Page last updated: 2024-11-09

methylthiouracil

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

Description

Methylthiouracil: A thiourea antithyroid agent that inhibits the synthesis of thyroid hormone. It is used in the treatment of hyperthyroidism. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID667493
CHEMBL ID1330588
CHEBI ID82346
SCHEMBL ID159989
SCHEMBL ID11433163
MeSH IDM0013669

Synonyms (214)

Synonym
HMS1757B09
6-methyl-2-sulfanylpyrimidin-4(3h)-one
STL352586
STL352692
nsc193526
nsc-193526
smr000059030
MLS000069452 ,
4(1h)-pyrimidinone, 2,3-dihydro-6-methyl-2-thioxo-
EU-0095998
DIVK1C_000719
KBIO1_000719
6-methyl-2-thioxo-2,3-dihydropyrimidin-4(1h)-one
6-methyl-2-sulfanylpyrimidin-4-ol
AC-907/30003038
SPECTRUM_001031
strumacil
6-methyl-2-thiouracil
thiothyron
tiomeracil
6-methyl-2-thio-2,3h)-pyrimidinedione
2-mercapto-6-methylpyrimid-4-one
thiothymin
basecil
thiomecil
thyreostat i
methicil
thyreostat
thioryl
methacil
antibason
56-04-2
muracil
methylthiouracil
MTU ,
usaf ek-6454
6-methylthiouracil
thyreonorm
tiotiron
thiomidil
basethyrin
tiorale m
2-thio-6-methyl-1,3-pyrimidin-4-one
uracil, 6-methyl-2-thio-
thimecil
2-mercapto-4-hydroxy-6-methylpyrimidine
nsc-9378
methiacil
6-thio-4-methyluracil
alkiron
orcanon
nsc9378
metacil
wln: t6mymvj bus f1
4-methyl-2-thiouracil
prostrumyl
6-methyl-2-mercaptouracil
muracin
thyril
2-thio-4-oxo-6-methyl-1,3-pyrimidine
thiuryl
2-mercapto-6-methyl-4-pyrimidone
methiocil
2-thio-6-methyluracil
2,3-dihydro-6-methyl-2-thioxo-4(1h)-pyrimidinone
PRESTWICK_330
methyl-6-thiouracil
BSPBIO_002371
NCGC00178683-01
methylthiouracil (inn)
thimecil (tn)
D07231
IDI1_000719
SPECTRUM5_001325
NCGC00091124-01
einecs 200-252-3
6-metil-tiouracile [italian]
metiltiouracilo [inn-spanish]
methacil (van)
ccris 409
methylthiouracil [inn]
4-hydroxy-2-mercapto-6-methylpyrimidine
nsc 193526
rcra waste number u164
6-methyl-2-thiouracyl [czech]
metiltiouracile [dcit]
hsdb 3366
6-methyl-4-oxo-2-thioxo1,2,3,4-tetrahydropyrimidine
2-mercapto-6-methyl-4-pyrimidinol
methylthiouracile [inn-french]
methylthiouracilum [inn-latin]
methyl thiouracil
ai3-25476
rcra waste no. u164
6-methyl-2-thio-2,4-(1h,3h)-pyrimidinedione
metacil (van)
6-methyl-2-thio-2,4-(1h3h)-pyrimidinedione
alkiron (van)
4-hydroxy-2-mercapto-6-methylpyrimidine, 95%
6-methyl-2-thioxo-1h-pyrimidin-4-one
4[1h]-pyrimidinone, 2,3-dihydro-6-methyl-thioxo
NCGC00091124-03
NCGC00091124-02
KBIO2_001511
KBIO2_004079
KBIO2_006647
KBIO3_001591
KBIOSS_001511
KBIOGR_001527
SPECTRUM2_001276
SPECTRUM4_000864
NINDS_000719
SPBIO_001272
SPECTRUM3_000676
SPECTRUM1500408
inchi=1/c5h6n2os/c1-3-2-4(8)7-5(9)6-3/h2h,1h3,(h2,6,7,8,9
uracil,6-methyl,2-thio
MLS002415706
AC-10803
HMS2091F08
4-hydroxy-6-methyl-2-thiopyrimidine
6-methyl-2-sulfanylidene-1h-pyrimidin-4-one
HMS502D21
2-mercapto-6-methylpyrimidin-4-ol
M0443
HMS1923M13
AKOS001015710
AKOS001777669
AKOS000119183
AKOS002663079
A830898
2-mercapto-6-methylpyrimidin-4(1h)-one
NCGC00091124-06
NCGC00091124-05
NCGC00091124-04
CHEMBL1330588
chebi:82346 ,
ksc-27-038
KUC108906N
metiltiouracile
6-methyl-2-thiouracyl
qw24888u5f ,
6-metil-tiouracile
methylthiouracile
unii-qw24888u5f
metiltiouracilo
methylthiouracilum
methylthiouracil [usp:inn]
C19265
NCGC00254505-01
NCGC00259419-01
tox21_300497
tox21_201870
STL163967
BBL013188
pharmakon1600-01500408
nsc757116
nsc-757116
cas-56-04-2
dtxsid2020890 ,
tox21_111088
dtxcid60890
HMS2231B20
CCG-39119
F0213-0019
FT-0621218
PS-4510
methylthiouracil [mi]
methylthiouracil [who-dd]
methylthiouracil [mart.]
methylthiouracil [iarc]
methylthiouracil [hsdb]
MLS004491793
S3138
HMS3370O12
CCG-214821
HY-B0513
6-methyl-2-sulfanylidene-1,2,3,4-tetrahydropyrimidin-4-one
4-hydroxy-6-methyl-pyrimidine-2-thiol
SCHEMBL159989
NCGC00093364-02
tox21_111088_1
SCHEMBL11433163
AKOS025117304
2-thiouracil, 6-methyl-
6-methyl-2-thio-2,4(1h,3h)-pyrimidinedione
6-methyl-2-thioxo-2,3-dihydro-4(1h)-pyrimidinone #
6-methyl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine
nsc 9378
AM87068
W-105535
STR00648
6-methyl-2-thioxo-2,3-dihydro-4(1h)-pyrimidinone
1123-10-0
OPERA_ID_172
F0827-0300
6-methyl-2-thiouracil, purum, >=98.0% s basis (elemental analysis)
mfcd00006040
sr-05000002026
SR-05000002026-1
6-methyl-2-thiouracil, vetranal(tm), analytical standard
HMS3652O03
4-hydroxy-6-methylpyrimidine-2(1h)-thione
SBI-0051446.P003
SW088218-2
BCP21374
4-hydroxy-2-mercapto-6-methyl pyrimidine
DB13644
2,3-dihydro-6-methyl-2-thioxopyrimidin-4(1h)-one
Q6824062
nsc 43815
6-methyl-2-(methylthio)-4(3h)-pyrimidinone; 6-methyl-2-(methylthio)-4-hydroxypyrimidine; 6-methyl-2-(methylthio)-4-pyrimidone; nsc 193525; nsc 37678
EN300-16769
Z56771013

Research Excerpts

Treatment

Methylthiouracil (MTU) treatment produced several-fold increases in the thyroid ODC activity and in the content of putrescine, spermidine and spermine within a week. In rats treated with MTU, inhibition of the thyroid iodothyronine production and change of the feedback mechanism function induce development of a hypertrophic goitre.

ExcerptReferenceRelevance
"Methylthiouracil treatment (100 mg/liter drinking water) effected 51% and 78% increases in synthetase activity by days 2 and 4, respectively."( Chronic regulation of rat thyroid prostaglandin synthetase activity by endogenous thyrotropin.
Burke, G; Friedman, Y; Levasseur, S, 1980
)
0.98
"Methylthiouracil (MTU) treatment produced several-fold increases in the thyroid ODC activity and in the content of putrescine, spermidine and spermine within a week."( Thyroid function and polyamines. III. Changes in ornithine decarboxylase activity and polyamine contents in the rat thyroid during hyperplasia and involution.
Hamana, K; Kakegawa, T; Matsuzaki, S; Suzuki, M, 1978
)
0.98
"In methylthiouracil-treated rats inhibition of the thyroid iodothyronine production and change of the feedback mechanism function induce development of a hypertrophic goitre in which degranulation of the mast cells accompanied by release of their bioamines induce dilatation of blood vessels and increase in the thyroid blood flow."( Circadian rhythm of the thyroid mast cells in untreated and methylthiouracil-treated rats.
Mödlinger, G, 1989
)
1.03

Toxicity

ExcerptReferenceRelevance
" While pharmacodynamically caused therapy effects are generally to be avoided, when considering the pathophysiology of the regulation of the thyroid gland, this is not the case as to allergic side effects and only to a limited extent with regard to toxic side effects."( [Thyrostatic therapy of hyperthyroidism with special reference to drug side effects].
Heberling, HJ; Lohmann, D, 1983
)
0.27

Bioavailability

ExcerptReferenceRelevance
"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

ExcerptRelevanceReference
" Content of sialic acids in blood plasma and liver tissue was shown to depend on dosage and length of administration of various thyrostatic preparations."( [Effect of thyroid inhibitors and thyroidectomy on sialic acid content of rat blood and liver].
Kuz'mak, NI,
)
0.13
" So 1-thyroxine, depending on the dosage used, may stimulate the development of tumor process in mammary glands, but exert no influence on it (an effect of "the effect extinction"), and finely suppress tumor development."( [The influence of thyroid and antithyroid preparations on the development of induced breast cancer].
Beskrovnyĭ, AM; Sukacheva, OA, 1976
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrimidoneA pyrimidine carrying one or more oxo substituents.
[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 (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.81140.140911.194039.8107AID2451
phosphopantetheinyl transferaseBacillus subtilisPotency55.52780.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency0.28180.031637.5844354.8130AID743255
AR proteinHomo sapiens (human)Potency20.14730.000221.22318,912.5098AID743036; AID743040; AID743042; AID743053; AID743054
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency23.19880.000214.376460.0339AID720691; AID720719
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency69.00830.001530.607315,848.9004AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency14.20470.000229.305416,493.5996AID743075; AID743079
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency50.11870.001024.504861.6448AID588535
IDH1Homo sapiens (human)Potency20.59620.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency25.11890.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.71010.001723.839378.1014AID743083
heat shock protein beta-1Homo sapiens (human)Potency37.57510.042027.378961.6448AID743210
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency74.97800.000627.21521,122.0200AID651741
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency6.30960.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency6.30960.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency6.30960.15855.287912.5893AID540303
survival motor neuron protein isoform dHomo sapiens (human)Potency0.35480.125912.234435.4813AID1458
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (70)

Assay IDTitleYearJournalArticle
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID566702Inhibition of human recombinant MMP1 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID566700Inhibition of human recombinant 5-lipoxygenase at 1 mM after 10 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566703Inhibition of human recombinant MMP2 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566706Inhibition of human recombinant MMP9 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566704Inhibition of human recombinant MMP3 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566705Inhibition of human recombinant MMP8 at 1 mM after 30 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID566699Inhibition of mushroom tyrosinase at 1 mM after 10 mins2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
AID566701Inhibition of recombinant anthrax lethal factor at 1 mM after 30 mins by fluorescence assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (831)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990764 (91.94)18.7374
1990's23 (2.77)18.2507
2000's9 (1.08)29.6817
2010's27 (3.25)24.3611
2020's8 (0.96)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.44

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 Index31.44 (24.57)
Research Supply Index6.91 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index47.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (0.71%)5.53%
Reviews16 (1.61%)6.00%
Case Studies7 (0.71%)4.05%
Observational0 (0.00%)0.25%
Other961 (96.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]