Page last updated: 2024-11-04

urethane

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Cross-References

ID SourceID
PubMed CID5641
CHEMBL ID462547
CHEBI ID17967
MeSH IDM0022330

Synonyms (139)

Synonym
BIDD:ER0508
CHEBI:17967 ,
KBIO1_000060
DIVK1C_000060
inchi=1/c3h7no2/c1-2-6-3(4)5/h2h2,1h3,(h2,4,5
SPECTRUM_001685
BSPBIO_002569
SPECTRUM5_001651
carbamic acid, ethyl ester
ethylurethane
rcra waste no. u238
urethane [inn:ban:dcf]
rcra waste number u238
ethylurethan
o-ethyl carbamate
uretano [dcit]
aethylcarbamat [german]
carbamidsaeure-aethylester [german]
einecs 200-123-1
o-ethylurethane
hsdb 2555
ethylester kyseliny karbaminove [czech]
uretan etylowy [polish]
ethyl ester of carbamic acid
ccris 619
ai3-00553
aethylurethan [german]
urethanum [inn-latin]
ethyl urethan
51-79-6
nsc-746
a 11032
x 41
leucothane
aethylurethan
carbamic acid ethyl ester
nsc 746
urethane ,
ethyl urethane
pracarbamine
C01537
o-ethyl urethane
estane 5703
pracarbamin
aethylcarbamat
urethan ,
u-compound
uretan
carbamidsaeure-aethylester
leucethane
wln: zvo2
nsc746
ethyl carbamate
ethylcarbamate
urethane, >=99%
DB04827
NCGC00095041-02
NCGC00095041-03
NCGC00095041-01
KBIO3_001789
KBIO2_004733
KBIO2_007301
KBIOGR_001464
KBIO2_002165
KBIOSS_002165
SPECTRUM3_000965
SPECTRUM4_001082
SPBIO_000758
SPECTRUM2_000909
NINDS_000060
SPECTRUM1503304
urethane + ethanol (combination)
IDI1_000060
NCGC00095041-04
carbamate, ethyl
urethane, >=99.0% (gc)
HMS2093C21
AKOS000118772
HMS500C22
CHEMBL462547
HMS1922A10
NCGC00095041-05
NCGC00095041-06
uretano
urethane [inn:dcf]
3in71e75z5 ,
unii-3in71e75z5
uretan etylowy
ethylester kyseliny karbaminove
urethanum
tox21_300494
tox21_201761
NCGC00259310-01
NCGC00254522-01
nsc-758452
pharmakon1600-01503304
nsc758452
dtxsid9021427 ,
dtxcid301427
tox21_111398
STL257390
cas-51-79-6
S4544
CCG-39905
FT-0675741
FT-0626365
AM20100253
BRD-K24297741-001-01-1
urethane [inn]
ethyl carbamate [iarc]
ethyl aminoformate
urethan [mi]
urethane [hsdb]
urethane [who-dd]
ethyl-carbamate
NCGC00095041-08
tox21_111398_1
CS-4731
nh2cooc2h5
HY-B1207
AB00052344_04
mfcd00007966
F0001-1333
urethane, analytical standard
sr-05000001854
SR-05000001854-1
SR-05000001854-2
ethyl carbamate (urethane)
SBI-0051812.P002
SBI-0051812.P003
urethane, inn
aethylurethan (german)
aethylcarbamat (german)
Z33546369
Q422884
F21294
HMS3885F08
ethyl carbamate;carbamic acid ethyl ester;ethylurethane
EN300-15607

Research Excerpts

Overview

Urethane is a chemical carcinogen found in tobacco smoke that causes activating mutations in Kras and induces lung tumors in mice. It is a common and often preferred anesthetic agent for urodynamic recordings in rats.

ExcerptReferenceRelevance
"Urethane (URE) is a known promutagen."( Betulinic acid modulates urethane-induced genotoxicity and mutagenicity in mice and Drosophila melanogaster.
Alves, BS; Constante, SAR; Cunha, WR; da Silva, LHD; de Morais, CR; de Oliveira, LTS; Esperandim, TR; Ferreira, NH; Naves, MPC; Oliveira, VC; Orsolin, PC; Rinaldi Neto, F; Spanó, MA; Tavares, DC, 2020
)
1.58
"Urethane is a recognized genotoxic carcinogen in fermented foods and beverages. "( Lasting glycolytic stress governs susceptibility to urethane-induced lung carcinogenesis in vivo and in vitro.
Cao, N; Deng, J; Du, G; Duan, Y; Geng, S; Guo, Z; Lin, H; Ma, X; Meng, M; Zheng, Y, 2016
)
2.13
"Urethane is a widely used anesthetic in animal lower urinary tract research. "( Urethane anesthesia in acute lower urinary tract studies in the male rat.
Choudhary, M; Clavica, F; van Asselt, E; van Mastrigt, R, 2017
)
3.34
"Urethane is a chemical carcinogen found in tobacco smoke that causes activating mutations in Kras and induces lung tumors in mice."( Overexpression of Sprouty 2 in mouse lung epithelium inhibits urethane-induced tumorigenesis.
Miller, YE; Minowada, G, 2009
)
1.31
"Urethane is a common and often preferred anesthetic agent for urodynamic recordings in rats, but its use is often restricted to terminal procedures because of a prolonged duration of action and potentially toxic effects. "( Differential effects of urethane and isoflurane on external urethral sphincter electromyography and cystometry in rats.
Chang, HY; Havton, LA, 2008
)
2.1
"Urethane is a chemical carcinogen which causes lung tumorigenesis in mice with similarities to human adenocarcinoma (AC). "( Lung tumor development in the presence of sphingosine 1-phosphate agonist FTY720.
Bueno, V; Lopes, CT; Oshima, CT; Palma, PV; Salinas, NR, 2009
)
1.8
"Urethane is a widely used anesthetic for animal experiments. "( Urethane suppresses hippocampal CA1 neuron excitability via changes in presynaptic glutamate release and in potassium channel activity.
Lei, T; Tian, Y; Yang, Z; Zhang, T, 2012
)
3.26
"Urethane is a carcinogen to which there is widespread exposure through the consumption of fermented foods and alcoholic beverages. "( Effect of ethanol on the tumorigenicity of urethane (ethyl carbamate) in B6C3F1 mice.
Beland, FA; Benson, RW; Doerge, DR; Fang, JL; Kovatch, RM; Mellick, PW; Roberts, DW, 2005
)
2.03
"Urethane is a multi-site animal carcinogen and was classified as "reasonably anticipated to be a human carcinogen." Urethane is a fermentation by-product and found at appreciable levels in alcoholic beverages and foods such as bread and cheese. "( Inhibition of urethane-induced genotoxicity and cell proliferation in CYP2E1-null mice.
Dixon, D; Ghanayem, BI; Hoffler, U; Peddada, S, 2005
)
2.13
"Urethane is a fermentation by-product and a potent animal carcinogen. "( Increased bioaccumulation of urethane in CYP2E1-/- versus CYP2E1+/+ mice.
Ghanayem, BI; Hoffler, U, 2005
)
2.06
"Urethane is an established animal carcinogen and has been classified as "reasonably anticipated to be a human carcinogen." Until recently, urethane metabolism via esterase was considered the main metabolic pathway of this chemical. "( Inhibition of urethane-induced carcinogenicity in cyp2e1-/- in comparison to cyp2e1+/+ mice.
Ghanayem, BI, 2007
)
2.14
"Urethane is a standard anesthetic utilized for in vivo recordings in the hippocampus. "( Field potential recordings in dentate gyrus of anesthetized rats: stability of baseline.
Gilbert, ME; Mack, CM, 1999
)
1.75
"Urethane is a strong clastogen in mice when administered either intraperitoneally or orally and the micronucleus test applied to adult and fetal erythroblasts is a convenient method of choice for studying the acute and subchronic clastogenicity of this carcinogen, its transplacental effects as well as the influence of modifying factors on these processes."( Clastogenic activity of urethane in mice.
Balansky, R; Blagoeva, P; Mircheva, Z, 1992
)
1.31
"Urethane is a good clastogen in mammalian somatic cells in vivo, but it shows variable results with cells in vitro."( Mutagenicity, metabolism, and DNA interactions of urethane.
Collins, TF; Sotomayor, RE, 1990
)
1.25
"Urethane is a widely used anesthetic and yohimbine is a well-known alpha 2-adrenergic antagonist. "( Effect of yohimbine on urethane-induced hyperglycemia in rats.
Aisaka, K; Ishihara, T; Kihara, T; Koike, M; Kuroki, M, 1989
)
2.03
"Urethane is an anesthetic which is commonly used in neurophysiological studies because it is presumed to have minimal effects upon neuronal activity. "( Urethane affects the rat visual system at subanesthetic doses.
Dyer, RS; Rigdon, GC, 1987
)
3.16

Effects

Thio-urethane oligomers have been shown to reduce stress and increase toughness in highly filled composite materials. Urethane has no effect to promote multiplication of the cells it has rendered neoplastic.

ExcerptReferenceRelevance
"Urethane has a suppressive effect on COX and iNOS RNA message in the lung and for this reason it should be avoided as an anesthetic when lung inflammatory processes are experimentally evaluated in the rat."( Urethane suppresses rat lung inducible cyclooxygenase and nitric oxide synthase mRNA levels.
Amankwah, EK; Belik, J; Harabor, A; Hart, DA; Martinez, FE, 2000
)
3.19
"Thiourethane oligomers have been shown to increase the fracture toughness and reduce the polymerization stress of methacrylate-based materials. "( Effect of the addition of thiourethane oligomers on the sol⿿gel composition of BisGMA/TEGDMA polymer networks.
Barcelos, LM; Borges, MG; Fugolin, APP; Huynh, V; Lewis, SH; Menezes, MS; Navarro, O; Pfeifer, CS; Soares, CJ, 2019
)
1.36
"Thio-urethane oligomers have been shown to reduce stress and increase toughness in highly filled composite materials. "( Rheological and mechanical properties and interfacial stress development of composite cements modified with thio-urethane oligomers.
Bacchi, A; Pfeifer, CS, 2016
)
1.16
"Urethane has no effect to promote multiplication of the cells it has rendered neoplastic, its whole role being to initiate neoplastic change."( Age of the host and other factors affecting the production with urethane of pulmonary adenomas in mice.
ROGERS, S, 1951
)
1.19
"Urethane has been known for its transplacental carcinogenic effect in mice. "( Organ-specific susceptibility to clastogenic effect of urethane, a trial of application of whole embryo culture to testing system for clastogen.
Itoh, A; Matsumoto, N, 1984
)
1.96
"Urethane has a suppressive effect on COX and iNOS RNA message in the lung and for this reason it should be avoided as an anesthetic when lung inflammatory processes are experimentally evaluated in the rat."( Urethane suppresses rat lung inducible cyclooxygenase and nitric oxide synthase mRNA levels.
Amankwah, EK; Belik, J; Harabor, A; Hart, DA; Martinez, FE, 2000
)
3.19

Actions

Urethane induced an increase of micronucleated PCE (MN PCE) frequency from 0.19% in the control to 8.63% at 24 h. Urethane was found to inhibit development of spontaneous mechanical activity.

ExcerptReferenceRelevance
"Urethane induced an increase of micronucleated PCE (MN PCE) frequency from 0.19% in the control to 8.63% at 24 h, followed by a decrease to 6.98% at 48 h."( Co-administration of ethanol transiently inhibits urethane genotoxicity as detected by a kinetic study of micronuclei induction in mice.
Choy, WN; Mandakas, G; Paradisin, W, 1996
)
1.27
"2 Urethane was found to inhibit development of spontaneous mechanical activity."( Urethane and contraction of vascular smooth muscle.
Altura, BM; Weinberg, J, 1979
)
2.26
"Urethane produced an increase in pulmonary tumor response in this study in agreement with previous investigations."( Pulmonary adenomas in A/J mice treated with silica.
Chrisp, CE; Fisher, GL; McNeill, DA, 1990
)
1

Treatment

Urethane treatment caused down-regulated expression of numerous genes involved in cell-cycle control. Urethane is the best treatment available for multiple myeloma.

ExcerptReferenceRelevance
"Urethane treatment induced 5 hyperplasias, 41 adenomas and 12 adenocarcinomas in the lungs of 8 A/J mice. "( SPECT/CT of lung nodules using 111In-DOTA-c(RGDfK) in a mouse lung carcinogenesis model.
Fujii, H; Hayakawa, T; Imai, T; Mutoh, M; Tsuta, K; Yanaka, A; Yoshimoto, M, 2013
)
1.83
"Urethane-treated animals showed 2.0+2.0 and 4.0+3.0 nodules respectively, in the filtered and non-filtered chambers (p = 0.02), thus showing experimental evidence of increased carcinogenic-induced lung cancer with increasing PM2.5 exposure."( Urban, traffic- related particles and lung tumors in urethane treated mice.
Assunção, JV; Lemos, M; Mauad, T; Pereira, FA; Saldiva, PH, 2011
)
1.34
"Urethane treatment caused down-regulated expression of numerous genes involved in cell-cycle control, while maternal immune stimulation caused comparative up-regulation of many of these genes."( Immune stimulation in urethane-exposed pregnant mice increases expression level of spleen leukocyte genes for TGFbeta3 GM-CSF and other cytokines that may play a role in reduced chemical-induced birth defects.
Chrisman, MV; Gogal, RM; Holladay, SD; Sharov, AA; Sharova, LV, 2002
)
1.35
"Urethane treatment also shifted placental cytokine gene expression toward a T cell helper 1 (Th1) profile, while immunostimulation tended to restore a Th2 profile that may be more beneficial to pregnancy and fetal development."( Maternal immune stimulation reduces both placental morphologic damage and down-regulated placental growth-factor and cell cycle gene expression caused by urethane: are these events related to reduced teratogenesis?
Gogal, RM; Holladay, SD; Sharov, AA; Sharova, LV; Smith, BJ; Sura, P, 2003
)
1.24
"Urethane is the best treatment available for multiple myeloma."( New therapy for leukemia, polycythemia, and lymphoma.
BARTLETT, GR; MARLOW, AA, 1953
)
0.95
"In urethane-treated mice, anti-inflammatory drugs increased the tumor incidence in AIRmax but not AIRmin mice, and an inverse correlation (P<.001) between the degree of acute inflammatory response (AIR) and lung tumorigenesis was found in an F2 (AIRmax x AIRmin) intercross population."( Genetic selection for high acute inflammatory response confers resistance to lung carcinogenesis in the mouse.
Cabrera, WH; De Franco, M; de Souza, VR; Di Pace, RF; Ibañez, OM; Maria, DA; Massa, S; Ribeiro, OG; Semen, M; Starobinas, N,
)
0.65
"Urethane/chloralose-treated mice demonstrated hypoglycaemia and enhanced serum levels of ALT and creatinine in response to LPS, but failed to show LPS-induced increases in serum lipase and lung MPO activity."( Comparison of urethane/chloralose and pentobarbitone anaesthesia for examining effects of bacterial lipopolysaccharide in mice.
Furman, BL; Kazerani, HR, 2006
)
1.42
"Urethane-treated mice revealed increased levels of MDA (62%) and catalase (70.7%) in blood-serum and in lung tissue (36.5%) as compared with control."( [Melatonin inhibits urethane-induced carcinogenesis tumors in murine lung].
Anisimov, VN; Plotnikova, NA; Semenchenko, AV; Vesnushkin, GM, 2006
)
1.38
"The urethane-treated MAK-4, MAK-5 and MAK4+5-fed mice had significantly higher activities of liver cytosolic enzymes compared to the urethane-treated controls and to untreated mice: GPX(0.23 +/- 0.08, 0.21 +/- 0.05, 0.25 +/- 0.04, 0.20 +/- 0.05, 0.21 +/- 0.03 U/mg protein, respectively), GST (2.0 +/- 0.4, 2.0 +/- 0.6, 2.1 +/- 0.3, 1.7 +/- 0.2, 1.7 +/- 0.2 U/mg protein, respectively) and QR (0.13 +/- 0.02, 0.12 +/- 0.06, 0.15 +/- 0.03, 0.1 +/- 0.04, 0.11 +/- 0.03 U/mg protein, respectively)."( MAK-4 and -5 supplemented diet inhibits liver carcinogenesis in mice.
Di Lorenzo, D; Hsiao, WL; Jeremic, M; Marra, M; Mazzoleni, G; Montani, C; Penza, M; Sharma, H, 2007
)
0.82
"Urethane treatment accelerated number and size of lung tumors developing in SOPten(flox/flox) mice of both ages."( Pten controls lung morphogenesis, bronchioalveolar stem cells, and onset of lung adenocarcinomas in mice.
Hamada, K; Horie, Y; Kawahara, K; Kishimoto, H; Kubo, H; Mak, TW; Nakano, T; Nakazato, M; Nishio, M; Sasaki, M; Sasaki, T; Suzuki, A; Whitsett, JA; Yajima, N; Yanagi, S, 2007
)
1.06
"Urethane, treated in a similar way, induced somatic mutations and malformations in the offspring."( A method to detect tumors and presumed somatic mutations in mice.
Hata, S; Nomura, T; Shibata, K, 1983
)
0.99
"Urethane treatment alone markedly increased the micronucleus frequency from 0.1% in the vehicle control to 2.47%."( A pharmacokinetic study of ethanol inhibition of micronuclei induction by urethane in mouse bone marrow erythrocytes.
Black, HE; Black, W; Choy, WN; Mandakas, G; Mirro, EJ, 1995
)
1.24
"In urethane-treated (0.6 g/kg, i.p.) decerebrate rats, GYKI 52466 (0.5-4 mg/kg, i.v.) depressed bladder contraction amplitude and sphincter EMG activity, similar to the effects in urethane-anesthetized (1.2 g/kg, s.c.) intact rats."( Effects of GYKI 52466 and CNQX, AMPA/kainate receptor antagonists, on the micturition reflex in the rat.
de Groat, WC; Roppolo, JR; Yoshiyama, M, 1995
)
0.81
"Urethane treatment produced robust Fos expression in the central nucleus of the amygdala and the paraventricular and supraoptic nuclei of the hypothalamus 1 h after treatment."( Lactation reduces Fos induction in the paraventricular and supraoptic nuclei of the hypothalamus after urethane administration in rats.
Amir, S; Woodside, B, 1997
)
1.23
"In urethane-treated rats, L-NAME administration did not change Fos-lir in lactating rats but reduced Fos-lir in nonlactating rats."( Effect of nitric oxide synthase inhibition on fos expression in the hypothalamus of female rats following central oxytocin and systemic urethane administration.
Popeski, N; Woodside, B, 2001
)
1.03
"Urethane treatment induced hepatic MT 14-fold over control; styrene treatment induced MT 2.5-fold."( The role of metallothionein induction and altered zinc status in maternally mediated developmental toxicity: comparison of the effects of urethane and styrene in rats.
Daston, GP; Keen, CL; Lehman-McKeeman, LD; Overmann, GJ; Rogers, JM; Taubeneck, MW, 1991
)
1.2
"Urethane treatment resulted in a significant elevation of central noradrenergic neuronal activity (NNA) as assessed from marked rises in hypothalamic DHPG concentrations and the ratio (DHPG/NA)."( Stimulation of the hypothalamic-pituitary-adrenal axis and inhibition of growth hormone release via increased central noradrenaline neuronal activity by urethane anaesthesia in the rat: blockade by clonidine.
Gleeson, RM; Smythe, GA; Stead, BH, 1987
)
1.19
"Urethane treated SWR mice received 6 fortnightly injections of lymphocytes sensitized in vitro against syngeneic fibroblasts."( Increased incidence of urethane induced lung adenomata by autosensitized lymphocytes.
Carnaud, C; Cohen, IR; Levo, Y; Trainin, N, 1974
)
1.29
"Urethane treatment is characterized by induction of a transient hypoplasia which is not in agreement with the level of cellular division."( Correlation of initial changes in the mouse epidermal cell population with two stage carcinogenesis-a quantitative study.
Major, IR, 1970
)
0.97
"The treatment with urethane was associated with the downregulation of Cx26, 32 and 46 expressions, and with the upregulation of Cx43 expression in lung tissue."( Altered expression of connexins in urethane-induced mouse lung adenomas.
Avanzo, JL; da Silva, TC; Dagli, ML; Fukumasu, H; Hernandez-Blazquez, FJ; Mesnil, M; Mori, CM; Yamasaki, H, 2006
)
0.93

Toxicity

The electrospun polycarbonate-urethane graft is safe in humans, permits early access obviating the need for venous catheters, and has equivalent patency to other prosthetic grafts at 1 year.

ExcerptReferenceRelevance
"Oral administration of NMU at maximally tolerated doses of guinea-pigs from day 34 to 58 of pregnancy induced embryotoxic effects, as evidenced by a high incidence of stillbirths and reduction in birth weight, and postnatal toxic effects, as evidenced by stunting, progressive mortality and extensive fatty degeneration of the liver in F1 progeny."( Prenatal and postnatal toxicity induced in guinea-pigs by nitrosomethylurea.
Epstein, SS; Hasumi, K; Iobal, ZM, 1976
)
0.26
"It is generally accepted that the sensitivity to toxic effects of digitalis increases with advancing age; however, the relative contribution of pharmacokinetics and pharmacodynamics to this aging-related change is presently unknown."( Digoxin cardiotoxicity in aging anesthetized F344 rats.
Kennedy, RH; Ruch, S; Seifen, E, 1992
)
0.28
" A rapid toxic effect was observed, especially with the urethane-linked network."( Skin organ culture model to test the toxicity of polyoxyethylene networks.
Beele, H; de Ridder, L; Deveux, R; Goethals, E; Thierens, H, 1992
)
0.53
" There was no laboratory evidence of a direct toxic effect by mercury on the patients."( Comprehensive medical examination of a group of patients with alleged adverse effects from dental amalgams.
Anneroth, G; Ericson, T; Johansson, I; Mörnstad, H; Ryberg, M; Skoglund, A; Stegmayr, B, 1992
)
0.28
"We hypothesize that maternal metallothionein (MT) induction by toxic dosages of chemicals may contribute to or cause developmental toxicity by a chain of events leading to a transient but developmentally adverse decrease in Zn availability to the embryo."( The role of metallothionein induction and altered zinc status in maternally mediated developmental toxicity: comparison of the effects of urethane and styrene in rats.
Daston, GP; Keen, CL; Lehman-McKeeman, LD; Overmann, GJ; Rogers, JM; Taubeneck, MW, 1991
)
0.48
" In an effort to characterize the cardiovascular effects and potential toxic action of copper, white New Zealand rabbits were instrumented for the measurement of cardiovascular parameters under urethane anesthesia."( Acute cardiovascular toxic effects of copper in anesthetized rabbits.
Dunlap, M; Rhee, HM, 1990
)
0.47
" According to median lethalities, all three known carcinogens were substantially more toxic than nitrosocimetidine whether administered by the intravenous, intraperitoneal, or oral routes."( Comparison of the acute toxicity of N-nitrosocimetidine with three structurally related carcinogens in the rat.
Hard, GC; Jensen, DE; Magee, PN; Ogiu, T, 1986
)
0.27
" The immune system can be a target for many chemicals including environmental contaminants and drugs with potential adverse effects on human health."( In vitro tests to evaluate immunotoxicity: a preliminary study.
Carfi', M; Corsini, E; Gennari, A; Gribaldo, L; Hartung, T; Malerba, I; Pallardy, M; Pieters, R; Van Loveren, H; Vohr, HW, 2007
)
0.34
" To determine the suitability of this model for screening inhaled toxicants, the EpiAirway tissue model (ETM) was treated apically with tobacco smoke components (nicotine, formaldehyde, cadmium, urethane) which are known to induce a variety of toxic effects (e."( An in vitro approach to assess the toxicity of inhaled tobacco smoke components: nicotine, cadmium, formaldehyde and urethane.
Balharry, D; BéruBé, KA; Sexton, K, 2008
)
0.74
" Liver-enzyme alterations at 250 and 1000 mg/kg were considered to be potentially adverse effects."( Subchronic, reproductive, and developmental toxicity of a fluorotelomer-based urethane polymeric product.
Buck, RC; Delker, DA; Everds, NE; Frame, SR; Loveless, SE; Malley, LA; Munley, SM; Mylchreest, E; Stadler, JC, 2008
)
0.57
"The electrospun polycarbonate-urethane graft is safe in humans, permits early access obviating the need for venous catheters, and has equivalent patency to other prosthetic grafts at 1 year."( Safety and efficacy of electrospun polycarbonate-urethane vascular graft for early hemodialysis access: first clinical results in man.
Kannangara, L; Wijeyaratne, SM,
)
0.67
" The nonobserved adverse effect levels (NOAELs) of the evaluated carbamates were 12."( Subchronic toxicity study in rats of two new ethyl-carbamates with ixodicidal activity.
Abrego-Reyes, VH; Alba-Hurtado, F; Angeles, E; Muñoz-Guzmán, MA; Prado-Ochoa, MG; Ramírez-Noguera, P; Velázquez-Sánchez, AM, 2014
)
0.4
" The oral LD50 of each carbamate was 300 to 2000 mg/kg, and the dermal LD50 of each carbamate was >5000 mg/kg."( Assessment of acute oral and dermal toxicity of 2 ethyl-carbamates with activity against Rhipicephalus microplus in rats.
Abrego-Reyes, VH; Alba-Hurtado, F; Angeles, E; Gutiérrez-Amezquita, RA; Muñoz-Guzmán, MA; Prado-Ochoa, MG; Ramírez-Noguera, P; Velázquez-Sánchez, AM, 2014
)
0.4
" The carcinogenic and toxic possibility of EC is thought to be related to its metabolite vinyl carbamate (VC)."( Lysosomal Reacidification Ameliorates Vinyl Carbamate-Induced Toxicity and Disruption on Lysosomal pH.
Chen, W; Cui, S; Hu, D; Li, Y; Qi, J, 2020
)
0.56
"The hypothesis of this parallel group randomized trial testifies if TissuGlu is a safe and an effective alternative to the conventional drainage placement in regard to post-operative fluid management in the abdominal donor site for autologous (DIEP flap) breast reconstruction with a higher postoperative patient quality of life."( Randomized Single-Center Study of Effectiveness and Safety of a Resorbable Lysine-Based Urethane Adhesive for a Drain-Free Closure of the Abdominal Donor Site in a DIEP Flap Breast Reconstruction Procedure.
Andree, C; Fertsch, S; Grueter, L; Hagouan, M; Kornetka, J; Michalak, M; Munder, B; Schulz, T; Stambera, P; Steammler, K; Wolter, A, 2022
)
0.94
"The abdominal closure with the surgical adhesive seems to be a safe procedure that contributes to patient satisfaction and increases the independence upon discharge in patients with adequate inclusion criteria."( Randomized Single-Center Study of Effectiveness and Safety of a Resorbable Lysine-Based Urethane Adhesive for a Drain-Free Closure of the Abdominal Donor Site in a DIEP Flap Breast Reconstruction Procedure.
Andree, C; Fertsch, S; Grueter, L; Hagouan, M; Kornetka, J; Michalak, M; Munder, B; Schulz, T; Stambera, P; Steammler, K; Wolter, A, 2022
)
0.94

Pharmacokinetics

Urethane as an anesthetic in pharmacokinetic studies still persists, particularly in experiments of long duration. Neither urethane-chloralose nor L-NAME modified estimation of pharmacokinetics parameters of carvedilol.

ExcerptReferenceRelevance
" The use of urethane as an anesthetic in pharmacokinetic studies still persists, particularly in experiments of long duration."( Possible hemodynamic basis to urethane anesthesia-induced reductions in renal clearance.
Gumbleton, M; Nicholls, PJ; Taylor, G,
)
0.8
" Under urethan anesthesia, thiamine displayed apparent dose-dependent kinetics as measured by the changes in the pharmacokinetic parameters, AUC,Vd(area), t0."( Thiamine whole blood and urinary pharmacokinetics in rats: urethan-induced dose-dependent pharmacokinetics.
Pipkin, JD; Stella, VJ, 1982
)
0.26
" Two pharmacokinetic parameters, Cmax and AUC, were estimated for each dose."( A pharmacokinetic study of ethanol inhibition of micronuclei induction by urethane in mouse bone marrow erythrocytes.
Black, HE; Black, W; Choy, WN; Mandakas, G; Mirro, EJ, 1995
)
0.52
"Neither urethane-chloralose nor L-NAME modified estimation of pharmacokinetic parameters of carvedilol."( Is urethane-chloralose anaesthesia appropriate for pharmacokinetic-pharmacodynamic assessment? Studies with carvedilol.
Bertera, FM; Bramuglia, GF; Di Verniero, CA; Höcht, C; Mayer, MA; Taira, CA,
)
1.19
" Anaesthesia did not modify pharmacokinetic behaviour of carvedilol in both normotensive and L-NAME hypertensive rats."( Is urethane-chloralose anaesthesia appropriate for pharmacokinetic-pharmacodynamic assessment? Studies with carvedilol.
Bertera, FM; Bramuglia, GF; Di Verniero, CA; Höcht, C; Mayer, MA; Taira, CA,
)
0.75

Compound-Compound Interactions

ExcerptReferenceRelevance
"Phenytoin is an anticonvulsant drug known to interact with many other drugs."( Studying long-term effect of phenytoin either alone or combined with ascorbic acid on the anesthetic effect of urethane in rats.
Abdulla, MM; El Desoky, ES, 2004
)
0.54
" The new procedure uses positive ion chemical ionisation (PICI) and tandem mass spectrometry (MS/MS), combined with gas chromatography (GC), on a 'bench-top' triple-quadrupole mass spectrometer."( Application of positive ion chemical ionisation and tandem mass spectrometry combined with gas chromatography to the trace level analysis of ethyl carbamate in bread.
Hamlet, CG; Jayaratne, SM; Morrison, C, 2005
)
0.33
"An analytical methodology based on headspace solid phase microextraction (HS-SPME) combined with comprehensive two-dimensional gas chromatography-time-of-flight mass spectrometry (GC x GC-ToFMS) was developed for the identification and quantification of the toxic contaminant ethyl carbamate (EC) directly in fortified wines."( Comprehensive two-dimensional gas chromatography with time-of-flight mass spectrometry combined with solid phase microextraction as a powerful tool for quantification of ethyl carbamate in fortified wines. The case study of Madeira wine.
Câmara, JS; Perestrelo, R; Petronilho, S; Rocha, SM, 2010
)
0.36

Bioavailability

ExcerptReferenceRelevance
" Curcumin has long been recognized as a chemopreventive agent, but poor bioavailability and weak Nrf2 induction have prohibited clinical application."( A Curcumin Derivative That Inhibits Vinyl Carbamate-Induced Lung Carcinogenesis via Activation of the Nrf2 Protective Response.
Chapman, E; Chen, J; Jiang, T; Long, M; Ren, DM; Shen, T; Wong, PK; Zhang, DD; Zhou, B, 2015
)
0.42
"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
" As olanzapine has shown poor bioavailability and permeability in the brain, the sustained release of olanzapine from the designed carriers could enhance pharmacokinetic effectiveness."( Sustained delivery of olanzapine from sunflower oil-based polyol-urethane nanoparticles synthesised through a cyclic carbonate ring-opening reaction.
Babanejad, N; Dorkoosh, F; Farhadian, A; Mozafari, M; Nabid, MR; Saeb, MR; Zarrintaj, P, 2019
)
0.75
" Compared to free GA, the optimized PEUU nanocarrier improves the intratumoral distribution of GA by more than 9-fold, which significantly enhances the bioavailability and persistence of GA after intravenous administration."( Optimization of amino acid-based poly(ester urea urethane) nanoparticles for the systemic delivery of gambogic acid for treating triple negative breast cancer.
Bian, Z; Chu, CC; Ji, Y; Kwan, HY; Li, J; Xiao, S, 2023
)
1.16

Dosage Studied

Urethane was studied for its potential to induce micronuclei in bone marrow of CD-1 mice following various dosing and sampling schedules. The influence of different baseline values (blood pressure, heart rate) on ED50- and Emax-values of isoprenaline dose-response curves (DRC) was assessed.

ExcerptRelevanceReference
" Dose-response curves were obtained using mice at pressures ranging from 1 to 125 atm for five agents, namely alpha-chloralose, ethylcarbamate, phenobarbital and, for comparison, nitrogen and argon."( The pressure reversal of a variety of anesthetic agents in mice.
Miller, KW; Wilson, MW, 1978
)
0.26
"The genotoxic carcinogen vinyl carbamate was dosed to C57Bl/10J strain mice for 35 weeks, and the study terminated after week 59."( Hepatocarcinogenic effect of vinyl carbamate in the C57Bl/10J strain mouse.
Marsden, AM; Orton, TC; Willets, JM; Wright, JA, 1991
)
0.28
"1 mg/kg po) in male A/JAX mice in a dose-response manner."( Studies on inhibition and induction of metabolism of ethyl carbamate by acetone and related compounds. Evidence for metabolism by cytochromes P-450.
Benz, FW; Hurst, HE; Kemper, RA; Kurata, N; Waddell, WJ,
)
0.13
"Detailed dose-response data for two reference aneugens, vincristine and nocodazole, have been derived for the mouse bone marrow micronucleus assay."( Micronucleus morphology as a means to distinguish aneugens and clastogens in the mouse bone marrow micronucleus assay.
Ashby, J; Tinwell, H, 1991
)
0.28
" The tumors with a clear dose-response relationship were lung tumor (alveolar/bronchiolar adenoma or carcinoma) and liver tumor (hemangioma or angiosarcoma)."( Quantitative risk assessment of carcinogenicity of urethane (ethyl carbamate) on the basis of long-term oral administration to B6C3F1 mice.
Arihiro, K; Inai, K; Khatun, N; Nishisaka, T; Tachiyama, Y; Takeshima, Y; Yonehara, S, 1991
)
0.53
" Positive results were obtained irrespective of the strain (CD1, CRH) or dosing regimen (single, triple-dose) used."( Activity of urethane in rat and mouse micronucleus tests after oral administration.
Gatehouse, D; Plumstead, M; Westmoreland, C, 1991
)
0.66
"Urethane was studied for its potential to induce micronuclei in bone marrow of CD-1 mice following various dosing and sampling schedules."( Induction of micronuclei in bone marrow of mice exposed to 1, 2 or 3 daily doses of urethane.
Holmstrom, M,
)
1.8
" Yohimbine caused about a 30 fold shift to the right in the dose-response curve whereas idazoxan almost completely abolished the mydriatic response to (+)-Amp."( Mechanism of dexamphetamine-induced mydriasis in the anaesthetized rat.
Hey, JA; Ito, T; Koss, MC, 1989
)
0.28
"The development of hepatic enzyme-altered foci (ATPase, GGTase) was investigated after dosing vinyl acetate (200 and 400 mg/kg per day, orally) to newborn rats for 3 weeks, with or without subsequent promotion by phenobarbital."( Vinyl acetate, a structural analog of vinyl carbamate, fails to induce enzyme-altered foci in rat liver.
Bolt, HM; Laib, RJ, 1986
)
0.27
"5 g/kg) and an anesthetic dosage (1."( Urethane affects the rat visual system at subanesthetic doses.
Dyer, RS; Rigdon, GC, 1987
)
1.72
"The influence of different baseline values (blood pressure, heart rate) on ED50- and Emax-values of isoprenaline dose-response curves (DRC) in the presence and absence of beta-blocking drugs was assessed in urethane-anesthetized rats."( Assessment of adrenergic beta-blockade in the anesthetized rat at different baseline values.
Brunner, F; Pöch, G, 1984
)
0.45
" After chronic dosing the sedative effects of flunitrazepam showed tolerance and the increases in exploration remained while locomotion was less increased."( Effects of agents which enhance GABA-mediated neurotransmission on licking conflict in rats and exploration in mice.
Gardner, CR; Piper, DC, 1982
)
0.26
" There is also a significant dose-response relationship."( Urethan (ethyl carbamate) alone is carcinogenic for mouse skin.
Iversen, OH, 1984
)
0.27
" The respiratory depression was prolonged by increased dosage with urethane and chloralose."( Effects of urethane-chloralose anaesthesia on respiration in the rat.
Hughes, EW; Martin-Body, RL; Sarelius, IH; Sinclair, JD,
)
0.76
"41) was taken into account in the dose-response data of the previous report, doubling doses were estimated to be about 25 and 50 rad for spermatids and spermatogonia respectively."( X-ray-induced germ-line mutation leading to tumors. Its manifestation in mice given urethane post-natally.
Nomura, T, 1983
)
0.49
" In contrast, exposure to the multipotential carcinogen, ethyl carbamate (urethan) at tumourigenic dosages caused severe myelotoxicity at all dosage levels."( Immune functions in methyl and ethyl carbamate treated mice.
Boorman, GA; Dean, JH; Dieter, MP; Hayes, HT; Luster, MI, 1982
)
0.26
" This inverse dose-response relationship mimics the previously reported effect of 5-methyl cytidine on mammary tumour growth in C3H mice."( Inhibition of urethan induced lung tumour growth in strain A mice by 5-methyl cytidine.
Theiss, JC, 1980
)
0.26
") administered 18 h prior to dosing with EC decreased the binding of [14C-ethyl]EC to cellular macromolecules."( The effect of pyridine on the in vitro and in vivo metabolism of ethyl carbamate (urethane) by rat and mouse.
Carlson, GP; Page, DA, 1994
)
0.51
" Dose-response relationship and sequential changes in lung tumorigenesis induced by urethan in athymic mice were compared with those in euthymic littermates."( Comparison of lung tumorigenesis induced by urethan in athymic nude mice and euthymic littermates.
Kobayashi, S; Noda, Y; Otsu, H, 1994
)
0.29
" The ability of intrathecal glycine and the glycine derivative betaine to reverse strychnine-induced allodynia was also determined using dose-response analysis."( Strychnine-dependent allodynia in the urethane-anesthetized rat is segmentally distributed and prevented by intrathecal glycine and betaine.
Loomis, CW; Sherman, SE, 1995
)
0.56
" An acute dosing of ethyl carbamate at 1 g/kg also caused not only a significant suppression of the antibody response, but also a decrease in thymus weight."( Role of metabolism in ethyl carbamate-induced suppression of antibody response to sheep erythrocytes in female Balb/C mice.
Cha, SW; Ha, CS; Han, SS; Jeong, TC; Park, JI; Roh, JK, 1995
)
0.29
"To test the hypothesis that altered neuronal activity may influence the extent and severity of the glio-vascular lesions produced by 1,3-dinitrobenzene (DNB), rats were either given the tremorgenic pyrethroid, Bifenthrin, or anaesthetised during various dosing schedules of DNB."( Increasing or decreasing nervous activity modulates the severity of the glio-vascular lesions of 1,3-dinitrobenzene in the rat: effects of the tremorgenic pyrethroid, Bifenthrin, and of anaesthesia.
Burr, SA; Cavanagh, JB; Holton, JL; Nolan, CC; Ray, DE, 1997
)
0.3
" However, the duration of this anesthesia was too short (approximately 30 minutes) to complete the necessary testing and additional dosing of the anesthetic generally obliterated the micturition reflex."( Effect of anesthetics on reflex micturition in the chronic cannula-implanted rat.
Downie, JW; Matsuura, S, 2000
)
0.31
" The United States Food and Drug Administration nominated urethane for study because of the widespread exposure of humans through the consumption of fermented foods and beverages and because of a lack of adequate dose-response data about the carcinogenicity of urethane with and without the coadministration of ethanol."( NTP technical report on toxicity studies of urethane in drinking water and urethane in 5% ethanol administered to F344/N rats and B6C3F1 mice.
Chan, PC, 1996
)
0.8
"8 tumors/mouse due to the Pas1 allele dosage effect."( Cancer modifier alleles inhibiting lung tumorigenesis are common in inbred mouse strains.
Acevedo, A; Dragani, TA; Galbiati, F; Giannì Barrera, R; Manenti, G; Noci, S; Salido, E, 2002
)
0.31
" Ten weekly ethyl carbamate (EC) doses caused a nearly 100% lung tumor incidence with a tumor multiplicity >2; multiple EC dosing is thus an alternative to the time-consuming transfer of transgenes and null mutations to susceptible backgrounds."( Induction of a high incidence of lung tumors in C57BL/6 mice with multiple ethyl carbamate injections.
Dwyer-Nield, LD; Franklin, WA; Keith, RL; Le, M; Malkinson, AM; Miller, YE, 2003
)
0.32
" Other metabolites which have been detected in urine of animals dosed with urethane and N-hydroxyurethane are ethylmercapturic acid, ethylmercapturic acid sulphoxide and N-acetyl-S-carbethoxycysteine."( THE MATABOLISM OF URETHANE AND RELATED COMPOUNDS.
BOYLAND, E; NERY, R, 1965
)
0.81
" A dose-response relationship of phenytoin in this regard is expected and needs further investigations."( Studying long-term effect of phenytoin either alone or combined with ascorbic acid on the anesthetic effect of urethane in rats.
Abdulla, MM; El Desoky, ES, 2004
)
0.54
" In conclusion, multiple dosing led to considerable bioaccumulation of urethane in mice of both genotypes; however, greater retention occurred in CYP2E1-/- versus CYP2E1+/+ mice."( Increased bioaccumulation of urethane in CYP2E1-/- versus CYP2E1+/+ mice.
Ghanayem, BI; Hoffler, U, 2005
)
0.85
"Comparisons on a linear and the Rozman logarithmic scale for dosage versus carcinogenicity in rodents are presented for methyl eugenol (ME), nitrosodiethylamine (NDEA), ethyl carbamate (EC) and 2-acetylaminofluorene (AAF)."( Comparisons of thresholds for carcinogenicity on linear and logarithmic dosage scales.
Waddell, WJ, 2005
)
0.33
" Three experiments were performed: (i) a dose-response study with vinyl carbamate-induced tumors; (ii) a limited treatment study also with vinyl carbamate and (iii) prevention of NNK-induced tumors."( Prevention of mouse lung tumors by targretin.
Alyaqoub, FS; Gunning, WT; Kramer, PM; Liu, Y; Lubet, RA; Nines, R; Pereira, MA; Steele, VE, 2006
)
0.33
" Antitumor and antioxidant effect of relatively low dosage of melatonin appeared to be more effective than those of a larger one."( [Melatonin inhibits urethane-induced carcinogenesis tumors in murine lung].
Anisimov, VN; Plotnikova, NA; Semenchenko, AV; Vesnushkin, GM, 2006
)
0.66
" If mice were fed either the methyl ester or the ethyl amide derivative of the synthetic triterpenoid 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO-ME and CDDO-EA, respectively), beginning 1 week after dosing with carcinogen, the number, size, and severity of lung carcinomas were markedly reduced."( The synthetic triterpenoids CDDO-methyl ester and CDDO-ethyl amide prevent lung cancer induced by vinyl carbamate in A/J mice.
Dmitrovsky, E; Gribble, GW; Honda, T; Liby, K; Risingsong, R; Royce, DB; Sporn, MB; Sporn, TA; Williams, CR; Yore, MM, 2007
)
0.34
" For the reproduction study, rats were dosed for 10 weeks prior to cohabitation and throughout mating, gestation, and lactation."( Subchronic, reproductive, and developmental toxicity of a fluorotelomer-based urethane polymeric product.
Buck, RC; Delker, DA; Everds, NE; Frame, SR; Loveless, SE; Malley, LA; Munley, SM; Mylchreest, E; Stadler, JC, 2008
)
0.57
" The risk assessment was conducted using the margin of exposure (MOE) approach with benchmark doses obtained from dose-response modelling of animal experiments."( Cancer risk assessment of ethyl carbamate in alcoholic beverages from Brazil with special consideration to the spirits cachaça and tiquira.
Kanteres, F; Kerr-Corrêa, F; Lachenmeier, DW; Lima, MC; Nóbrega, IC; Pereira, JA; Rehm, J, 2010
)
0.36
" Extending the single-exposure setting, representations of risk are based on a joint-action dose-response model involving both agents."( Benchmark dose profiles for joint-action continuous data in quantitative risk assessment.
Deutsch, RC; Piegorsch, WW, 2013
)
0.39
" PCA has been orally feed to urethane (ethyl carbamate) primed lung cancerous mice at a dosage of 100 mg/kg body weight for 30 consecutive days."( Antineoplastic and immunomodulatory effect of polyphenolic components of Achyranthes aspera (PCA) extract on urethane induced lung cancer in vivo.
Kumar, A; Narayan, C, 2014
)
0.91
" Recent clinical data suggest that these different dosing schedules may adversely affect antigen-specific immunotherapy."( Assessing the Effects of Concurrent versus Sequential Cisplatin/Radiotherapy on Immune Status in Lung Tumor-Bearing C57BL/6 Mice.
DeGregorio, MW; Griffey, SM; Kao, CJ; Lin, YC; Vang, DP; Wolf, M; Wurz, GT, 2015
)
0.42
" Our objective was to investigate the quality of anesthesia and the correlation between bladder (voiding) contractions, micturition pressure, bladder capacity and urethane dosage and body weight."( Urethane anesthesia in acute lower urinary tract studies in the male rat.
Choudhary, M; Clavica, F; van Asselt, E; van Mastrigt, R, 2017
)
2.09
" Furthermore, comparison of the magnitude of the genotoxicity responses indicated that the micronucleus and Comet endpoints generally produced greater responses with the higher dose, short-term treatments in the 3-day study, while the Pig-a assay responded better to the cumulative effects of the lower dose, but repeated subchronic dosing in the 28-day study."( Assessment of the Pig-a, micronucleus, and comet assay endpoints in rats treated by acute or repeated dosing protocols with procarbazine hydrochloride and ethyl carbamate.
Chen, G; Huang, Z; Jiang, H; Mao, Z; Miao, Y; Song, J; Wang, C; Wang, W; Wang, X; Wen, H; Yang, Y, 2019
)
0.51
" We designed acyclovir dosage forms to be administered less frequently by being retained in the stomach and releasing drug over an extended duration."( Hydrophilic Poly(urethanes) Are an Effective Tool for Gastric Retention Independent of Drug Release Rate.
Lowinger, MB; Maier, EY; Williams, RO; Zhang, F, 2020
)
0.9
" However, whether high dosage of CPFX has side effects on gut barrier integrity is still unclear."( Assessment of oral ciprofloxacin impaired gut barrier integrity on gut bacteria in mice.
Li, H; Li, Z; Liang, J; Lv, C; Niu, M; Xu, K; Zeng, L; Zhao, K; Zhu, S, 2020
)
0.56
"To evaluate the effects of pentobarbital dosages on lower urinary tract function and to define an appropriate dosage of sodium pentobarbital that would be suitable for urodynamic studies in which recovery from anesthesia and long term survive were needed for subsequent experiment."( Verification and Defined Dosage of Sodium Pentobarbital for a Urodynamic Study in the Possibility of Survival Experiments in Female Rat.
Abulikim, K; Cao, P; Du, GH; Tan, HB; Xu, SF, 2020
)
0.56
"This study confirmed significant dose-dependent effects of pentobarbital on lower urinary tract function and 32 mg/kg pentobarbital as an appropriate dosage for recovery urodynamic testing, which enable the achievement of expected essential micturition under satisfactory anesthesia in female rats."( Verification and Defined Dosage of Sodium Pentobarbital for a Urodynamic Study in the Possibility of Survival Experiments in Female Rat.
Abulikim, K; Cao, P; Du, GH; Tan, HB; Xu, SF, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
mutagenAn agent that increases the frequency of mutations above the normal background level, usually by interacting directly with DNA and causing it damage, including base substitution.
fungal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in fungi, the kingdom that includes microorganisms such as the yeasts and moulds.
[role 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]

Drug Classes (1)

ClassDescription
carbamate esterAny ester of carbamic acid or its N-substituted 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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency39.81070.012610.691788.5700AID887
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency1.50893.189029.884159.4836AID1224846
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.92670.000214.376460.0339AID720691
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency65.06770.003041.611522,387.1992AID1159552
retinoid X nuclear receptor alphaHomo sapiens (human)Potency17.37390.000817.505159.3239AID1159531
estrogen nuclear receptor alphaHomo sapiens (human)Potency37.66510.000229.305416,493.5996AID743075; AID743079
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency21.87240.023723.228263.5986AID743223
Cellular tumor antigen p53Homo sapiens (human)Potency1.18830.002319.595674.0614AID651631
[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 (146)

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)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

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)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

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)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1134605Oil-water partition coefficient, log P of the compound1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Hydrogen-bonding parameter and its significance in quantitative structure--activity studies.
AID409949Inhibition of human liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1145367Drug absorption in intestine (unknown origin) assessed as tissue-bound transfer1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
Molecular connectivity. 6. Examination of the parabolic relationship between molecular connectivity and biological activity.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1145377Drug absorption in intestine (unknown origin) assessed as mucosal loss1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
Molecular connectivity. 6. Examination of the parabolic relationship between molecular connectivity and biological activity.
AID1134606Et2O-water partition coefficient, log P of the compound1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Hydrogen-bonding parameter and its significance in quantitative structure--activity studies.
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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1145376Drug absorption in intestine (unknown origin) assessed as serosal transfer1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
Molecular connectivity. 6. Examination of the parabolic relationship between molecular connectivity and biological activity.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID409951Inhibition of human liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
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.
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.
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.
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 (4,651)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902774 (59.64)18.7374
1990's592 (12.73)18.2507
2000's508 (10.92)29.6817
2010's587 (12.62)24.3611
2020's190 (4.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 71.78

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index71.78 (24.57)
Research Supply Index8.52 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index198.89 (26.88)
Search Engine Supply Index3.04 (0.95)

This Compound (71.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials36 (0.72%)5.53%
Reviews122 (2.45%)6.00%
Case Studies30 (0.60%)4.05%
Observational1 (0.02%)0.25%
Other4,797 (96.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Evaluation of an Experimental Urethane Dimethacrylate Resin Based Composite [NCT02018822]85 participants (Actual)Interventional2013-06-30Completed
Drain-Less Abdominally Based Breast Reconstruction Using a Novel Lysine-Derived Urethane Adhesive (TissueGlu, Cohera Medical) [NCT03159598]0 participants (Actual)Interventional2020-11-01Withdrawn(stopped due to PI left institution, never submitted to IRB)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02018822 (5) [back to overview]Percent of Teeth Scored as A or B for Color Match
NCT02018822 (5) [back to overview]Percent of Teeth With Marginal Discoloration of A or B
NCT02018822 (5) [back to overview]Percent of Teeth With Marginal Integrity Graded A, B1 and B2
NCT02018822 (5) [back to overview]Percent of Teeth With Polish-ability of A, B1 or B2
NCT02018822 (5) [back to overview]Percent of Teeth With Proximal Contact

Percent of Teeth Scored as A or B for Color Match

"A=The restoration appears to match the shade and translucency of adjacent tooth structure.~B=The restoration does not match the shade and translucency of adjacent tooth structure, but the mismatch is within the normal range of tooth shades and translucency." (NCT02018822)
Timeframe: 24 months

,,
Interventionteeth (Count of Units)
AB
Participants That Completed Esthet-X Intervention401
TPH3402
UDMA413

[back to top]

Percent of Teeth With Marginal Discoloration of A or B

"A= There is no visual evidence of marginal discoloration different from the color of the restorative material and from the color the adjacent tooth structure.~B= There is visual evidence of marginal discoloration at the junction of the tooth structure and the restoration, but the discoloration has not penetrated along the restoration in a pulpal direction." (NCT02018822)
Timeframe: 24 months

,,
Interventionteeth (Count of Units)
AB
Teeth That Received Esthet-X-HD392
Teeth That Received TPH3402
Teeth That Received UDMA395

[back to top]

Percent of Teeth With Marginal Integrity Graded A, B1 and B2

A= No visible evidence of a crevice along the margin into which the explorer will penetrate B1= Explorer clicks on the margin B2= Visible evidence of a crevice (NCT02018822)
Timeframe: 24 months

,,
Interventionteeth (Count of Units)
AB1B2
Teeth That Received Esthet-X-HD3911
Teeth That Received TPH33642
Teeth That Received UDMA3923

[back to top]

Percent of Teeth With Polish-ability of A, B1 or B2

A= Smooth & highly shiny, similar to enamel B1= Smooth & satin, highly reflective B2= Smooth & shiny but not highly reflective (NCT02018822)
Timeframe: 24 months

,,
Interventionteeth (Count of Units)
AB1B2
Teeth That Received Esthet-X-HD4010
Teeth That Received TPH34011
Teeth That Received UDMA4121

[back to top]

Percent of Teeth With Proximal Contact

A= Tight proximal contacts evaluated with dental floss. B= Proximal contacts are weak but present. C= No proximal contacts but not visibly open. NA= Class I restorations (NCT02018822)
Timeframe: 24 months

,,
Interventionteeth (Count of Units)
ABCNA
Teeth That Received Esthet-X-HD292010
Teeth That Received TPH328419
Teeth That Received UDMA32417

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