Compounds > c 1303
Page last updated: 2024-12-07

c 1303

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

Description

C 1303: DNa-binding drug; structure given indicates that the cpd should be the dimethylamino cpd, but it is named as the diethylamino cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID124496
CHEMBL ID95704
MeSH IDM0214056

Synonyms (17)

Synonym
smr001565158
CHEMBL95704
NCI60_015716
nsc645827
5-(2-(dimethylamino)ethylamino)-8-hydroxy-6h-[1,3]triazolo[4,5,1-de]acridin-6-one
nsc-645827
mls002701557 ,
6h-(1,2,3)triazolo(4,5,1-de)acridin-6-one, 5-((2-(dimethylamino)ethyl)amino)-8-hydroxy-
5-(2-(diethylamino)ethylamino)-8-hydroxy-6h-(1,2,3)triazolo(4,5-1-de)acridin-6-one
128113-19-9
c-1303 ,
c 1303
DTXSID30155810
5VNA4LC5RU
5-[[2-(dimethylamino)ethyl]amino]-8-hydroxy-6h-[1,2,3]triazolo[4,5,1-de]acridin-6-one
6h-[1,2,3]triazolo[4,5,1-de]acridin-6-one, 5-[[2-(dimethylamino)ethyl]amino]-8-hydroxy-
10-(2-(dimethylamino)ethylamino)-5-oxidanyl-1,14,15-triazatetracyclo(7.6.1.02,7.013,16)hexadeca-2,4,6,9(16),10,12,14-heptaen-8-one
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency7.94330.01846.806014.1254AID624417
TDP1 proteinHomo sapiens (human)Potency0.18360.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency15.84890.00527.809829.0929AID588855
67.9K proteinVaccinia virusPotency1.45020.00018.4406100.0000AID720579; AID720580
IDH1Homo sapiens (human)Potency23.10930.005210.865235.4813AID686970
flap endonuclease 1Homo sapiens (human)Potency10.54070.133725.412989.1251AID588795; AID720498
eyes absent homolog 2 isoform aHomo sapiens (human)Potency1.69471.199814.641950.1187AID720540
DNA polymerase eta isoform 1Homo sapiens (human)Potency14.12540.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency35.48130.025911.239831.6228AID602313
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.94331.995325.532750.1187AID624287
C-terminal-binding protein 1Homo sapiens (human)Potency1.19980.30149.321019.0148AID720541
[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)
rac GTPase-activating protein 1 isoform aHomo sapiens (human)IC50 (µMol)62.56007.390057.8904301.2400AID624330
NADHomo sapiens (human)IC50 (µMol)0.70000.00260.80763.4000AID277029
[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)
Microphthalmia-associated transcription factorHomo sapiens (human)AC5015.06030.015010.904946.0480AID493073; AID493102; AID493177; AID540346
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (53)

Processvia Protein(s)Taxonomy
protein polyubiquitinationNADHomo sapiens (human)
response to ischemiaNADHomo sapiens (human)
NADH oxidationNADHomo sapiens (human)
ubiquinone metabolic processNADHomo sapiens (human)
xenobiotic metabolic processNADHomo sapiens (human)
nitric oxide biosynthetic processNADHomo sapiens (human)
response to oxidative stressNADHomo sapiens (human)
synaptic transmission, cholinergicNADHomo sapiens (human)
response to nutrientNADHomo sapiens (human)
response to toxic substanceNADHomo sapiens (human)
response to hormoneNADHomo sapiens (human)
response to carbohydrateNADHomo sapiens (human)
response to amineNADHomo sapiens (human)
removal of superoxide radicalsNADHomo sapiens (human)
protein catabolic processNADHomo sapiens (human)
response to estradiolNADHomo sapiens (human)
response to lipopolysaccharideNADHomo sapiens (human)
response to testosteroneNADHomo sapiens (human)
cellular response to oxidative stressNADHomo sapiens (human)
negative regulation of protein catabolic processNADHomo sapiens (human)
vitamin E metabolic processNADHomo sapiens (human)
vitamin K metabolic processNADHomo sapiens (human)
negative regulation of apoptotic processNADHomo sapiens (human)
response to alkaloidNADHomo sapiens (human)
positive regulation of neuron apoptotic processNADHomo sapiens (human)
innate immune responseNADHomo sapiens (human)
cell redox homeostasisNADHomo sapiens (human)
response to ethanolNADHomo sapiens (human)
response to electrical stimulusNADHomo sapiens (human)
cellular response to hydrogen peroxideNADHomo sapiens (human)
NADPH oxidationNADHomo sapiens (human)
cellular response to metal ionNADHomo sapiens (human)
negative regulation of ferroptosisNADHomo sapiens (human)
response to tetrachloromethaneNADHomo sapiens (human)
response to L-glutamineNADHomo sapiens (human)
response to hydrogen sulfideNADHomo sapiens (human)
response to flavonoidNADHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIC-terminal-binding protein 1Homo sapiens (human)
protein phosphorylationC-terminal-binding protein 1Homo sapiens (human)
negative regulation of cell population proliferationC-terminal-binding protein 1Homo sapiens (human)
viral genome replicationC-terminal-binding protein 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionC-terminal-binding protein 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionC-terminal-binding protein 1Homo sapiens (human)
synaptic vesicle endocytosisC-terminal-binding protein 1Homo sapiens (human)
white fat cell differentiationC-terminal-binding protein 1Homo sapiens (human)
regulation of cell cycleC-terminal-binding protein 1Homo sapiens (human)
synaptic vesicle clusteringC-terminal-binding protein 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIC-terminal-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
RNA bindingNADHomo sapiens (human)
cytochrome-b5 reductase activity, acting on NAD(P)HNADHomo sapiens (human)
superoxide dismutase activityNADHomo sapiens (human)
protein bindingNADHomo sapiens (human)
NADPH dehydrogenase (quinone) activityNADHomo sapiens (human)
identical protein bindingNADHomo sapiens (human)
NADH:ubiquinone reductase (non-electrogenic) activityNADHomo sapiens (human)
NAD(P)H dehydrogenase (quinone) activityNADHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
transcription corepressor bindingC-terminal-binding protein 1Homo sapiens (human)
chromatin bindingC-terminal-binding protein 1Homo sapiens (human)
transcription corepressor activityC-terminal-binding protein 1Homo sapiens (human)
protein bindingC-terminal-binding protein 1Homo sapiens (human)
oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptorC-terminal-binding protein 1Homo sapiens (human)
protein domain specific bindingC-terminal-binding protein 1Homo sapiens (human)
identical protein bindingC-terminal-binding protein 1Homo sapiens (human)
NAD bindingC-terminal-binding protein 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingC-terminal-binding protein 1Homo sapiens (human)
DNA-binding transcription factor bindingC-terminal-binding protein 1Homo sapiens (human)
transcription coactivator activityC-terminal-binding protein 1Homo sapiens (human)
transcription coregulator bindingC-terminal-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
nucleusNADHomo sapiens (human)
cytoplasmNADHomo sapiens (human)
cytosolNADHomo sapiens (human)
dendriteNADHomo sapiens (human)
neuronal cell bodyNADHomo sapiens (human)
synapseNADHomo sapiens (human)
cytosolNADHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
nucleusC-terminal-binding protein 1Homo sapiens (human)
nucleoplasmC-terminal-binding protein 1Homo sapiens (human)
presynaptic active zone cytoplasmic componentC-terminal-binding protein 1Homo sapiens (human)
glutamatergic synapseC-terminal-binding protein 1Homo sapiens (human)
GABA-ergic synapseC-terminal-binding protein 1Homo sapiens (human)
transcription repressor complexC-terminal-binding protein 1Homo sapiens (human)
nucleusC-terminal-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745850Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1745849Viability Counterscreen for CMV-Luciferase Assay of 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.
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.
AID1745847CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1745848Confirmatory qHTS for Inhibitors of ATXN expression
AID153634In vivo antileukemic activity against P388 leukemia at dose 25 mp/kg administered intraperitoneally (30 days survivors, 3/6)1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity.
AID1096392Binding affinity to Bos taurus (calf) thymus DNA assessed as change in melting temperature at drug to DNA base pair ratio 0.25 M2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8
Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies.
AID87734In vitro cytotoxicity against HeLa S3 cell lines1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity.
AID277029Inhibition of human recombinant NQO12006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
In silico identification and biochemical characterization of novel inhibitors of NQO1.
AID1096393Antitumor activity against Mus musculus (mouse) P388 cells xenografted in Mus musculus (mouse) assessed as increase in survival time relative to control2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8
Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (25.00)18.2507
2000's2 (25.00)29.6817
2010's3 (37.50)24.3611
2020's1 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.45

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 Index32.45 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index36.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.45)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ametantrone
ametantrone: RN given refers to parent cpd; structure		1.9710
acridines
Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.		1.9810acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene		genotoxin
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		1.98101,2,3-triazole
c 1311
C 1311: an imidazoacridinone; arrests cell-cycle progression in the G2 phase of L1210 cells; structure given in first source		2.0610
c 1310
C 1310: an imidazoacridinone; arrests cell-cycle progression in the G2 phase of L1210 cells; structure given in first source		2.0610
nsc 366140
NSC 366140: a 9-methoxypyrazoloacridine; structure given in first source		2.0310
bisantrene
[no description available]		2.0310
dicumarol
Dicumarol: An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases.		2.0310hydroxycoumarinanticoagulant;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
Hsp90 inhibitor;
vitamin K antagonist
ConditionIndicatedRelationship StrengthStudiesTrials
Innate Inflammatory Response
[description not available]		02.0510
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.0510