationProtein arginine N-methyltransferase 1Homo sapiens (human)
DNA damage responseProtein arginine N-methyltransferase 1Homo sapiens (human)
cell surface receptor signaling pathwayProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of cell population proliferationProtein arginine N-methyltransferase 1Homo sapiens (human)
RNA splicingProtein arginine N-methyltransferase 1Homo sapiens (human)
peptidyl-arginine methylationProtein arginine N-methyltransferase 1Homo sapiens (human)
viral protein processingProtein arginine N-methyltransferase 1Homo sapiens (human)
regulation of BMP signaling pathwayProtein arginine N-methyltransferase 1Homo sapiens (human)
neuron projection developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of erythrocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
regulation of megakaryocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
negative regulation of megakaryocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of translationProtein arginine N-methyltransferase 1Homo sapiens (human)
negative regulation of JNK cascadeProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of hemoglobin biosynthetic processProtein arginine N-methyltransferase 1Homo sapiens (human)
cardiac muscle tissue developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
protein homooligomerizationProtein arginine N-methyltransferase 1Homo sapiens (human)
cellular response to methionineProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of p38MAPK cascadeProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of TORC1 signalingProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationProtein arginine N-methyltransferase 1Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 1Homo sapiens (human)
peptidyl-arginine methylation, to asymmetrical-dimethyl arginineProtein arginine N-methyltransferase 1Homo sapiens (human)
7-methylguanosine mRNA cappingRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
RNA 5'-cap (guanine-N7)-methylationRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
methylationRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
chromatin organizationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
peptidyl-lysine monomethylationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
peptidyl-lysine dimethylationHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
regulation of embryonic developmentHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
response to fungicideHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (67)

Processvia Protein(s)Taxonomy
RNA bindingtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
tRNA methyltransferase activitytRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
tRNA (cytidine-5-)-methyltransferase activitytRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
p53 bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
transcription corepressor activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
methyl-CpG bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein-arginine omega-N symmetric methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
identical protein bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
ribonucleoprotein complex bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
histone H4R3 methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein heterodimerization activityProtein arginine N-methyltransferase 5Homo sapiens (human)
E-box bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
histone H3 methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
histone arginine N-methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
RNA bindingmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
mRNA 5'-cap (guanine-N7-)-methyltransferase activitymRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
protein bindingmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
thioether S-methyltransferase activityIndolethylamine N-methyltransferaseHomo sapiens (human)
protein bindingIndolethylamine N-methyltransferaseHomo sapiens (human)
amine N-methyltransferase activityIndolethylamine N-methyltransferaseHomo sapiens (human)
S-adenosyl-L-methionine:beta-alanine N-methyltransferase activityIndolethylamine N-methyltransferaseHomo sapiens (human)
N-methyltransferase activityIndolethylamine N-methyltransferaseHomo sapiens (human)
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
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
protein-L-isoaspartate (D-aspartate) O-methyltransferase activityProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
protein bindingProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
cadherin bindingProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
nicotinamide N-methyltransferase activityNicotinamide N-methyltransferaseHomo sapiens (human)
pyridine N-methyltransferase activityNicotinamide N-methyltransferaseHomo sapiens (human)
protein bindingThiopurine S-methyltransferaseHomo sapiens (human)
thiopurine S-methyltransferase activityThiopurine S-methyltransferaseHomo sapiens (human)
S-adenosyl-L-methionine bindingThiopurine S-methyltransferaseHomo sapiens (human)
protein bindingGlycine N-methyltransferaseHomo sapiens (human)
folic acid bindingGlycine N-methyltransferaseHomo sapiens (human)
glycine bindingGlycine N-methyltransferaseHomo sapiens (human)
glycine N-methyltransferase activityGlycine N-methyltransferaseHomo sapiens (human)
identical protein bindingGlycine N-methyltransferaseHomo sapiens (human)
S-adenosyl-L-methionine bindingGlycine N-methyltransferaseHomo sapiens (human)
nucleic acid bindingHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
DNA bindingHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
protein bindingHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
histone methyltransferase activityHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
histone H3 methyltransferase activityHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
histone H3K79 trimethyltransferase activityHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
histone H3K79 methyltransferase activityHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone H3 methyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
histone H3K4 monomethyltransferase activityHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromatin bindingHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
enzyme bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
C2H2 zinc finger domain bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K56 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
histone H3K9me2 methyltransferase activityHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
promoter-specific chromatin bindingHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
RNA bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
N-methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
protein methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
methyl-CpG bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
enzyme bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine omega-N monomethyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine omega-N asymmetric methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
identical protein bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
histone H4R3 methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
mitogen-activated protein kinase p38 bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
GATOR1 complex bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
S-adenosyl-L-methionine bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
RNA bindingRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
protein bindingRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
enzyme activator activityRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
molecular function activator activityRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
transcription corepressor bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
p53 bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
protein bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
zinc ion bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
protein-lysine N-methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K9 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K27 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
C2H2 zinc finger domain bindingHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
histone H3K9me2 methyltransferase activityHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
nucleoplasmtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
cytoplasmtRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
nucleustRNA (cytosine(38)-C(5))-methyltransferaseHomo sapiens (human)
nucleusProtein arginine N-methyltransferase 5Homo sapiens (human)
nucleoplasmProtein arginine N-methyltransferase 5Homo sapiens (human)
Golgi apparatusProtein arginine N-methyltransferase 5Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 5Homo sapiens (human)
methylosomeProtein arginine N-methyltransferase 5Homo sapiens (human)
chromatinProtein arginine N-methyltransferase 5Homo sapiens (human)
cytoplasmProtein arginine N-methyltransferase 5Homo sapiens (human)
histone methyltransferase complexProtein arginine N-methyltransferase 5Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 5Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 5Homo sapiens (human)
fibrillar centermRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
nucleusmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
nucleoplasmmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
mRNA capping enzyme complexmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
receptor complexmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
mRNA cap methyltransferase RNMT:RAMAC complexmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
nucleusmRNA cap guanine-N7 methyltransferaseHomo sapiens (human)
cytosolIndolethylamine N-methyltransferaseHomo sapiens (human)
cytosolIndolethylamine N-methyltransferaseHomo sapiens (human)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cytosolProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
extracellular exosomeProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
extracellular vesicleProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
cytoplasmProtein-L-isoaspartate(D-aspartate) O-methyltransferaseHomo sapiens (human)
cytosolNicotinamide N-methyltransferaseHomo sapiens (human)
cytosolNicotinamide N-methyltransferaseHomo sapiens (human)
cytosolThiopurine S-methyltransferaseHomo sapiens (human)
cytosolGlycine N-methyltransferaseHomo sapiens (human)
cytosolGlycine N-methyltransferaseHomo sapiens (human)
nucleusHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
cytoplasmHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
intracellular membrane-bounded organelleHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
protein-containing complexHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
nucleusHistone-lysine N-methyltransferase, H3 lysine-79 specificHomo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromosomeHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
nucleolusHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
chromosomeHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase SETD7Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nuclear speckHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT2Homo sapiens (human)
lysosomal membraneProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleoplasmProtein arginine N-methyltransferase 1Homo sapiens (human)
cytoplasmProtein arginine N-methyltransferase 1Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 1Homo sapiens (human)
methylosomeProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleusRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
mRNA capping enzyme complexRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
mRNA cap methyltransferase RNMT:RAMAC complexRNA guanine-N7 methyltransferase activating subunitHomo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nucleoplasmHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nuclear bodyHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
chromatinHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
nucleusHistone-lysine N-methyltransferase EHMT1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (102)

Assay IDTitleYearJournalArticle
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.
AID1347150Optimization screen NINDS AMC qHTS for Zika virus inhibitors: Linked 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.
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.
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.
AID1347155Optimization screen NINDS Rhodamine qHTS for Zika virus inhibitors: Linked 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.
AID1347151Optimization of GU AMC 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.
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.
AID1806268MTase Filter-Binding Assay (FBA) from Article 10.1021/acs.jmedchem.2c00120: \\Potent Inhibition of SARS-CoV-2 nsp14 \\2022Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
Potent Inhibition of SARS-CoV-2 nsp14
AID1631411Inhibition of Dengue virus ribose 2'-O methyltransferase using RNA substrate after 20 mins in presence of [methyl-3H]-AdoMet by microbeta counting analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
The Medicinal Chemistry of Dengue Virus.
AID1631412Binding affinity to His-tagged Dengue virus 3 methyltransferase expressed in Escherichia coli Rosetta 2(DE3) by VP-ITC isothermal titration calorimetry2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
The Medicinal Chemistry of Dengue Virus.
AID1881246Inhibition of DNMT2-mediated tRNA methylation in human HEK293 cells assessed as reduction in m5C at C38 of tRNA at 100 uM incubated for 24 hrs by LC-MS/MS analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1631413Potency index, ratio of S-adenosyl-L-methionine Kd to sinefungin Kd for His-tagged Dengue virus 3 methyltransferase expressed in Escherichia coli Rosetta 2(DE3)2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
The Medicinal Chemistry of Dengue Virus.
AID1908797Inhibition of N7-MTase activity of SARS-CoV-2 N-terminus hexahistidine tag nsp14 expressed in Escherichia coli C2566 at 5 uM using [3H]SAM as substrate incubated for 30 mins in presence of mGpppAC4 synthetic RNA by filter binding assay relative to control2022Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
Potent Inhibition of SARS-CoV-2 nsp14
AID1461884Inhibition of EHMT2 (unknown origin)2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1718106Inhibition of Transmissible gastroenteritis coronavirus H16 guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1)2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID96105Growth inhibition of Leishmania donovani promastigotes by the compound at 0.26 uM1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Total synthesis of uracil analogues of sinefungin.
AID1461878Inhibition of EHMT1 (unknown origin) preincubated for 5 mins followed by SAM and biotinylated H3K9 peptide addition measured after 120 mins by HTRF assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1718108Inhibition of human guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1)2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1881233Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as dissociation constant at 100 uM by isothermal titration calorimetry assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID476874Inhibition of GST-fused human recombinant SET7 after 90 mins by SDS-PAGE based scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases.
AID1739792Inhibition of N-terminal His6-tagged human RNA-N7 MTase expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1777106Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1718109Inhibition of SARS coronavirus WHU guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1)2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1558311Inhibition of Zika virus MTase (4 to 278 residues) expressed in Escherichia coli T7 using GpppAC4 as substrate in presence of [3H]SAM incubated for 30 mins by liquid scintillation counter method2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1881235Selectivity ratio of Kd for binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as dissociation constant to IC50 for inhibition of full length human N-terminal his6-tagged DNMT2 expr2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1390742Inhibition of recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) using oligonucleosome as substrate measured after 30 mins in presence of SAM by AlphaLISA assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay.
AID164156Kinetic constant was measured for Protein Methylase II of Leishmania donovani promastigotes using supernatant (S12) fraction1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Total synthesis of uracil analogues of sinefungin.
AID1461879Inhibition of EHMT2 (unknown origin) preincubated for 15 mins followed by SAM and biotinylated H3K9 peptide addition measured after 30 mins by TR-FRET assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1881241Inhibition of full length human NSUN6 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM measured at 20 mins by liquid scintillation counting analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1461877Inhibition of EHMT2 (unknown origin) at 400 uM preincubated for 15 mins followed by SAM and biotinylated H3K9 peptide addition measured after 30 mins by TR-FRET assay relative to control2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1408347Antiviral activity against Zika virus SMGC infected in BHK cells assessed as inhibition of virus induced cytopathic effect after 8 days by CellTiter-Glo luminescent cell viability assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.
AID1558312Inhibition of Zika virus MTase (4 to 278 residues) expressed in Escherichia coli T7 using A27 RNA as substrate in presence of [3H]SAM incubated for 30 mins by liquid scintillation counter method2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1777105Cytotoxicity against mouse BALB/c3T3 clone A31 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1881237Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as change in enthalpy change at 100 uM by isothermal titration calorimetry assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1777107Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by neutral red uptake assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1893719Antiviral activity against SARS-CoV-2 infected in human A549 cells overexpressing ACE2 and TMPRSS2 assessed as inhibition of viral growth at 50 uM incubated for 48 hrs by DAPI staining based immunofluorescence assay
AID1881240Inhibition of full length recombinant human NSUN2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM measured at 20 mins by liquid scintillation counting analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1885879Inhibition of N-terminal 6His-tagged full length human recombinant INMT (1 to 263 residues) expressed in Escherichia coli BL21 (DE3) cells using S-(5'-Adenosyl)-L-methionine chloride dihydrochloride and 9H-pyrido[3,4-b]indole as substrate incubated for 2.2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
AID1777103Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 Wuhan-Hu-1 NSP16/10 expressed in Escherichia coli using m7GpppA-RNA and SAM as substrate incubated for 2 hrs by HTRF assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1461876Inhibition of EHMT1 (unknown origin) at 200 uM preincubated for 5 mins followed by SAM and biotinylated H3K9 peptide addition measured after 120 mins by HTRF assay relative to control2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1777112Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP16 (6776 to 7073 residues) expressed in Escherichia coli C41(DE3) using 7MeGpppAC5 and [3H]AdoMet as substrate incubated for 4 hrs by filter binding assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1893717Inhibition of MTase activity of SARS-CoV-2 NSP14 expressed in Escherichia coli BL21(DE3) using GpppA and SAM as substrate preincubated for 15 mins followed by SAM addition incubated for 15 mins by LC-MS/MS analysis
AID1881243Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM by liquid scintillation counting analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1777113Inhibition of MTase activity of SARS-CoV-1 WHU NSP14 expressed in Escherichia coli BL21(DE3) using GpppA and S-adenosyl-[methyl-3H]methionine as substrate preincubated with enzyme for 20 mins followed by S-adenosyl-[methyl-3H]methionine addition and measu2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1718112Inhibition of N-terminus hexa-histidine tagged-human guanine-N7 methyltransferase expressed in Escherichia coli using GpppAC4 RNA as substrate incubated for 30 mins by liquid scintillation counting method2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1739793Binding affinity to SARS-CoV nsp14 assessed as increase in melting temperature at 1 mM at pH 7.5 by differential scanning fluorimetry2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1699913Inhibition of Dengue virus 2'-O methyltransferase incubated for 15 mins followed by [methyl-3-H]-AdoMet addition and measured after 30 mins by microbeta counter method2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro.
AID1777114Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate incubated for 30 mins by filter binding assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1881232Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using tRNA asp as substrate and SAM as co-substrate incubated for 5 mins by tritium incorporation assay relative to control2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1881234Inhibition of full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS by isothermal titration calorimetry assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1885881Inhibition of NNMT in HEK293 cells measured after 20 to 24 hrs by RapidFire Mass Spectrometry2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
AID1893721Cytotoxicity against human A549 cells overexpressing ACE2 and TMPRSS2 assessed as cell viability at 50 uM incubated for 48 hrs by MTS assay
AID1881238Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as change in entropy at 100 uM by isothermal titration calorimetry assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1530641Inhibition of full-length N-terminal FLAG-tagged PRMT5 (unknown origin) (1 to 637 residues) expressed in baculovirus infected Sf9 insect cells using histone H4 as peptide after 5 hrs in presence of [H3]AdoMet by scintillation proximity assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors.
AID772727Inhibition of Escherichia coli TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
AID1461881Antiproliferative activity against human HL60 cells at 200 uM after 72 hrs by CCK8 assay relative to control2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1699915Inhibition of Dengue virus N-7 methyltransferase incubated for 15 mins followed by [methyl-3-H]-AdoMet addition and measured after 15 mins by microbeta counter method2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro.
AID1777109Permeability of the compound in human A549 cells at 20 uM incubated for 24 hrs with 2*10^4 cells/ml media by LC/MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID476872Inhibition of GST-fused human recombinant PRMT1 after 90 mins by SDS-PAGE based scintillation counting2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases.
AID1783405Inhibition of full length ZIKV NS5-MTase domain using 7MeGpppAC4 as a substrate incubated for 30 mins by filter binding assay2021European journal of medicinal chemistry, Nov-15, Volume: 224System-oriented optimization of multi-target 2,6-diaminopurine derivatives: Easily accessible broad-spectrum antivirals active against flaviviruses, influenza virus and SARS-CoV-2.
AID1881247Inhibition of DNMT2-mediated tRNA methylation in human HEK293 cells assessed as reduction in m5C at C38 of tRNA by measuring m5C level at 100 uM incubated for 24 hrs by bisulfite sequencing analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1739791Inhibition of N7-MTase activity of N-terminal His6-tagged SARS-CoV nsp14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1226489Displacement of [3H]-SAM from biotinylated Dengue virus 3 methyltransferase expressed in Escherichia coli at 20 uM preincubated for 20 mins followed by [3H]-SAM addition measured after 15 mins by scintillation counting analysis2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus.
AID772726Inhibition of Staphylococcus aureus TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
AID1739789Inhibition of N7-MTase activity of Vaccinia virus mRNA capping enzyme D1/D12 complex using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1881245Cytotoxicity against human HEK293 cells assessed as cell viability at 100 uM measured after 24 hrs by MTT assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1718110Selectivity index, ratio of IC50 for human guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1) to IC50 for SARS coronavirus WHU guanine-N7 methyltransferase expressed in Sacchar2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1510775Inhibition of wild-type human full length NNMT expressed in Escherichia coli BL21(DE3) cells assessed as reduction in 1-methyl-nicotinamide formation at 250 uM pre-incubated for 10 mins followed by AdoMet and nicotinamide addition measured after 30 mins b2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Bisubstrate Inhibitors of Nicotinamide
AID1137571Inhibition of methyltransferase activity of EHMT1 (unknown origin)-mediated dimethylation of a biotinylated histone H3 peptide at lysine-9 by FRET-based LANCE ultra G9a assay2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.
AID1777104Inhibition of N-terminal His-tagged human recombinant Glycine-N-methyltransferase (1 to 295 residues) expressed in Escherichia coli using glycine and SAM as substrate incubated for 30 mins by HTRF assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1885883Inhibition of N-terminal 6His-tagged full length human recombinant NNMT (1 to 264 residues) expressed in Escherichia coli BL21 (DE3) cells using S-adenosyl-L-methionine and NAM as substrate incubated for 2 hrs by by RapidFire Mass Spectrometry2022Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15
Peptide-to-Small Molecule: A Pharmacophore-Guided Small Molecule Lead Generation Strategy from High-Affinity Macrocyclic Peptides.
AID1739790Inhibition of N-terminal His6-tagged human RNA-N7 MTase expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1461885Inhibition of EHMT1 (unknown origin)2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1908796Inhibition of SARS-CoV-2 nsp14 N7-MTase activity using [3H]SAM as substrate incubated for 30 mins in presence of GpppAC4 synthetic RNA and 7mGpppAC4 by DEAE radioactive filter binding assay2022Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
Potent Inhibition of SARS-CoV-2 nsp14
AID1461882Antiproliferative activity against human MDA-MB-231 cells at 200 uM after 72 hrs by sulforhodamine B assay relative to control2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
AID1718113Selectivity ratio of IC50 for N-terminus hexa-histidine tagged-human guanine-N7 methyltransferase expressed in Escherichia coli to IC50 for N-terminus hexa-histidine tagged-SARS-coV guanine-N7 methyltransferase expressed in Escherichia coli2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1510774Inhibition of wild-type human full length NNMT expressed in Escherichia coli BL21(DE3) cells assessed as reduction in 1-methyl-nicotinamide formation pre-incubated for 10 mins followed by AdoMet and nicotinamide addition measured after 30 mins by UHP-HILI2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Bisubstrate Inhibitors of Nicotinamide
AID1908792Inhibition of N7-MTase activity of SARS-CoV-2 N-terminus hexahistidine tag nsp14 expressed in Escherichia coli C2566 using [3H]SAM as substrate incubated for 30 mins in presence of mGpppAC4 synthetic RNA by radioactive filter binding assay2022Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
Potent Inhibition of SARS-CoV-2 nsp14
AID772725Inhibition of Haemophilus influenzae TrmD using S-[methyl-3H] adenosyl-L-methionine as substrate assessed as leucine-tRNA methylation after 1 hr by scintillation proximity assay2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
AID164155Kinetic constant was measured for Protein Methylase II of Leishmania donovani promastigotes using protein extracted from the 12000g pellet(P12).1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Total synthesis of uracil analogues of sinefungin.
AID1408348Cytotoxicity against BHK cells after 8 days by CellTiter-Glo assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.
AID1881239Inhibition of recombinant human DNMT3A-3L expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using Poly(dI-dC)-Poly(dI-dC) as substrate measured at 150 mins by liquid scintillation counting analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1137572Inhibition of methyltransferase activity of EHMT2 (unknown origin)-mediated dimethylation of a biotinylated histone H3 peptide at lysine-9 by FRET-based LANCE ultra G9a assay2014ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.
AID1179566Binding affinity to thiopurine methyltransferase (unknown origin) by NMR analysis2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Elements and modulation of functional dynamics.
AID1631410Inhibition of Dengue virus guanine N-7 methyltransferase using RNA substrate after 20 mins in presence of [methyl-3H]-AdoMet by microbeta counting analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
The Medicinal Chemistry of Dengue Virus.
AID1739788Inhibition of N7-MTase activity of N-terminal His6-tagged SARS-CoV nsp14 expressed in Escherichia coli using GpppAC4 and [3H]SAM as substrate at 50 uM preincubated with enzyme followed by substrate addition and measured after 30 mins by filter binding ass2020European journal of medicinal chemistry, Sep-01, Volume: 201Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.
AID1777111Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-1 NSP14 (5903 to 6429 residues) expressed in Escherichia coli C41(DE3) using GpppAC5 and [3H]AdoMet as substrate incubated for 4 hrs by filter binding assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1718107Inhibition of Avian infectious bronchitis virus (strain-Beaudette CK) guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1)2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1783404Inhibition of DENV NS5-MTase domain using GpppA2'OMe-RNA74 as a substrate incubated for 30 mins by filter binding assay2021European journal of medicinal chemistry, Nov-15, Volume: 224System-oriented optimization of multi-target 2,6-diaminopurine derivatives: Easily accessible broad-spectrum antivirals active against flaviviruses, influenza virus and SARS-CoV-2.
AID1718105Inhibition of MHV-A59 guanine-N7 methyltransferase expressed in Saccharomyces cerevisiae YBS40 (MATa leu2 ade2 trp1 his3 ura3 can1 abd1::hisGp360-ABD1)2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Druggable targets from coronaviruses for designing new antiviral drugs.
AID1881231Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM incubated for 5 mins by microscale thermophoresis assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1881236Binding affinity to full length human N-terminal his6-tagged DNMT2 expressed in Escherichia coli Rosetta2(DE3)pLysS assessed as gibbs free energy change at 100 uM by isothermal titration calorimetry assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1777108Permeability of the compound in human A549 cells at 20 uM incubated for 24 hrs with 1*10^4 cells/ml media by LC/MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID1777102Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 NSP14 expressed in Escherichia coli BL21(DE3) using GpppG and SAM as substrate incubated for 20 mins by HTRF assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
AID772713Inhibition of human SET7/92013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Selective inhibitors of bacterial t-RNA-(N(1)G37) methyltransferase (TrmD) that demonstrate novel ordering of the lid domain.
AID1881242Inhibition of recombinant human EHMT2 G9a expressed in Escherichia coli Rosetta2(DE3)pLysS at 100 uM using histone H3 as substrate measured at 120 mins by liquid scintillation counting analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment.
AID1811Experimentally measured binding affinity data derived from PDB1999Journal of molecular biology, Jun-04, Volume: 289, Issue:2
The 2.2 A structure of the rRNA methyltransferase ErmC' and its complexes with cofactor and cofactor analogs: implications for the reaction mechanism.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1999Journal of molecular biology, Jun-04, Volume: 289, Issue:2
The 2.2 A structure of the rRNA methyltransferase ErmC' and its complexes with cofactor and cofactor analogs: implications for the reaction mechanism.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB1997Journal of molecular biology, Jan-10, Volume: 265, Issue:1
Differential binding of S-adenosylmethionine S-adenosylhomocysteine and Sinefungin to the adenine-specific DNA methyltransferase M.TaqI.
AID1811Experimentally measured binding affinity data derived from PDB1997Journal of molecular biology, Jan-10, Volume: 265, Issue:1
Differential binding of S-adenosylmethionine S-adenosylhomocysteine and Sinefungin to the adenine-specific DNA methyltransferase M.TaqI.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2006The Journal of biological chemistry, Jul-14, Volume: 281, Issue:28
Catalytic roles for carbon-oxygen hydrogen bonding in SET domain lysine methyltransferases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (194)

TimeframeStudies, This Drug (%)All Drugs %
pre-199037 (19.07)18.7374
1990's53 (27.32)18.2507
2000's37 (19.07)29.6817
2010's50 (25.77)24.3611
2020's17 (8.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.97

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 Index34.97 (24.57)
Research Supply Index5.29 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index48.16 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews6 (3.03%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other192 (96.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]