Page last updated: 2024-12-08

2-guanidine-4-methylquinazoline

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

Description

2-guanidine-4-methylquinazoline: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID345657
CHEMBL ID602365
SCHEMBL ID2330055
MeSH IDM0276487

Synonyms (46)

Synonym
EN300-14418
bdbm50335552
HMS2638L21
n-(4-methylquinazolin-2-yl)guanidine
smr000280403
MLS000710636
TIMTEC1_000349
nsc-403387
716-11-0
nsc403387
1-(4-methylquinazolin-2-yl)guanidine
STK063157
HMS1534P19
AKOS000270579
BRD-K94348506-001-01-2
CHEMBL602365 ,
gnf-pf-3515 ,
2-(4-methylquinazolin-2-yl)guanidine
amino(4-methylquinazolin-2-yl)carboxamidine
bdbm93094
2-guanidino-4-methylguinazoline
SS-4549
gtpl4203
2-guanidine-4-methylquinazoline
HMS3364G12
gmq ,
2-gmq
AB00075950-01
SCHEMBL2330055
n-(4-methyl-2-quinazolinyl)guanidine
ONQKSKDLYYDFLL-UHFFFAOYSA-N
cambridge id 5228468
sr-01000493239
SR-01000493239-1
DTXSID20323223
mfcd00023908
Z56754371
AKOS030240850
1-[(2e)-4-methylquinazolin-2(1h)-ylidene]guanidine
STL514058
n-(4-methyl-2-quinazolinyl)-guanidine
CS-0182121
Q27077823
2-(4-methylquinazolin-2-yl)guanidine.
AKOS037491725
A917905

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
WRNHomo sapiens (human)Potency25.11890.168331.2583100.0000AID651768
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency12.43470.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency14.47470.00527.809829.0929AID588855; AID720534
flap endonuclease 1Homo sapiens (human)Potency63.59380.133725.412989.1251AID588795; AID720498
[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)
MyeloperoxidaseHomo sapiens (human)IC50 (µMol)0.90000.02001.88117.6800AID1446226
Trypanothione reductaseTrypanosoma cruziIC50 (µMol)100.00005.80005.80005.8000AID562116
[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)
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC5013.69000.150012.066235.2100AID652116
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
response to yeastMyeloperoxidaseHomo sapiens (human)
hypochlorous acid biosynthetic processMyeloperoxidaseHomo sapiens (human)
respiratory burst involved in defense responseMyeloperoxidaseHomo sapiens (human)
defense responseMyeloperoxidaseHomo sapiens (human)
response to oxidative stressMyeloperoxidaseHomo sapiens (human)
response to mechanical stimulusMyeloperoxidaseHomo sapiens (human)
removal of superoxide radicalsMyeloperoxidaseHomo sapiens (human)
response to foodMyeloperoxidaseHomo sapiens (human)
response to lipopolysaccharideMyeloperoxidaseHomo sapiens (human)
low-density lipoprotein particle remodelingMyeloperoxidaseHomo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
negative regulation of apoptotic processMyeloperoxidaseHomo sapiens (human)
defense response to fungusMyeloperoxidaseHomo sapiens (human)
response to gold nanoparticleMyeloperoxidaseHomo sapiens (human)
defense response to bacteriumMyeloperoxidaseHomo sapiens (human)
proteolysisComplement C1s subcomponentHomo sapiens (human)
complement activation, classical pathwayComplement C1s subcomponentHomo sapiens (human)
innate immune responseComplement C1s subcomponentHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
chromatin bindingMyeloperoxidaseHomo sapiens (human)
peroxidase activityMyeloperoxidaseHomo sapiens (human)
protein bindingMyeloperoxidaseHomo sapiens (human)
heparin bindingMyeloperoxidaseHomo sapiens (human)
heme bindingMyeloperoxidaseHomo sapiens (human)
metal ion bindingMyeloperoxidaseHomo sapiens (human)
serine-type endopeptidase activityComplement C1s subcomponentHomo sapiens (human)
calcium ion bindingComplement C1s subcomponentHomo sapiens (human)
protein bindingComplement C1s subcomponentHomo sapiens (human)
identical protein bindingComplement C1s subcomponentHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
extracellular regionMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
nucleusMyeloperoxidaseHomo sapiens (human)
nucleoplasmMyeloperoxidaseHomo sapiens (human)
lysosomeMyeloperoxidaseHomo sapiens (human)
secretory granuleMyeloperoxidaseHomo sapiens (human)
azurophil granule lumenMyeloperoxidaseHomo sapiens (human)
azurophil granuleMyeloperoxidaseHomo sapiens (human)
intracellular membrane-bounded organelleMyeloperoxidaseHomo sapiens (human)
extracellular exosomeMyeloperoxidaseHomo sapiens (human)
phagocytic vesicle lumenMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
extracellular regionComplement C1s subcomponentHomo sapiens (human)
blood microparticleComplement C1s subcomponentHomo sapiens (human)
extracellular spaceComplement C1s subcomponentHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID602118NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence.2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID558399Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID562116Inhibition of Trypanosoma cruzi X10/1 trypanothione reductase assessed as inhibition of thionitrobenzoate formation by microplate reader analysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID1917342Induction of read through activity at T-p53 R213X mutant premature termination codon in human HDQ-P1 cells assessed as increase in production of full length p53 protein by MSD assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Guanidino quinazolines and pyrimidines promote readthrough of premature termination codons in cells with native nonsense mutations.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID562113Antiprotozoal activity against Leishmania donovani MHOM/ET/67/L82 amastigotes2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID558400Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID1446226Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID562115Antiplasmodial activity against Plasmodium falciparum 3D7 erythrocytic stage2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID558402Cytotoxicity against rat L6 cells2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID1799881Enzymatic Assay from Article 10.1021/bi00839a042: \\Nature of the active site of a subunit of the first component of human complement.\\1969Biochemistry, Nov, Volume: 8, Issue:11
Nature of the active site of a subunit of the first component of human complement.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (3.57)18.7374
1990's0 (0.00)18.2507
2000's3 (10.71)29.6817
2010's20 (71.43)24.3611
2020's4 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.21

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 Index11.21 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other29 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]