Page last updated: 2024-11-13

unc 0321

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Description

7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine: a G9a antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46901937
CHEMBL ID1214066
CHEBI ID94307
SCHEMBL ID16512777
MeSH IDM0549681

Synonyms (28)

Synonym
CHEMBL1214066 ,
NCGC00187789-01
bdbm50323813
7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-n-(1-methylpiperidin-4-yl)quinazolin-4-amine
BRD-K74236984-001-01-4
HY-10930
unc 0321
unc-0321
unc0321
SCHEMBL16512777
7-[2-[2-(dimethylamino)ethoxy]ethoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-n-(1-methylpiperidin-4-yl)quinazolin-4-amine
gtpl8389
1238673-32-9
AKOS030526346
7-{2-[2-(dimethylamino)ethoxy]ethoxy}-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-n-(1-methylpiperidin-4-yl)quinazolin-4-amine
CHEBI:94307
unc0321(tfa salt)
BCP24241
EX-A7316
Q27089085
BCP12391
SB19348
F85003
MS-29574
YSZC347
A927576
DTXSID201025974
AC-35493
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline 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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency36.25290.100020.879379.4328AID588453; AID588456
TDP1 proteinHomo sapiens (human)Potency35.48130.000811.382244.6684AID686979
flap endonuclease 1Homo sapiens (human)Potency28.18380.133725.412989.1251AID588795
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.11870.050127.073689.1251AID588590
[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)
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC50 (µMol)0.01500.00040.21474.0000AID497477
Protein arginine N-methyltransferase 3Homo sapiens (human)IC50 (µMol)40.00000.01901.29957.1000AID497482
Histone-lysine N-methyltransferase SETD7Homo sapiens (human)IC50 (µMol)40.00000.00202.52666.0800AID497480
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC50 (µMol)6.50220.00251.14809.2000AID497473; AID497475; AID618483; AID618490
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC50 (µMol)0.01900.01300.79954.9000AID497474; AID497477
N-lysine methyltransferase KMT5AHomo sapiens (human)IC50 (µMol)40.00000.21002.37389.0000AID497481
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
negative regulation of protein ubiquitinationProtein arginine N-methyltransferase 3Homo sapiens (human)
methylationProtein arginine N-methyltransferase 3Homo sapiens (human)
negative regulation of retinoic acid biosynthetic processProtein arginine N-methyltransferase 3Homo sapiens (human)
peptidyl-arginine methylation, to asymmetrical-dimethyl arginineProtein arginine N-methyltransferase 3Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 3Homo sapiens (human)
protein methylationProtein arginine N-methyltransferase 3Homo 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)
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)
negative regulation of transcription by RNA polymerase IIN-lysine methyltransferase KMT5AHomo sapiens (human)
chromatin remodelingN-lysine methyltransferase KMT5AHomo sapiens (human)
mitotic chromosome condensationN-lysine methyltransferase KMT5AHomo sapiens (human)
peptidyl-lysine monomethylationN-lysine methyltransferase KMT5AHomo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorN-lysine methyltransferase KMT5AHomo sapiens (human)
negative regulation of DNA-templated transcriptionN-lysine methyltransferase KMT5AHomo sapiens (human)
cell divisionN-lysine methyltransferase KMT5AHomo sapiens (human)
regulation of signal transduction by p53 class mediatorN-lysine methyltransferase KMT5AHomo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationN-lysine methyltransferase KMT5AHomo sapiens (human)
regulation of transcription by RNA polymerase IIN-lysine methyltransferase KMT5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
protein bindingProtein arginine N-methyltransferase 3Homo sapiens (human)
methyltransferase activityProtein arginine N-methyltransferase 3Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 3Homo sapiens (human)
protein-arginine omega-N monomethyltransferase activityProtein arginine N-methyltransferase 3Homo sapiens (human)
protein-arginine omega-N asymmetric methyltransferase activityProtein arginine N-methyltransferase 3Homo sapiens (human)
ribosome bindingProtein arginine N-methyltransferase 3Homo sapiens (human)
metal ion bindingProtein arginine N-methyltransferase 3Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 3Homo 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)
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)
transcription corepressor activityN-lysine methyltransferase KMT5AHomo sapiens (human)
protein bindingN-lysine methyltransferase KMT5AHomo sapiens (human)
lysine N-methyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
protein-lysine N-methyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
histone methyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
histone H4K20 methyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
histone H4 methyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
histone H4K20 monomethyltransferase activityN-lysine methyltransferase KMT5AHomo sapiens (human)
transcription regulator activityN-lysine methyltransferase KMT5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
cytoplasmProtein arginine N-methyltransferase 3Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 3Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 3Homo 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)
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)
nucleoplasmN-lysine methyltransferase KMT5AHomo sapiens (human)
cytosolN-lysine methyltransferase KMT5AHomo sapiens (human)
chromatinN-lysine methyltransferase KMT5AHomo sapiens (human)
polytene chromosomeN-lysine methyltransferase KMT5AHomo sapiens (human)
nucleusN-lysine methyltransferase KMT5AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID497473Inhibition of methyl transferase activity of G9a assessed as inhibition of H3K9 methylation by chemiluminescence based oxygen tunneling assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497475Activity at methyl transferase activity G9a by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497477Activity at methyl transferase activity GLP by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497481Activity at methyl transferase activity SET8/preSet7 by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497474Activity at methyl transferase activity GLP by chemiluminescence based oxygen tunneling assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497480Activity at methyl transferase activity SET7/9 by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497482Activity at methyl transferase activity PRMT3 by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID497483Activity at methyl transferase activity JMJD2E by enzyme coupled S-adenocylehomocystein detection assay2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
AID618483Inhibition of G9a assessed as hydrolysis of S-adenosyl-L-homocysteine after 2 mins by SAHH-coupled fluorescence assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
AID618490Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
AID618491Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
AID1346126Human euchromatic histone lysine methyltransferase 2 (2.1.1.43 Histone methyltransferases (HMTs))2010Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (80.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.28

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

MetricThis Compound (vs All)
Research Demand Index13.28 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]