Compounds > 2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
Page last updated: 2024-12-09

2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide

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

Cross-References

ID SourceID
PubMed CID1309471
CHEMBL ID1340423
CHEBI ID121826

Synonyms (23)

Synonym
MLS001034883 ,
smr000665339
CHEBI:121826
STK815315
2-imino-10-methyl-n-[2-(morpholin-4-yl)ethyl]-5-oxo-1-(pyridin-3-ylmethyl)-1,5-dihydro-2h-dipyrido[1,2-a:2',3'-d]pyrimidine-3-carboxamide
AKOS001660984
HMS2981B05
MLS003906005
CHEMBL1340423
2-imino-5-keto-10-methyl-n-(2-morpholinoethyl)-1-(3-pyridylmethyl)dipyrido[3,4-c:1'',2''-f]pyrimidine-3-carboxamide
2-azanylidene-10-methyl-n-(2-morpholin-4-ylethyl)-5-oxidanylidene-1-(pyridin-3-ylmethyl)dipyrido[3,4-c:1'',2''-f]pyrimidine-3-carboxamide
2-imino-10-methyl-n-(2-morpholin-4-ylethyl)-5-oxo-1-(pyridin-3-ylmethyl)dipyrido[3,4-c:1'',2''-f]pyrimidine-3-carboxamide
bdbm53247
cid_1309471
2-imino-10-methyl-n-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c:1'',2''-f]pyrimidinecarboxamide
2-imino-10-methyl-n-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-1,5-dihydro-2h-dipyrido[1,2-a:2',3'-d]pyrimidine-3-carboxamide
2-imino-10-methyl-n-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c:1',2'-f]pyrimidinecarboxamide
Q27210402
Z57785291
2-imino-10-methyl-n-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-1,5-dihydro-2h-dipyrido[1,2-a:2,3-d]pyrimidine-3-carboxamide
6-imino-11-methyl-n-(2-morpholin-4-ylethyl)-2-oxo-7-(pyridin-3-ylmethyl)-1,7,9-triazatricyclo[8.4.0.03,8]tetradeca-3(8),4,9,11,13-pentaene-5-carboxamide
618410-36-9
2-imino-10-methyl-n-(2-morpholinoethyl)-5-oxo-1-(pyridin-3-ylmethyl)-2,5-dihydro-1h-dipyrido[1,2-a:2',3'-d]pyrimidine-3-carboxamide
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyridopyrimidineAny organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency25.11895.623417.292931.6228AID485281
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
glp-1 receptor, partialHomo sapiens (human)Potency3.98110.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency61.19360.100020.879379.4328AID588453; AID588456
TDP1 proteinHomo sapiens (human)Potency10.59740.000811.382244.6684AID686978; AID686979
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency3.54810.707912.194339.8107AID720542
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency112.20200.035520.977089.1251AID504332
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency16.36010.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency44.66843.548119.542744.6684AID743266
importin subunit beta-1 isoform 1Homo sapiens (human)Potency35.48135.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency35.48135.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency35.48135.804816.996225.9290AID540253
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency12.58930.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency3.08460.004611.374133.4983AID624296; AID624297
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.48131.995325.532750.1187AID624287
[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)
nuclear receptor coactivator 1 isoform 1 [Homo sapiens]Homo sapiens (human)IC50 (µMol)11.56401.15306.28039.9630AID602235
transactivating tegument protein VP16 [Human herpesvirus 1]Human alphaherpesvirus 1 (Herpes simplex virus type 1)IC50 (µMol)13.49000.94604.70169.4870AID602236
nuclear receptor coactivator 3 isoform aHomo sapiens (human)IC50 (µMol)12.71700.14764.33099.9200AID602234
[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)
POsterior SegregationCaenorhabditis elegansEC50 (µMol)300.00002.201047.1808186.6810AID1964
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC50 (µMol)87.17500.082031.0243168.9080AID1960
Zinc finger protein mex-5Caenorhabditis elegansEC50 (µMol)87.17500.082033.5679168.9080AID1960
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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
AID699027Binding affinity to HIV 1 fluorescein-labeled SL3 RNA by fluorescence spectrometry2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Identification of small molecule inhibitors of the HIV-1 nucleocapsid-stem-loop 3 RNA complex.
AID699031Binding affinity to single stranded RNA by fluorescence spectrometry2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Identification of small molecule inhibitors of the HIV-1 nucleocapsid-stem-loop 3 RNA complex.
AID699030Binding affinity to double stranded RNA by fluorescence spectrometry2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Identification of small molecule inhibitors of the HIV-1 nucleocapsid-stem-loop 3 RNA complex.
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).
[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's0 (0.00)18.2507
2000's1 (12.50)29.6817
2010's5 (62.50)24.3611
2020's2 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.17

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 Index12.17 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.17)

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
trifluoperazine
[no description available]		2.0710N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
1-amino-9,10-dioxo-4-(3-sulfamoylanilino)anthracene-2-sulfonic acid
1-amino-9,10-dioxo-4-(3-sulfamoylanilino)anthracene-2-sulfonic acid: inhibits PH domain leucine-rich repeat protein phosphatase; structure in first source		2.0710
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
HIV Coinfection
[description not available]		02.0710
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		02.0710
Plasmodium falciparum Malaria
[description not available]		02.110
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.110