Compounds > ormetoprim
Page last updated: 2024-12-06

ormetoprim

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

Description

Ormetoprim is a synthetic antibacterial agent that belongs to the dihydrofolate reductase (DHFR) inhibitor class. It is a prodrug of trimethoprim, which is an important component of the antimicrobial combination therapy trimethoprim-sulfamethoxazole. Ormetoprim undergoes enzymatic hydrolysis in the body to release trimethoprim. The compound exhibits broad-spectrum antibacterial activity against a wide range of gram-positive and gram-negative bacteria. It is effective in treating various bacterial infections, including urinary tract infections, respiratory tract infections, and skin infections. The mechanism of action of ormetoprim is based on its ability to inhibit the bacterial enzyme DHFR, which is essential for the synthesis of tetrahydrofolic acid, a vital coenzyme involved in the biosynthesis of purines and thymidylate. By inhibiting DHFR, ormetoprim disrupts the bacterial metabolism and ultimately leads to cell death. Ormetoprim is studied extensively due to its potential applications in the treatment of bacterial infections, particularly in the context of drug resistance and emerging bacterial strains. Research on ormetoprim focuses on understanding its pharmacokinetics, pharmacodynamics, and clinical efficacy in various patient populations. Additionally, studies explore the potential for ormetoprim to be used in combination therapies with other antimicrobial agents to overcome drug resistance and enhance treatment outcomes.'

ormetoprim: proposed chemotherapeutic agent; minor descriptor (75-84); on-line & Index Medicus search PYRIMIDINES (75-84) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23418
CHEMBL ID494760
CHEBI ID94553
SCHEMBL ID93810
MeSH IDM0262729

Synonyms (89)

Synonym
HMS3393K20
5-[(4,5-dimethoxy-2-methyl-phenyl)methyl]pyrimidine-2,4-diamine
6981-18-6
2,4-diamino-5-(6-methylveratryl)pyrimidine
cv564
nsc95072
ormetoprim
sd-051044
ormetorprim
nsc-95072
component of rofenaid
ro 5-9754
2, 5-[(4,5-dimethoxy-2-methylphenyl)methyl]-
pyrimidine,4-diamino-5-(6-methylveratryl)-
D05273
ormetoprim (usan/inn)
MLS001424067
smr000466374
MLS000759503
NCIOPEN2_006334
NCGC00167523-01
HMS2051K20
5-[(4,5-dimethoxy-2-methylphenyl)methyl]pyrimidine-2,4-diamine
ormethoprim
ro-5-9754
ormetroprim
CHEMBL494760
ro-59754
A836658
NCGC00167523-02
tox21_112520
dtxcid9026689
dtxsid1046689 ,
cas-6981-18-6
AKOS015917221
CCG-100900
2,4-pyrimidinediamine, 5-((4,5-dimethoxy-2-methylphenyl)methyl)-
nsc 95072
ormetoprimum [inn-latin]
ormetoprim [usan:inn]
ormetoprime [inn-french]
einecs 230-246-6
ormetoprima [inn-spanish]
m3efs94984 ,
unii-m3efs94984
pyrimidine, 2,4-diamino-5-(6-methylveratryl)-
ormetoprime
ormetoprimum
2,4-diamino-5-(4,5-dimethoxy-2-methylbenzyl)pyrimidin
ormetoprima
bdbm50413401
FT-0630358
AM20041036
5-(4,5-dimethoxy-2-methylbenzyl)-2,4-pyrimidinediamine
ormetoprim [inn]
ormetoprim [jan]
ormetoprim [usan]
ormetoprim [green book]
ormetoprim [mart.]
S5290
AB00639990-08
SCHEMBL93810
NC00150
tox21_112520_1
NCGC00167523-03
2,4-diamino-5-(4,5-dimethoxy-2-methylbenzyl) pyrimidine
KEEYRKYKLYARHO-UHFFFAOYSA-N
5-(4,5-dimethoxy-2-methyl-benzyl)-pyrimidine-2,4-diamine
W-104583
O0424
2,4-diamino-5-(4,5-dimethoxy-2-methylbenzyl)pyrimidine
5-(4,5-dimethoxy-2-methylbenzyl)-2,4-diaminopyrimidine
2,4-pyrimidinediamine, 5-[(4,5-dimethoxy-2-methylphenyl)methyl]-
CHEBI:94553
AS-71719
BCP06018
Q27166391
5-(4,5-dimethoxy-2-methylbenzyl)pyrimidine-2,4-diamine
mfcd00057747
T72844
SB60507
ormetoprim 100 microg/ml in acetonitrile
HY-121466
BO164180
CS-0082144
ormetoprima (inn-spanish)
ormetoprimum (inn-latin)
ormetoprime (inn-french)
ormetoprim (mart.)

Research Excerpts

Overview

Ormetoprim (OMP) is an antibiotic approved for use in the United States to prevent the spread of disease in freshwater aquaculture.

ExcerptReferenceRelevance
"Ormetoprim (OMP) is an antibiotic approved for use in the United States to prevent the spread of disease in freshwater aquaculture. "( Photodegradation of ormetoprim in aquaculture and stream-derived dissolved organic matter.
Chin, YP; Guerard, JJ, 2012)		2.15

Pharmacokinetics

ExcerptReferenceRelevance
"Selected pharmacokinetic parameters for sulfadimethoxine and ormetoprim, administered in a 5:1 ratio, via the oral and intraperitoneal (i."( Pharmacokinetics of sulfadimethoxine and ormetoprim in a 5:1 ratio following intraperitoneal and oral administration, in the hybrid striped bass (Morone chrysops x Morone saxitalis).
Bai, SA; Bakal, RS; Stoskopf, MK, 2004)		0.83

Bioavailability

ExcerptReferenceRelevance
" Peak absorption time of orally administered OMP was 12 h with an apparent bioavailability of 87%."( Bioavailability, disposition and pharmacokinetics of 14C-ormetoprim in rainbow trout (Salmo gairdneri).
Droy, BF; Goodrich, MS; Kleinow, KM; Lech, JJ, 1990)		0.52
" Peak plasma concentrations of 14C-SDM following oral administration of SDM/OMP were observed at 20 hr with an apparent bioavailability of 38%."( Influence of ormetoprim on the bioavailability, distribution, and pharmacokinetics of sulfadimethoxine in rainbow trout (Oncorhynchus mykiss).
Droy, BF; Kleinow, KM; Lech, JJ; Tate, T, 1989)		0.65
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

Six healthy adult mares were each given an oral loading dose of ormetoprim(OMP)-sulfadimethoxine (SDM) at a dosage of 9 mg/kg. Uptake, bioavailability, tissue disposition, and elimination of 14C were examined in rainbow trout following intravascular and per os dosing.

ExcerptRelevanceReference
" Uptake, bioavailability, tissue disposition, and elimination of 14C were examined in rainbow trout following intravascular and per os dosing of 14C-ormetoprim (8 mg/kg)."( Bioavailability, disposition and pharmacokinetics of 14C-ormetoprim in rainbow trout (Salmo gairdneri).
Droy, BF; Goodrich, MS; Kleinow, KM; Lech, JJ, 1990)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
dimethoxybenzeneAny methoxybenzene that consists of a benzene skeleton substituted with two methoxy groups and its 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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency79.43280.100020.879379.4328AID588453
GALC proteinHomo sapiens (human)Potency0.707928.183828.183828.1838AID1159614
TDP1 proteinHomo sapiens (human)Potency22.41930.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency15.72890.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency1.18830.000221.22318,912.5098AID1259243
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency20.05260.003041.611522,387.1992AID1159552; AID1159553; AID1159555
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency13.33220.001019.414170.9645AID743191
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency1.58490.009610.525035.4813AID1479145
[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)
P2X purinoceptor 3Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.01000.08260.2400AID417912
P2X purinoceptor 3Homo sapiens (human)IC50 (µMol)10.00000.00000.20301.5136AID417913
P2X purinoceptor 2Homo sapiens (human)IC50 (µMol)10.00000.00830.43452.0200AID417913
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
response to hypoxiaP2X purinoceptor 3Homo sapiens (human)
signal transductionP2X purinoceptor 3Homo sapiens (human)
neuromuscular synaptic transmissionP2X purinoceptor 3Homo sapiens (human)
response to heatP2X purinoceptor 3Homo sapiens (human)
response to coldP2X purinoceptor 3Homo sapiens (human)
response to mechanical stimulusP2X purinoceptor 3Homo sapiens (human)
response to carbohydrateP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 3Homo sapiens (human)
urinary bladder smooth muscle contractionP2X purinoceptor 3Homo sapiens (human)
peristalsisP2X purinoceptor 3Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 3Homo sapiens (human)
regulation of synaptic plasticityP2X purinoceptor 3Homo sapiens (human)
behavioral response to painP2X purinoceptor 3Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 3Homo sapiens (human)
sensory perception of tasteP2X purinoceptor 3Homo sapiens (human)
establishment of localization in cellP2X purinoceptor 3Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 3Homo sapiens (human)
protein homotrimerizationP2X purinoceptor 3Homo sapiens (human)
cellular response to ATPP2X purinoceptor 3Homo sapiens (human)
inorganic cation transmembrane transportP2X purinoceptor 3Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 3Homo sapiens (human)
response to hypoxiaP2X purinoceptor 2Homo sapiens (human)
response to ischemiaP2X purinoceptor 2Homo sapiens (human)
detection of hypoxic conditions in blood by carotid body chemoreceptor signalingP2X purinoceptor 2Homo sapiens (human)
neuromuscular synaptic transmissionP2X purinoceptor 2Homo sapiens (human)
neuromuscular junction developmentP2X purinoceptor 2Homo sapiens (human)
sensory perception of soundP2X purinoceptor 2Homo sapiens (human)
response to carbohydrateP2X purinoceptor 2Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 2Homo sapiens (human)
urinary bladder smooth muscle contractionP2X purinoceptor 2Homo sapiens (human)
peristalsisP2X purinoceptor 2Homo sapiens (human)
response to ATPP2X purinoceptor 2Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 2Homo sapiens (human)
behavioral response to painP2X purinoceptor 2Homo sapiens (human)
skeletal muscle fiber developmentP2X purinoceptor 2Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 2Homo sapiens (human)
sensory perception of tasteP2X purinoceptor 2Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 2Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
purinergic nucleotide receptor activityP2X purinoceptor 3Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 3Homo sapiens (human)
ATP bindingP2X purinoceptor 3Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 2Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 2Homo sapiens (human)
ATP bindingP2X purinoceptor 2Homo sapiens (human)
ligand-gated monoatomic ion channel activityP2X purinoceptor 2Homo sapiens (human)
identical protein bindingP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneP2X purinoceptor 3Homo sapiens (human)
axonP2X purinoceptor 3Homo sapiens (human)
Schaffer collateral - CA1 synapseP2X purinoceptor 3Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseP2X purinoceptor 3Homo sapiens (human)
postsynapseP2X purinoceptor 3Homo sapiens (human)
receptor complexP2X purinoceptor 3Homo sapiens (human)
plasma membraneP2X purinoceptor 3Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneP2X purinoceptor 2Homo sapiens (human)
apical plasma membraneP2X purinoceptor 2Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 2Homo sapiens (human)
postsynapseP2X purinoceptor 2Homo sapiens (human)
neuronal dense core vesicleP2X purinoceptor 2Homo sapiens (human)
receptor complexP2X purinoceptor 2Homo sapiens (human)
plasma membraneP2X purinoceptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID417912Antagonist activity at rat recombinant P2X3 receptor expressed in CHO cells by FLIPR assay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID417913Antagonist activity at human recombinant P2X2/3 receptor expressed in human 1321N1 cells by FLIPR assay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (19.51)18.7374
1990's10 (24.39)18.2507
2000's8 (19.51)29.6817
2010's9 (21.95)24.3611
2020's6 (14.63)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.09

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 Index33.09 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index48.20 (26.88)
Search Engine Supply Index2.41 (0.95)

This Compound (33.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (4.55%)5.53%
Reviews0 (0.00%)6.00%
Case Studies2 (4.55%)4.05%
Observational0 (0.00%)0.25%
Other40 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
amprolium
Amprolium: A veterinary coccidiostat that interferes with THIAMINE metabolism.. amprolium : An organic chloride salt having 1-[(4-amino-2-propylpyrimidin-5-yl)methyl]-2-methylpyridin-1-ium as the counterion. Used for prevention of coccidiosis in poultry and cattle.. amprolium(1+) : A pyridinium ion that is the cationic portion of amprolium, a veterinary drug which is used for prevention of coccidiosis in poultry and cattle.		2.3820pyridinium ioncoccidiostat
dinitolmide
Dinitolmide: A coccidiostat for poultry.		2.3820dinitrotoluene
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		210fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
oxolinic acid
quinolone antibiotic : An organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.		2.0310aromatic carboxylic acid;
organic heterotricyclic compound;
oxacycle;
quinolinemonocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antifungal agent;
antiinfective agent;
antimicrobial agent;
enzyme inhibitor
pyrimethamine
Maloprim: contains above 2 cpds		7.420aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sulfadimethoxine
Sulfadimethoxine: A sulfanilamide that is used as an anti-infective agent.. sulfadimethoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 2- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position.		5.72201aromatic ether;
pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
drug allergen;
environmental contaminant;
xenobiotic
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		1.9810isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfamonomethoxine
Sulfamonomethoxine: Long acting sulfonamide antibacterial agent.		3.7721benzenes;
sulfonamide
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		7.4320aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		1.97102-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.3820azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
diaveridine
diaveridine: RN given refers to parent cpd; structure. diaveridine : An aminopyrimidine in which the pyrimidine ring carries amino substituents at C-2 and C-4 and a 3,4-dimethoxybenzyl group at C-5. A folic acid antagonist, it is used as a synergist with sulfonamides against the parasitic Eimeria species.		7.4320aminopyrimidineantiparasitic agent;
drug allergen
copper sulfate
Copper Sulfate: A sulfate salt of copper. It is a potent emetic and is used as an antidote for poisoning by phosphorus. It also can be used to prevent the growth of algae.. copper(II) sulfate : A metal sulfate compound having copper(2+) as the metal ion.		2.0210metal sulfateemetic;
fertilizer;
sensitiser
thiamphenicol
[no description available]		2.0310monocarboxylic acid amide;
sulfone		antimicrobial agent;
immunosuppressive agent
halofuginone
[no description available]		2.3820quinazolines
florfenicol
florfenicol: structure given in first source. florfenicol : A carboxamide that is the N-dichloroacetyl derivative of (1R,2S)-2-amino-3-fluoro-1-[4-(methanesulfonyl)phenyl]propan-1-ol. A synthetic veterinary antibiotic that is used for treatment of bovine respiratory disease and foot rot; also used in aquaculture.		2.0310organochlorine compound;
organofluorine compound;
secondary alcohol;
secondary carboxamide;
sulfone		antimicrobial agent
monensin
Monensin: An antiprotozoal agent produced by Streptomyces cinnamonensis. It exerts its effect during the development of first-generation trophozoites into first-generation schizonts within the intestinal epithelial cells. It does not interfere with hosts' development of acquired immunity to the majority of coccidial species. Monensin is a sodium and proton selective ionophore and is widely used as such in biochemical studies.. monensin A : A spiroketal, monensin A is the major component of monensin, a mixture of antibiotic substances produced by Streptomyces cinnamonensis. An antiprotozoal, it is used as the sodium salt as a feed additive for the prevention of coccidiosis in poultry and as a growth promoter in cattle.		7.6630cyclic hemiketal;
monocarboxylic acid;
polyether antibiotic;
spiroketal		antifungal agent;
coccidiostat;
ionophore
potassium permanganate
Potassium Permanganate: Permanganic acid (HMnO4), potassium salt. A highly oxidative, water-soluble compound with purple crystals, and a sweet taste. (From McGraw-Hill Dictionary of Scientific and Technical Information, 4th ed)		2.0210
chloramine-t
chloramine-T: RN given refers to unlabeled parent cpd. chloramine T : An organic sodium salt derivative of toluene-4-sulfonamide with a chloro substituent in place of an amino hydrogen.		2.0210organic sodium saltallergen;
antifouling biocide;
disinfectant
lasalocid
Lasalocid: Cationic ionophore antibiotic obtained from Streptomyces lasaliensis that, among other effects, dissociates the calcium fluxes in muscle fibers. It is used as a coccidiostat, especially in poultry.. lasalocid : A polyether antibiotic used for prevention and treatment of coccidiosis in poultry.		6.9710beta-hydroxy ketone;
monocarboxylic acid;
monohydroxybenzoic acid;
oxanes;
oxolanes;
polyether antibiotic;
secondary alcohol;
tertiary alcohol		bacterial metabolite;
coccidiostat;
ionophore
af 353
5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source		2.0510
cellulose
DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications.		2.1510glycoside
dibutyltin dilaurate
dibutyltin dilaurate: used in prevention of parasitic dieases in cattle and sheep		2.3820
ethyl cellulose
[no description available]		2.1510glycoside
piperidines
Piperidines: A family of hexahydropyridines.		2.3820
oxytetracycline, anhydrous
Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.		2.4320
ConditionIndicatedRelationship StrengthStudiesTrials
Ache
[description not available]		02.0510
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.0510
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Flavobacteriaceae Infections
Infections with bacteria of the family FLAVOBACTERIACEAE.		02.0210
Fish Diseases
Diseases of freshwater, marine, hatchery or aquarium fish. This term includes diseases of both teleosts (true fish) and elasmobranchs (sharks, rays and skates).		02.0210
Canine Diseases
[description not available]		02.3920
Nephrotic Syndrome
A condition characterized by severe PROTEINURIA, greater than 3.5 g/day in an average adult. The substantial loss of protein in the urine results in complications such as HYPOPROTEINEMIA; generalized EDEMA; HYPERTENSION; and HYPERLIPIDEMIAS. Diseases associated with nephrotic syndrome generally cause chronic kidney dysfunction.		07.0210
Bovine Diseases
[description not available]		03.7721
Besnoitiasis
[description not available]		04.0531
Weight Gain
Increase in BODY WEIGHT over existing weight.		02.3820
Poultry Diseases
Diseases of birds which are raised as a source of meat or eggs for human consumption and are usually found in barnyards, hatcheries, etc. The concept is differentiated from BIRD DISEASES which is for diseases of birds not considered poultry and usually found in zoos, parks, and the wild.		02.3720
Fetal Death
Death of the developing young in utero. BIRTH of a dead FETUS is STILLBIRTH.		01.9710
Goiter
Enlargement of the THYROID GLAND that may increase from about 20 grams to hundreds of grams in human adults. Goiter is observed in individuals with normal thyroid function (euthyroidism), thyroid deficiency (HYPOTHYROIDISM), or hormone overproduction (HYPERTHYROIDISM). Goiter may be congenital or acquired, sporadic or endemic (GOITER, ENDEMIC).		01.9710
Swine Diseases
Diseases of domestic swine and of the wild boar of the genus Sus.		01.9710
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		01.9710
Protozoan Infections, Animal
Infections with unicellular organisms formerly members of the subkingdom Protozoa. The infections may be experimental or veterinary.		01.9610
Histomoniasis
[description not available]		01.9610
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9710
Infections, Pasteurella
[description not available]		01.9710
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		01.9710
Pneumonia
Infection of the lung often accompanied by inflammation.		06.9710
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		01.9610