Page last updated: 2024-11-09

thiourea

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

Description

Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur. [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]

Cross-References

ID SourceID
PubMed CID2723790
CHEMBL ID260876
CHEBI ID36946
MeSH IDM0021386

Synonyms (120)

Synonym
BIDD:ER0582
wln: zyzus
thiuronium
pseudothiourea
urea, thio-
.beta.-thiopseudourea
nsc-5033
usaf ek-497
urea, 2-thio-
nsc5033
62-56-6
sulourea
2-thiourea
pseudourea, 2-thio-
thiourea
thiocarbamide
thiocarbonic acid diamide
h2nc(s)nh2
thiokarbamid
thiocarbamid
aminothioamide
aminothiocarboxamide
thioharnstoff
carbonothioic diamide
CHEBI:36946 ,
TOU ,
sulfouren
NCGC00091199-01
2-thiopseudourea
rcra waste number u219
epa pesticide chemical code 080201
nsc 5033
ai3-03582
caswell no. 855
sulfocarbamide
tsizp 34
thiomocovina [czech]
hsdb 1401
isothiourea
rcra waste no. u219
ccris 588
beta-thiopseudourea
einecs 200-543-5
thiourea, acs reagent, >=99.0%
sulfourea
thiourea, reagentplus(r), >=99.0%
thiourea, puriss. p.a., acs reagent, >=99.0%
bdbm50229993
CHEMBL260876 ,
AKOS000269032
MLS002454451
smr000857187
thiourea, acs
A833853
NCGC00091199-03
NCGC00091199-02
T2835
dtxsid9021348 ,
dtxcid101348
cas-62-56-6
NCGC00256530-01
tox21_302767
tox21_201873
NCGC00259422-01
17356-08-0
T0445
T2475
HMS2234E12
FT-0675198
thiomocovina
gyv9am2qag ,
ec 200-543-5
unii-gyv9am2qag
carbamimidothioic acid
HMS3369M21
thiourea [mi]
thiourea [vandf]
thiourea [iarc]
propylthiouracil impurity a [ep impurity]
thiourea [hsdb]
thiourea [inci]
thiourea [who-dd]
BP-31025
CCG-207963
thiopseudourea
thio-urea
un 2877
(nh2)2cs
mfcd00008067
AKOS028109302
J-524966
T-3650
F0001-1650
thiourea, jis special grade, >=98.0%
thiourea, >=99.999% (metals basis)
thiourea, 99%
thiourea, lr, >=98%
thiourea, pharmaceutical secondary standard; certified reference material
thiourea, p.a., acs reagent, 99.0%
thiocarbonic diamide
beta -thiopseudourea
urea, thio- (8ci)
2-thio-urea
2-thio-pseudourea
thiourea acs reagent grade
Q528995
BCP27948
doi:10.14272/umgdcjdmyokajw-uhfffaoysa-n.1
10.14272/UMGDCJDMYOKAJW-UHFFFAOYSA-N.1
STL194300
STR00054
AMY40190
s c (n h2)2
EN300-19634
caswell no 855
propylthiouracil impurity a (ep impurity)
thiourea; thiocarbamide
thiocarbmate
urea, 2-thio
thiourea (iarc)

Research Excerpts

Overview

Thiourea (TU) is a chemo-priming agent and non-physiological reactive oxygen species (ROS) scavenger. It has been found to reduce As accumulation in rice grains along with improved growth and yield. Thioureas are an uncommon underrecognized cause of allergic contact dermatitis (ACD)

ExcerptReferenceRelevance
"Thiourea (TU) is a chemo-priming agent and non-physiological reactive oxygen species (ROS) scavenger whose application has been found to reduce As accumulation in rice grains along with improved growth and yield. "( Antioxidant enzymes and transporter genes mediate arsenic stress reduction in rice (Oryza sativa L.) upon thiourea supplementation.
Bose, S; Majumdar, A; Srivastava, AK; Srivastava, S; Suprasanna, P; Upadhyay, MK, 2022
)
2.38
"Thiourea is a classical urease inhibitor which is usually used as a positive control, and many N,N'-disubstituted thioureas have been determined as urease inhibitors. "( Synthesis and Structure-Activity Relationship Studies of N-monosubstituted Aroylthioureas as Urease Inhibitors.
Fang, HL; Fu, ZJ; Li, F; Li, K; Li, WY; Liu, L; Ni, WW; Ouyang, H; Xiao, ZP; Ye, YX; Zhu, HL; Zhu, WY; Zou, X, 2021
)
2.29
"Thiourea is a typical nitrification inhibitor that shows a strong inhibitory effect against the biological nitrification process. "( Inhibitory effect of thiourea on biological nitrification process and its eliminating method.
He, L; Jin, X; Wang, Y; Zhang, W, 2017
)
2.22
"Isothioureas are a class of amphiphilic compounds carrying a highly basic isothiourea group of pKa ranging between 10 and 11. "( New benzimidazole-derived isothioureas as potential antileukemic agents--studies in vitro.
Chilmonczyk, Z; Kazimierczuk, Z; Koronkiewicz, M; Romiszewska, A, 2015
)
1.33
"Thiourea (TU) is a thyroid carcinogen which has previously been shown to cause genotoxicity in various test systems in vitro and in vivo. "( S-oxygenation of thiourea results in the formation of genotoxic products.
Andrae, U; Nill, S; Pan, JF; Ziegler-Skylakakis, K, 1998
)
2.08
"Thioureas are an uncommon underrecognized cause of allergic contact dermatitis (ACD). "( Clinical review: thioureas and allergic contact dermatitis.
McCleskey, PE; Swerlick, RA, 2001
)
2.09

Effects

Thiourea (TU) has been found to enhance the stress tolerance of plants in our earlier field trials. Thioureas have been employed as potent hydroxyl radical scavengers and also inhibit production of oxygen free radicals.

ExcerptReferenceRelevance
"Allylthiourea (ATU) has been found to specifically inhibit ammonia oxidation."( Responses of AOA and AOB activity and DNA/cDNA community structure to allylthiourea exposure in the water level fluctuation zone soil.
He, X; Ji, G, 2020
)
1.24
"Thiourea derivatives have been proven to exhibit antifungal and antibacterial effects."( Inhibitory effect of thiourea derivatives on the growth of blue-green algae.
Kasan, NA; Khairul, WM; Manan, H; Yusof, SZM; Zakeri, HA, 2021
)
1.66
"Thiourea derivatives have been reported to possess many biological activities, among them antiviral and antitumoral properties. "( New thiourea and 1,3-thiazolidin-4-one derivatives effective on the HIV-1 virus.
Bielenica, A; Giliberti, G; Jóźwiak, M; Kozioł, AE; Madeddu, S; Materek, IB; Sanna, G; Sawczenko, A; Serra, A; Struga, M, 2017
)
2.46
"Thiourea (TU) has been identified as an effective bioregulator imparting stress tolerance to crops."( Thiourea modulates the expression and activity profile of mtATPase under salinity stress in seeds of Brassica juncea.
D'Souza, SF; Jincy, MG; Mukopadhyaya, R; Ramaswamy, NK; Srivastava, AK, 2009
)
2.52
"Thiourea (TU) has been found to enhance the stress tolerance of plants in our earlier field trials. "( Thiourea orchestrates regulation of redox state and antioxidant responses to reduce the NaCl-induced oxidative damage in Indian mustard (Brassica juncea (L.) Czern.).
D'Souza, SF; Penna, S; Srivastava, AK; Srivastava, S, 2011
)
3.25
"Thiourea (TU) has unique properties that make it an interesting candidate."( Intracochlear administration of thiourea protects against cisplatin-induced outer hair cell loss in the guinea pig.
Ehrsson, H; Ekborn, A; Laurell, G; Miller, J, 2003
)
1.32
"The thiourea group has been exploited to link two or four carbohydrate units at the upper rim of tetrapropoxycalix[4]arene derivatives in the cone conformation. "( Thiourea-linked upper rim calix[4]arene neoglycoconjugates: synthesis, conformations and binding properties.
Casnati, A; Chierici, E; Sansone, F; Ungaro, R, 2003
)
2.32
"Thiourea derivatives have been shown to posses several biological activities. "( In vivo metabolism of N-phenyl-N'-(3,5-dimethylpyrazole-4-yl) thiourea in rats.
Kartal-Aricioğlu, F; Kaymakcioğlu, BK; Rollas, S,
)
1.81
"Thioureas have been employed as potent hydroxyl radical scavengers and also inhibit production of oxygen free radicals. "( Thioureas differentially induce rat hepatic microsomal epoxide hydrolase and rGSTA2 irrespective of their oxygen radical scavenging effect: effects on toxicant-induced liver injury.
Kim, HJ; Kim, SG; Yang, CH, 1999
)
3.19

Actions

Isothiourea DHPB promotes the diastereoselective C-acylation of silyl ketene acetals with anhydrides or benzoyl fluoride. Thioureas inhibit the ATP-induced decrease in turbidity (measured as delta A350) of axonemal suspensions.

ExcerptReferenceRelevance
"Isothiourea DHPB promotes the diastereoselective C-acylation of silyl ketene acetals with anhydrides or benzoyl fluoride, giving 3-acyl-3-aryl or 3-acyl-3-alkylfuranones in excellent yields and stereoselectivities (up to 99:1 dr)."( Isothiourea-mediated stereoselective C-acylation of silyl ketene acetals.
Bragg, RA; Lebl, T; Morrill, LC; Slawin, AM; Smith, AD; Woods, PA, 2010
)
1.6
"Thiourea does not cause increases in DNA above that seen in controls, although thyroid weight increases."( Comparative effects of three goitrogenic treatments on White Leghorn chickens.
Chiasson, RB; Handa, RJ,
)
0.85
"The thioureas inhibit the ATP-induced decrease in turbidity (measured as delta A350) of axonemal suspensions."( Effect of thiourea and substituted thioureas on dynein ATPase and on the turbidity response of Tetrahymena cilia.
Blum, JJ; Hayes, A, 1979
)
1.14
"Thiourea is known to suppress the contractile response of Mytilus anterior byssus retractor muscle and toad sartorious muscle following electrical or chemical stimulation without abolishing of the electrical responses. "( Suppression of crossbridge motions of isolated thick myofilaments in ATP-free medium by thiourea.
Chu, B; Dewey, MM; Fan, SF, 1992
)
1.95
"Thiourea (TU) fails to enhance the incidence of foci deficient in adenosine-5'-triphosphatase (ATPase) either by initiation or by promotion in a rat liver foci bioassay. "( Lack of initiating and promoting activity of thiourea in rat liver foci bioassay.
Deml, E; Oesterle, D, 1988
)
1.98

Treatment

Thiourea did not prevent the Hb transition, which occurred even at concentrations of thyroid hormones that did not permit induction of anatomical metamorphosis. Treatment restored transfectivity to all inactivated fractions, showing that these lesions are reversible.

ExcerptReferenceRelevance
"Thiourea treatment maintained the viability of seeds exposed to NaCl for 6 h. "( Thiourea modulates the expression and activity profile of mtATPase under salinity stress in seeds of Brassica juncea.
D'Souza, SF; Jincy, MG; Mukopadhyaya, R; Ramaswamy, NK; Srivastava, AK, 2009
)
3.24
"Thiourea-treated males had narrowed seminiferous lobules with fewer spermatozoa in testis, very little or no secretory fluid, reduced protein and sialic acid levels in seminal vesicles when compared to controls."( Thiourea-induced thyroid hormone depletion impairs testicular recrudescence in the air-breathing catfish, Clarias gariepinus.
Dutta-Gupta, A; Kagawa, H; Majumdar, KC; Raghuveer, K; Rajasekhar, M; Rasheeda, MK; Senthilkumaran, B; Sreenivasulu, G; Supriya, A; Swapna, I; Tanaka, H, 2006
)
2.5
"In thiourea-treated embryos the opposite effects on the hatching process and on the motility and respiration pattern are registered."( Motility pattern and lung respiration of embryonic chicks under the influence of L-thyroxine and thiourea.
Kugler, W; Petry, H; Wittmann, J, 1983
)
1
"Thiourea treatment restored transfectivity to all inactivated fractions, showing that these lesions are reversible."( The nature of inactivating lesions produced by platinum(II) complexes in phage lambda DNA.
Bonner, WM; Filipski, J; Kohn, KW, 1980
)
0.98
"The thiourea treated mongooses display an increase in the number and size of the calcitonin cells. "( Effect of thiourea on calcitonin cells of the Indian grey mongoose Herpestes edwardsi (Geoffroy).
Das, VK; Swarup, K, 1975
)
1.21
"Thiourea-treated hypothyroid fishes showed significantly decreased level of malic enzyme activity (delta OD/min/mg cytosolic protein or DNA) and cytosolic protein content in liver."( Demonstration of hepatic cytosolic malic enzyme activity as a thyroid hormone sensitive physiologic parameter in a teleost, Heteropneustes fossilis bloch.
De, S; Medda, AK; Ray, AK, 1988
)
1
"Treatment with thiourea, especially when applied at 10 mM, improved the above parameters and induced non-enzymatic and enzymatic antioxidants responsible for antioxidation."( Influence of thiourea application on some physiological and molecular criteria of sunflower (Helianthus annuus L.) plants under conditions of heat stress.
Akladious, SA, 2014
)
1.11
"Treatment with thiourea did not prevent the Hb transition, which occurred even at concentrations of thyroid hormones that did not permit induction of anatomical metamorphosis."( Effect of thyroid hormones on the switch from larval to adult hemoglobin synthesis in the salamander Pleurodeles waltlii.
Duprat, AM; Flavin, M; Rosa, J, 1982
)
0.6

Toxicity

Thiourea is a small, highly diffusible molecule that effectively scavenges toxic oxygen metabolites in vitro and reduces oxidative injury. It is suggested that these changes represent a toxic effect rather than a retardation of pulmonary development.

ExcerptReferenceRelevance
"Reactive oxygen metabolites have been postulated to play an important role in both toxic and ischemic forms of acute renal tubular epithelial injury."( Hydrogen peroxide cytotoxicity in LLC-PK1 cells: a role for iron.
Shah, SV; Walker, PD, 1991
)
0.28
" mortality was high), while the nymphal instars showed an adverse effect on ecdysis and adults which emerged from the treated last nymphal instar were characterized by high mortality, abnormal behaviour and reduced fecundity and viability."( Thiourea as a xenobiotic, showing its adverse effects on mortality, behaviour and metamorphosis and on histopathological and cytological changes in the developing ovaries of Dysdercus similis.
Bhide, M, 1991
)
1.72
" Reserpine did not alter survival time after NMTB or ANTU and did not shift the 14-day LD50 of NMTB."( The involvement of serotonin in the pneumotoxicity induced by N-methylthiobenzamide.
Feny, FJ; Gibbs, LS; Traiger, GJ, 1988
)
0.27
" The optimal toxic effect was obtained when ara-C and cis-DDP were added together."( Kinetics and mechanism of the 1-beta-D-arabinofuranosylcytosine-induced potentiation of cis-diamminedichloroplatinum(II) cytotoxicity.
Drewinko, B; Vadi, H, 1986
)
0.27
" It is suggested that these changes represent a toxic effect of thiourea rather than a retardation of pulmonary development."( Lung development under the influence of thiourea and L-thyroxine. Retarding and toxic effects of thiourea.
Hammel, W; Liebich, HG; Steib, A; Wittmann, J, 1987
)
0.78
" We investigated this newly discovered effect of PTU and its analogues in relation to the toxic effects of Cu ion."( Phenylthiourea enhances Cu cytotoxicity in cell cultures: its mode of action.
Eguchi, G; Masuda, A, 1984
)
0.75
" The substances are approximately 100 mg/kg more toxic for Wistar rats as compared to mice."( [Toxicity of single and multiple administrations of phosphorus-containing isothiuronim derivatives possessing radioprotective properties].
Iakovleva, ND; Zav'ialov, IuV,
)
0.13
"Dimethylthiourea (DMTU) is a small, highly diffusible molecule that effectively scavenges toxic oxygen metabolites in vitro and reduces oxidative injury in many biologic systems."( Toxic effects of dimethylthiourea in rats.
Beehler, CJ; Ely, ME; Reiss, OK; Repine, JE; Rutledge, KS; Shanley, PF; Simchuk, ML, 1994
)
1.03
"For the last 30 years the Joint FAO/WHO Meeting on Pesticide Residues (JMPR) has carried out toxicological evaluations and safety assessments of dithiocarbamate pesticides, continuously adjusting previous appraisals in the light of new data and advances in the understanding of the principles and mechanisms of toxic action of these compounds."( International safety assessment of pesticides: dithiocarbamate pesticides, ETU, and PTU--a review and update.
Almeida, WF; Burin, GJ; Jaeger, RB; Puga, FR; Rahde, AF; Reyes, FG; Schvartsman, S; Vettorazzi, G,
)
0.13
" Ethanol was toxic to HepG2 E9 cells, which express CYP2E1, but not to HepG2 MV5 cells, which do not express CYP2E1."( Ethanol cytotoxicity to a transfected HepG2 cell line expressing human cytochrome P4502E1.
Cederbaum, AI; Wu, D, 1996
)
0.29
" Iron has been implicated to play an important role in several models of tissue injury, presumably through the generation of hydroxyl radicals via the Haber-Weiss reaction or other highly toxic free radicals."( In vitro and in vivo evidence suggesting a role for iron in cisplatin-induced nephrotoxicity.
Baliga, M; Baliga, R; Shah, SV; Ueda, N; Zhang, Z, 1998
)
0.3
"Phencyclidine and other N-methyl-D-aspartate receptor antagonists are toxic to pyramidal neurons in the posterior cingulate/retrosplenial cortex of rat brain."( Acute phencyclidine neurotoxicity in rat forebrain: induction of haem oxygenase-1 and attenuation by the antioxidant dimethylthiourea.
Fix, AS; Rajdev, S; Sharp, FR, 1998
)
0.51
" Similarly, ring fusion of a benzene nucleus to the C-4,5 double bond, forming 2-mercapto-1-methylbenzimidazole, abolished the toxic potency."( Evidence for the involvement of N-methylthiourea, a ring cleavage metabolite, in the hepatotoxicity of methimazole in glutathione-depleted mice: structure-toxicity and metabolic studies.
Kawazoe, S; Mizutani, T; Murakami, M; Shirai, M; Yoshida, K, 2000
)
0.57
" Thiourea (TU), phenylthiourea (PTU), and alpha-naphthylthiourea (ANTU) were toxic to FMO 3 cells but not to parental and FMO 1 clones; 50% toxicity was attained at 1x10(-4) M TU, 5x10(-6) M PTU, and 1x10(-6) M ANTU."( Thiourea toxicity in mouse C3H/10T1/2 cells expressing human flavin-dependent monooxygenase 3.
Crespi, C; Smith, PB, 2002
)
2.67
"Cerebellar granule cells (CGCs) express K+-dependent (NCKX) and K+-independent (NCX) plasmalemmal Na+/Ca2+ exchangers which, under plasma membrane-depolarizing conditions and high cytosolic [Na+], may reverse and mediate potentially toxic Ca2+ influx."( In depolarized and glucose-deprived neurons, Na+ influx reverses plasmalemmal K+-dependent and K+-independent Na+/Ca2+ exchangers and contributes to NMDA excitotoxicity.
Czyz, A; Kiedrowski, L, 2002
)
0.31
" Repeated intravaginal exposure of CD-1 mice to increasing concentrations of PHI-346 for 13 weeks had no adverse effect on their subsequent reproductive capability, perinatal outcome, growth, and development of offspring."( A 13-week subchronic intravaginal toxicity study of the novel broad-spectrum anti-HIV and spermicidal agent, N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (PHI-346) in mice.
D'Cruz, OJ; Uckun, FM; Waurzyniak, B,
)
0.33
" We tested whether the NCX or NCKX family of exchangers contributes most to the toxic NMDA-induced Ca(2+) influx in depolarized neurons."( Differential contribution of plasmalemmal Na/Ca exchange isoforms to sodium-dependent calcium influx and NMDA excitotoxicity in depolarized neurons.
Baranauskas, G; Czyz, A; Kiedrowski, L; Li, XF; Lytton, J, 2004
)
0.32
"Metals and polycyclic aromatic hydrocarbons (PAHs) are known to be toxic to plants."( Biochemical responses of the aquatic higher plant Lemna gibba to a mixture of copper and 1,2-dihydroxyanthraquinone: synergistic toxicity via reactive oxygen species.
Babu, TS; Greenberg, BM; Tripuranthakam, S, 2005
)
0.33
" In contrast to ThU SA was considered safe for drought-stress alleviation in crop plant agriculture."( Screening the bio-safety of wheat produced from pretreated grains to enhance tolerance against drought using physiological and spectroscopic methods.
Abdelkader, AF; Abo-Aly, MM; Attia, MS; Bakir, EM; Hassanein, RA, 2010
)
0.36
" The multiple-dose pharmacokinetics of the amuvatinib LSC 300 mg administered every 8 h exhibited improved accumulation compared with the 12-h regimens and achieved presumed therapeutic level safely with no serious or severe adverse events reported."( Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers.
Azab, M; Choy, G; Collier, J; Fine, G; Joshi-Hangal, R; Kissling, J; Oganesian, A; Rasmussen, S; Redkar, S; Sahai, A, 2012
)
0.38
" We have shown that 1 when photoactivated accumulates in tumor cells and binds strongly to nuclear DNA under conditions in which it is toxic to tumor cells."( Interactions of DNA with a new platinum(IV) azide dipyridine complex activated by UVA and visible light: relationship to toxicity in tumor cells.
Brabec, V; Farrer, NJ; Kasparkova, J; Novakova, O; Pracharova, J; Sadler, PJ; Stepankova, J; Zerzankova, L, 2012
)
0.38
" Administration of this drug, often in a chronic manner, is associated with several adverse drug reactions in humans, including life-threatening hepatotoxicity."( Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes.
Babaei, H; Eghbal, M; Heidari, R, 2013
)
0.39
" Among evaluated compounds, derivatives 9w, 9r and 9k had safe profile regarding ATP production and cell viability."( Synthesis and evaluation of new pyridyl/pyrazinyl thiourea derivatives: Neuroprotection against amyloid-β-induced toxicity.
Elkamhawy, A; Hassan, AHE; Lee, J; Pae, AN; Paik, S; Park, BG; Park, JE; Roh, EJ, 2017
)
0.71
" Acute toxicity study revealed that LD50 of compound (1) and (3) is 120 mg/kg body weight."( Synthesis, acute toxicity, analgesic activity and cytotoxicity of Some bisthiourea derivatives.
Hussain, H; Shah, SWA; Shoaib, M; Ullah, A; Umar, MN, 2017
)
0.69
" Interaction with AhR for the studied compounds is impossible for steric reasons and, as a consequence, toxic effects on the immune and other organ systems associated with the activation of the AhR signaling pathway are excluded."( In silico toxicity evaluation of Salubrinal and its analogues.
Kharchenko, AV; Kiselev, VV; Zadorozhnii, PV, 2020
)
0.56
" The most common adverse drug reactions (ADRs) were neutrophil count decreased (75%), aspartate aminotransferase increased (50%), and platelet count decreased (50%); 85% of patients had grade ≥ 3 ADRs."( Efficacy and safety of TAS-115, a novel oral multi-kinase inhibitor, in osteosarcoma: an expansion cohort of a phase I study.
Doi, T; Imura, Y; Iwata, S; Kawai, A; Kitano, S; Kobayashi, E; Naito, Y; Naka, N; Nakatani, F; Outani, H; Shimomura, A; Takahashi, S; Tamiya, H; Yamamoto, N; Yonemori, K, 2021
)
0.62

Pharmacokinetics

The purpose of the present study was to examine the pharmacokinetic features and tissue distribution of N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) The compounds showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay.

ExcerptReferenceRelevance
" A number of pharmacokinetic parameters were calculated from serum concentration data in rabbits and humans."( Liquid chromatographic determination of noxytiolin and 1-methyl-2-thiourea in serum: application to pharmacokinetic studies in rabbits and humans.
Bigot, MC; Bricard, H; Debruyne, D; Moulin, MA, 1985
)
0.51
"The purpose of the present study was to examine the pharmacokinetic features and tissue distribution of N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240), a novel non-nucleoside inhibitor of HIV reverse transcriptase with potent anti-viral activity against AZT-sensitive as well as multidrug-resistant HIV-1 strains."( Evaluation of the pharmacokinetic features and tissue distribution of the potent nonnucleoside inhibitor of HIV-1 reverse transcriptase, N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) with an analytical HPLC method.
Chen, CL; Uckun, FM, 1999
)
0.69
"A sensitive and accurate high performance liquid chromatography (HPLC)-based quantitative detection method was established to measure concentrations of HI-240 in pharmacokinetic studies."( Evaluation of the pharmacokinetic features and tissue distribution of the potent nonnucleoside inhibitor of HIV-1 reverse transcriptase, N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) with an analytical HPLC method.
Chen, CL; Uckun, FM, 1999
)
0.49
"HI-240 had an elimination half-life of 78."( Evaluation of the pharmacokinetic features and tissue distribution of the potent nonnucleoside inhibitor of HIV-1 reverse transcriptase, N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) with an analytical HPLC method.
Chen, CL; Uckun, FM, 1999
)
0.49
"The HPLC-based accurate and precise analytical detection method and pilot pharmacokinetic studies described herein provide the basis for advanced preclinical pharmacodynamic studies of HI-240."( Evaluation of the pharmacokinetic features and tissue distribution of the potent nonnucleoside inhibitor of HIV-1 reverse transcriptase, N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) with an analytical HPLC method.
Chen, CL; Uckun, FM, 1999
)
0.49
" The purpose of the present study was to examine in vivo toxicity, pharmacokinetic features and tissue distribution of HI-236 in mice."( In vivo toxicity, pharmacokinetic features and tissue distribution of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236), a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Chelstrom, L; Chen, CL; Uckun, FM; Venkatachalam, TK; Waurzyniak, B, 2001
)
0.52
" Serial samples of blood were collected from four animals and CSF samples from three animals for pharmacokinetic studies."( Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates.
Baxter, PA; Blaney, SM; Choy, G; Dauser, RC; Gibson, BW; Inloes, R; McGuffey, LM; Nuchtern, JG; Redkar, S; Shi, C; Thompson, PA, 2011
)
0.37
" The half-life of MP470 in the plasma was 11."( Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates.
Baxter, PA; Blaney, SM; Choy, G; Dauser, RC; Gibson, BW; Inloes, R; McGuffey, LM; Nuchtern, JG; Redkar, S; Shi, C; Thompson, PA, 2011
)
0.37
" Herein we report the synthesis, structure-activity relationships (SARs), and pharmacokinetic properties of this new class of thiourea compounds that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay."( Synthesis, activity, and pharmacokinetic properties of a series of conformationally-restricted thiourea analogs as novel hepatitis C virus inhibitors.
Chao, YS; Chern, JH; Hsu, SJ; Kang, IJ; Lee, CC; Lee, YC; Wang, JC; Wang, LW; Wu, YS; Yeh, TK; Yueh, A, 2010
)
0.79
"Three studies were conducted in a total of 58 healthy subjects: a food-effect study using amuvatinib DPC, a single-dose pharmacokinetic study comparing amuvatinib DPC to a new lipid-suspension capsules (LSC), and a multiple-dose pharmacokinetic study using amuvatinib LSC."( Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers.
Azab, M; Choy, G; Collier, J; Fine, G; Joshi-Hangal, R; Kissling, J; Oganesian, A; Rasmussen, S; Redkar, S; Sahai, A, 2012
)
0.38
"  Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h."( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics.
Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
" In this study, we evaluate whether MP470, a novel receptor tyrosine kinase inhibitor alone or in combination with Erlotinib has inhibitory effect on prostate cancer in vitro and in vivo."( MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer.
Bearss, D; Cooke, LS; Croce, KD; Mahadevan, D; Qi, W; Riley, C; Saldanha, JW; Stejskal, A, 2009
)
0.35
" Additive effects on both cytotoxicity and induction of apoptosis were observed when LNCaP were treated with MP470 in combination with Erlotinib."( MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer.
Bearss, D; Cooke, LS; Croce, KD; Mahadevan, D; Qi, W; Riley, C; Saldanha, JW; Stejskal, A, 2009
)
0.35
"To study the protective effect of mitochondrial ATP-sensitive K(+) channel (mitoK(ATP) channel) opener, nicorandil, combined with Na(+)/Ca(2+) exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in isolated rat hearts; the isolated rat heart was perfused by modified Langendorff device, after 15-min balanced perfusion, 45-min ischemia (about left and right coronary perfusion flow reduced to 5% of the original irrigation flow), and 2-h reperfusion were performed."( The protective effect of mitochondrial ATP-sensitive K+ channel opener, nicorandil, combined with Na+/Ca2+ exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in rat.
Jia, D, 2011
)
0.37
" Salubrinal, an agent that can sustain the activity of a key regulator of the ISR eIF2α, further increased the expression of ATF3 and demonstrated synergistic cytotoxicity in combination with lovastatin in SCC cells."( Lovastatin-induced apoptosis is mediated by activating transcription factor 3 and enhanced in combination with salubrinal.
Corsten, M; Dimitroulakos, J; Gorn-Hondermann, I; Johnson-Obeseki, S; Ma, L; Niknejad, N; Zahr, S, 2014
)
0.4
"Amuvatinib was well tolerated, modulated RAD51, and showed antitumor activity when combined with paclitaxel/carboplatin and carboplatin/etoposide in NE, NSCLC, and SCLC tumors."( Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors.
Azab, M; Bristow, R; Choy, G; Gordon, M; Kapoor, N; Mita, M; Oganesian, A; Redkar, S; Rosen, L; Sahai, A; Taverna, P; Tolcher, AW, 2014
)
0.4
"To explore therapeutic effects and underlying mechanism of Salubrinal combined with Ulinastatin (UTI) on acute Paraquat (PQ) poisoning."( Therapeutical effects and mechanism of salubrinal combined with ulinastatin on treating paraquat poisoning.
Guo, H; Jiang, C; Sun, X, 2014
)
0.4
" Lastly, doses of proteasome inhibitors that are inadequate to block the activity of the proteasomes, caused cell death when combined with mifepristone; this phenotype was accompanied by accumulation of poly-ubiquitinated proteins denoting proteasome inhibition."( Mifepristone increases mRNA translation rate, triggers the unfolded protein response, increases autophagic flux, and kills ovarian cancer cells in combination with proteasome or lysosome inhibitors.
Callegari, EA; Chien, J; Drappeau, DD; Eyster, KM; Gamarra-Luques, CD; Goyeneche, AA; Hapon, MB; Knapp, JR; Pan, B; Srinivasan, R; Telleria, CM; Terpstra, EJ; Wang, X; Zhang, L, 2016
)
0.43
" And, DPB inhibited A549 cell growth more effectively in combination with autophagy inhibitors 3-MA (5 mmol/L) or 3-benzyl-5-((2-nitrophenoxy) methyl)-dihydrofuran-2(3H)-one (3BDO, 30 μmol/L)."( HSP90 inhibitor DPB induces autophagy and more effectively apoptosis in A549 cells combined with autophagy inhibitors.
Li, K; Su, L; Zhao, B; Zhao, Y, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" When (35S)PR solution was injected through a tracheal cannula in control animals and the percentage of the tracheal cannula in control animals and the percentage of the dose unabsorbed plotted semilogarithmically against time, an apparent first-order absorption rate was obtained."( Effect of pulmonary edema on drug transport and binding in rat lung.
Gardiner, TH; Goodman, FR, 1977
)
0.26
" ratios indicate that, relative to ranitidine, the bioavailability of AY-29,315 by the oral route was low, particularly in the dog."( Antisecretory and antiulcer activities of a potent new histamine H2-receptor antagonist with an intermediate duration of action.
Borella, L; Failli, A; Grimes, D; Mir, GN; Rimele, TJ; Russell, J, 1988
)
0.27
" Bioavailability and/or biotransformation are the factors most likely to account for the differences observed between species, and between in vivo and in vitro studies for this long-acting antisecretory agent."( In vivo and in vitro effects of CM 57755, a new gastric antisecretory agent acting on histamine H2 receptors.
Aureggi, G; Bianchetti, A; Carminati, P; Lavezzo, A; Manzoni, L; Nisato, D, 1984
)
0.27
" The intraperitoneal bioavailability was estimated at 23."( Evaluation of the pharmacokinetic features and tissue distribution of the potent nonnucleoside inhibitor of HIV-1 reverse transcriptase, N-[2-(2-fluorophenethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-240) with an analytical HPLC method.
Chen, CL; Uckun, FM, 1999
)
0.49
" The effective combinations (L-TC + DOX, NAC + DOX, NAC + DMTU, NAC + HMT, NC + DOX) combined agents, reducing the bioavailability of the mustard with compounds possibly acting on the consequences of alkylation."( Efficient protection of human bronchial epithelial cells against sulfur and nitrogen mustard cytotoxicity using drug combinations.
Baeza-Squiban, A; Calvet, J; Marano, F; Rappeneau, S, 2000
)
0.31
" Through an integrated effort involving synthesis, docking studies, and biological and pharmacokinetic evaluation, we investigated the structural dependence of the poor bioavailability and rapid clearance within the thioureidic series of antivirals."( Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Aiello, F; Armaroli, S; Bergamini, A; Bolacchi, F; Bongiovanni, B; Caccia, S; Campiani, G; Capozzi, M; Coletta, M; Fabbrini, M; Garofalo, A; Greco, G; Guiso, G; Maga, G; Marini, S; Morelli, E; Nacci, V; Novellino, E; Ramunno, A; Spadari, S; Ventura, L, 2001
)
0.62
" The intraperitoneal bioavailability was estimated at 42."( In vivo toxicity, pharmacokinetic features and tissue distribution of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236), a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Chelstrom, L; Chen, CL; Uckun, FM; Venkatachalam, TK; Waurzyniak, B, 2001
)
0.52
"We previously reported a potent calpain inhibitor 1 (SJA6017, N-(4-fluorophenyl)-l-valyl-l-leucinal), which displayed relatively low oral bioavailability (BA)."( Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivatives.
Inoue, J; Miyashita, H; Nakamura, M; Sakai, O; Shirasaki, Y; Yamaguchi, M, 2006
)
0.33
" Here the identification of a novel oleic acid containing lead formulation of HI-443 is described which resulted in a approximately 10-fold improvement of its oral bioavailability yielding 10-fold higher systemic exposure levels in mice."( Improved oral bioavailability of anti-HIV agent N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443) in a novel lipophilic formulation.
Erbeck, D; Qazi, S; Tibbles, H; Uckun, FM; Venkatachalam, TK, 2007
)
0.56
" Planned linear contrasts were performed to identify which formulations showed the highest bioavailability at 10, 30, 60 min and at all time points relative to DMSO alone."( In vivo pharmacokinetics and toxicity of a novel hydrophilic oral formulation of the potent non-nucleoside reverse transcriptase inhibitor compound N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443).
Erbeck, D; Qazi, S; Tibbles, H; Uckun, FM; Venkatachalam, TK, 2007
)
0.53
" This compound displayed oral bioavailability and analgesic activity."( 2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs.
Chiba, H; Hasegawa, Y; Hattori, M; Iwamoto, Y; Kai, H; Koike, K; Koriyama, Y; Morioka, Y; Okamoto, K; Shinohara, S; Takahashi, K; Tanimoto, N, 2008
)
0.35
"5nM, EC(2xPT)=32muM) as a selective, orally bioavailable FXa inhibitor with an excellent in vitro liability profile, favorable pharmacokinetics and pharmacodynamics in animal models."( Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Atwal, KS; Bisaha, SN; Chong, S; Hartl, KS; Kish, K; Klei, HE; Li, C; Liu, EC; O'Connor, SP; Pudzianowski, AT; Schumacher, WA; Seiler, SM; Shi, M; Shi, Y; Sitkoff, D; Stein, PD; Steinbacher, TE; Yanchunas, J; Zhang, J, 2009
)
0.35
" Previously, we showed that the selective iNOS inhibitor S,S'-1,4-phenylenebis(1,2-ethanediyl)bis-isothiourea (PBIT) caused significant inhibition of colon carcinogenesis induced by azoxymethane (AOM), although it did not completely abrogate NO production due to the exogenous bioavailability of NO and NO generation by eNOS in tumor tissues."( Chemopreventive effects of PBI-Se, a selenium-containing analog of PBIT, on AOM-induced aberrant crypt foci in F344 rats.
Amin, S; Choi, CI; Desai, D; Janakiram, NB; Mohammed, A; Rao, CV; Ravillah, D; Zhang, Y, 2013
)
0.61
"  Pharmacokinetic analysis of Inh-1 revealed an absolute bioavailability (F) of 21% and a short t1/2 of <1 h."( Bacterial β-glucuronidase inhibition protects mice against enteropathy induced by indomethacin, ketoprofen or diclofenac: mode of action and pharmacokinetics.
Boelsterli, UA; Fujimoto, K; Lee, KK; Redinbo, MR; Saitta, KS; Zhang, C, 2014
)
0.4
" Recently, the next-generation orally bioavailable irreversible proteasome inhibitor oprozomib was developed."( Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma.
Bogaerts, E; Coucke, C; Devisscher, L; Geerts, A; Laukens, D; Libbrecht, L; Paridaens, A; Raevens, S; Van Steenkiste, C; Van Vlierberghe, H; Vandewynckel, YP; Vandierendonck, A; Verhelst, X, 2016
)
0.43
" For example, a reaction of ITC with nucleophilic amino acid side chains of proteins such as cysteine and lysine can occur, reducing the bioavailability of indispensable amino acids and protein functions may be altered."( Determination of isothiocyanate-protein conjugates in milk and curd after adding garden cress (Lepidium sativum L.).
Hanschen, FS; Kühn, C; Rohn, S; von Oesen, T, 2018
)
0.48
" The physicochemical properties of the proposed 2-amino-5-carboxamide thiazole derivatives were calculated and showed potential to be an reasonable oral bioavailability drug properties as determined by Lipinski's Rule."( Synthesis of 2-Amino-5-Carboxamide Thiazole Derivatives via Dehydrative Cyclization of Thiourea Intermediate Resin on Solid Phase.
Gong, YD; Han, SY; Kim, YJ; Kwon, HJ, 2019
)
0.74
" Under the alternating magnetic field (AMF), the specific absorption rate (66."( A novel biocompatible core-shell magnetic nanocomposite based on cross-linked chitosan hydrogels for in vitro hyperthermia of cancer therapy.
Asgharnasl, S; Eivazzadeh-Keihan, R; Hajizadeh, Z; Maleki, A; Radinekiyan, F; Salimi Bani, M, 2019
)
0.51
" This process effectively reduced Cd bioavailability in the soil system."( Remediation of Soil Polluted with Cd in a Postmining Area Using Thiourea-Modified Biochar.
Chen, F; Hu, G; Ma, J; Yu, R; Zhang, S; Zhu, Y, 2020
)
0.8
" Furthermore, penetration of endocrine disruptors into aquatic organisms especially in amphibians is even easier because of more permeable skin, resulting in high bioavailability and bioaccumulation of chemicals."( Changes in thyroid histomorphology and thyroglobulin immunostaining upon exposure to thiourea in Triturus newts.
Ajduković, M; Cvijanović, M; Filipović, B; Šošić-Jurjević, B; Vučić, T, 2022
)
0.95

Dosage Studied

Fish with a low dosage of exogenous triiodothyronine and those treated with thiourea exhibited retarded development of bony plates.

ExcerptRelevanceReference
" Metamide, at doses of 3 X 10(-6)M, and 3 X 10(-5)M, caused a parallel displacement of the histamine dose-response curve, indicating competitive antagonism."( A quantitative study of metiamide, a histamine H2-antagonist, on the isolated whole rat stomach.
Bunce, KT; Parsons, ME, 1976
)
0.26
"Cumulative dose-response curves for histamine were determined on acid secretion from the isolated guinea pig gastric mucosa."( Analysis of the actions of cimetidine and metiamide on gastric acid secretion in the isolated guinea pig gastric mucosa.
Olbe, L; Ryberg, B; Sjöstrand, SE, 1977
)
0.26
" A dose-response curve revealed that a 50-mg dose of metiamide was required to suppress food-stimulated acid secretion by 50%."( The effect of an H2-receptor antagonist on food-stimulated acid secretion, serum gastrin, and gastric emptying in patients with duodenal ulcers. Comparison with an anticholinergic drug.
Bailey, BA; Fordtran, JS; Richardson, CT; Walsh, JH, 1975
)
0.25
" Reciprocal plots (rate response versus histamine concentration) of dose-response curves are linear for both rabbit and guinea pig atria."( A Quantitative study of histamine H2-receptor bockade by burimamide in isolated artica.
Coret, IA; Hughes, MJ, 1975
)
0.25
" The effect of a specific histamine H2-receptor antagonist, metiamide, on the acid dose-response curves for pentagastrin or methacholine was studied in rats provided with Heidenhain pouches."( Displacement by metiamide of the dose-response curves to pentagastrin and methacholine in the conscious rat.
Lundell, L, 1975
)
0.25
" Endotoxin treatment was associated with increased activity of the protectant antioxidant enzyme systems of the lung in an apparent dose-response manner."( Endotoxin protection against oxygen-induced acute and chronic lung injury.
Frank, L; Roberts, RJ, 1979
)
0.26
"The clinical, endoscopic, and biochemical effects of metiamide, a histamine H2-receptor antagonist, in therapeutic dosage have been studied in a 28-day open trial in patients with duodenal ulcer disease."( Early clinical experience with metiamide, a histamine H2-receptor antagonist, in patients with duodenal ulcer.
Dale, G; Reed, JD; Thompson, MH; Venables, CW, 1975
)
0.25
" To resolve this conflict experiments were conducted to calibrate absolutely the dose-response curves for the radiation damage, and to measure the force production and the mechanochemical energy conversion after irradiation in bull sperm."( Radiation damage to bull sperm motility. III. Further x-ray studies.
Rikmenspoel, R, 1975
)
0.25
"0 mg/kg dosage group, however, demonstrated significantly fewer ulcers than the saline animals and the lesions that did occur were significantly smaller than those noted in the control animals."( The effects of metiamide on the "activity-stress" ulcer in rats.
Cash, RJ; Houser, VP; van Hart, DA, 1975
)
0.25
" Rats maintained under these conditions were treated with DMTU at different concentrations and dosing schedules and then exposed for various times to intense visible light, either intermittently (1 hr light and 2 hr dark) or continuously."( Protection by dimethylthiourea against retinal light damage in rats.
Blanks, JC; Darrow, RM; Jiang, YI; Marak, GE; Organisciak, DT, 1992
)
0.6
" Daily dosage levels (mg/kg/day) were ETU at 0, 15, 25 and 35; DMT at 0, 15, 25, 50, 100, and 200; DBT at 0, 15, 25, 50, 100, and 200; and DPT at 0, 25, 50, 100, and 200."( Difference in the developmental toxicity of ethylenethiourea and three N,N'-substituted thiourea derivatives in rats.
de Ceaurriz, J; Langonne, I; Sabate, JP; Saillenfait, AM, 1991
)
0.53
" All motor endpoints were decreased in a dosage- and time-dependent manner; the higher the dosage the longer the effects lasted."( The effects of 2,4-dithiobiuret on sensory and motor function.
Boyes, WK; Crofton, KM; Dean, KF; Hamrick, RC, 1991
)
0.28
" The following methods were used: a) gastric acid hypersecretion induced by histamine and carbachol in the pylorus-ligated rat preparation; b) contractile dose-response curves to histamine and carbachol in the guinea pig ileum; c) dimaprit-stimulated guinea pig atrium in vitro."( Mechanism of action of doxepin in the treatment of chronic urticaria.
Almeida, L; Figueiredo, A; Gonçalo, M; Poiares-Baptista, A; Ribeiro, CA; Teixeira, F, 1990
)
0.28
" It was of interest to determine whether subtle changes in neuromuscular transmission are produced by DTB under dosing conditions in which gross muscle weakness is not apparent."( Acute alterations in murine neuromuscular transmission following exposure to a nonparalytic dose of dithiobiuret.
Atchison, WD; Spitsbergen, JM, 1990
)
0.28
" to rats for 4 days at a daily dosage of 1 mg/kg and the development of the lesion associated with neuromuscular dysfunction studied in hindlimb lumbrical muscles."( Dithiobiuret neurotoxicity: an ultrastructural investigation of the lesion in preterminal axons and motor endplates in the rat lumbrical muscle.
Jones, HB, 1989
)
0.28
" Omeprazole caused a non-competitive inhibition of the dose-response curve to dimaprit, whereas famotidine induced a parallel shift to the right without depressing the maximum response."( Antisecretory activity of omeprazole in the conscious gastric fistula cat: comparison with famotidine.
Bertaccini, G; Coruzzi, G,
)
0.13
" According to the two dosing schedules adopted to evaluate the duration of action, mifentidine, compared to cimetidine and ranitidine, required considerably lower oral dosages to display its protective effect."( Cimetidine, ranitidine and mifentidine in specific gastric and duodenal ulcer models.
Cereda, E; Del Soldato, P; Donetti, A; Ghiorzi, A, 1985
)
0.27
" In the second set of experiments, equiactive doses (that is the respective ED50s calculated from the previously established dose-response curves) of all the compounds were infused during dimaprit-induced acid hypersecretion, in order to evaluate their duration of action."( Effect of the new H2-receptor antagonist mifentidine on gastric acid secretion in the cat: comparison with cimetidine and ranitidine.
Bertaccini, G; Scarpignato, C; Tangwa, M; Tramacere, R, 1985
)
0.27
" the respective ED50s calculated from the previously established dose-response curves) of all the three antagonists was completely different."( The effect of the new H2-receptor antagonist mifentidine on gastric secretion, gastric emptying and experimental gastric and duodenal ulcers in the rat: comparison with cimetidine and ranitidine.
Del Soldato, P; Scarpignato, C; Tangwa, M; Tramacere, R, 1986
)
0.27
" The maximum pepsin output obtained from a set of complete dose-response curves of dimaprit was not statistically different from basal values."( Comparison of the effects of structurally different H2-antagonists on acid and pepsin activity stimulated by dimaprit in conscious cats.
Barocelli, E; Chiavarini, M; Impicciatore, M; Molina, E; Morini, G; Plazzi, PV, 1985
)
0.27
" Intravenous infusion of CM 57755 induced a parallel shift to the right of the dimaprit dose-response curve."( Inhibition of dimaprit- and pentagastrin-induced gastric acid secretion in cats by the new histamine H2 antagonist, CM 57755.
Bianchetti, A; Lavezzo, A; Manara, L; Manzoni, L, 1986
)
0.27
"32 mumol kg-1 h-1) caused a parallel displacement of the dose-response curve to dimaprit to the right, without reducing the maximum response to the stimulant, thus behaving as a competitive antagonist, like ranitidine."( Inhibitory effect of famotidine on cat gastric secretion.
Bertaccini, G; Coruzzi, G; Dobrilla, G; Noci, MT, 1986
)
0.27
" Dose-response curves to dimaprit in stimulating gastric secretion were displaced to the right in a dose-related fashion by both drugs."( Kinetic analysis of the interaction of mifentidine with gastric H2-receptors in the conscious dog.
Giachetti, A; Pagani, F; Zecca, M, 1987
)
0.27
" The muscarinic antagonist atropine, 1 microM, and the beta 2-adrenoceptor antagonist propranolol, 10 microM, had no effect on the dose-response curve for dimaprit-induced relaxation of the lung strip."( A study of the histamine H2-receptor mediating relaxation of the parenchymal lung strip preparation of the guinea-pig.
Foreman, JC; Rising, TJ; Webber, SE, 1985
)
0.27
" H1-agonists (2-methylHi and 2-thiazolylethylamine) also depressed the avoidance response; their dose-response lines run parallel to that of Hi."( The effects of histamine and some related compounds on conditioned avoidance response in rats.
Akahori, H; Kamei, C; Kitazumi, K; Tasaka, K, 1985
)
0.27
" In an apparently all-or-none manner, both caused a sinistral shift in dose-response curves for the phasic component of the contractile response to histamine at H1 receptors on the ileum."( Metronidazole and 5-aminosalicylic acid enhance the contractile activity of histaminergic agonists on the guinea-pig isolated ileum.
Barker, LA; Winbery, SL, 1986
)
0.27
" Conversely, following potentiation of the response to histamine with DTT, exposure of the tissue to desensitizing concentrations of histamine resulted in a dextral shift of the dose-response curve (dose ratio = 39."( Selective enhancement of histamine H1-receptor responses in guinea-pig ileal smooth muscle by 1,4-dithiothreitol.
Donaldson, J; Hill, SJ, 1986
)
0.27
" The selective histamine H1-receptor antagonist chlorpheniramine shifted the dose-response curves of histamine and 2-PEA for inducing vasoconstriction to the right."( Characteristics of histamine receptors in the isolated and perfused canine coronary arteries.
Chiba, S; Nakane, T, 1987
)
0.27
" Since DMTU not only scavenges O2 metabolites but is also consumed in a dose-response manner following reaction with hydrogen peroxide (H2O2) in vitro, we wondered whether DMTU would also be consumed by O2 metabolites in biological systems and if DMTU consumption would then reflect O2 metabolite concentrations and O2 metabolite-mediated injury."( Dimethylthiourea consumption reflects H2O2 concentrations and severity of acute lung injury.
Jackson, JH; Parker, NB; Repine, JE; Ryan, JW; White, CW, 1985
)
0.7
" A non-linear dose-response relationship with respect to enzyme activity was observed with different doses of T3."( Induction of hepatic mitochondrial alpha-glycerophosphate dehydrogenase by L-triiodothyronine in Singi fish (Heteropneustes fossilis Bloch).
De, S; Ghosh, N; Ghosh, RK; Medda, AK; Ray, AK, 1987
)
0.27
" Clinical inspection, weight gain, haematological findings, blood sugar, serum transaminases, properties of urine and faeces, carcass examination and histological study (internal organs, endocrine glands, skeletal muscle) showed that the 1 mg/kg dosage had no toxic effect."( [Effect of long-term application of SUISYNCHRON-premix on swine].
Chemnitius, KH; Oettel, M; Schimke, E; Zieger, M, 1974
)
0.25
"Twelve groups of German Edelschwein were given the recommended dosage of metallibure zinc complex (SUISYNCHRON) or 5 and 10 times this dosage."( [Pharmacologic-endocrinological findings in animal experiments with TURISYNCHRON and SUISYNCHRON. 4. Analysis of residuals in pig carcasses].
Chemnitius, KH; Claussen, C; Grass, M; Räche, K; Steiner, G, 1974
)
0.25
" Pretreatment of parenchymal strips with cimetidine or YM-11170, H2-receptor antagonists, resulted in a parallel shift of the dimaprit dose-response curve to the right."( Effects of histamine H2-receptor agonists and antagonists on isolated guinea-pig airway muscles.
Tomioka, K; Yamada, T, 1982
)
0.26
" Using quantitative cytochemistry of CA activity in guinea-pig oxyntic cells, we compared the dose-response relationships (1."( Evidence for histamine H1 and H2 receptors in guinea-pig oxyntic cells.
Heldsinger, AA; Skoglund, ML; Vinik, AI, 1983
)
0.27
" This study serves to quantitate the pharmacologic effects of several agents on anti-IgE-mediated histamine release from dispersed human lung mast cells and has further suggested that the dispersed cell system is similar to the standard chopped lung system in dose-response relationships, kinetics, and pharmacologic modulation."( Dispersed human lung mast cells. Pharmacologic aspects and comparison with human lung tissue fragments.
Lichtenstein, LM; MacGlashan, DW; Newball, HH; Peters, SP; Schleimer, RP; Schulman, ES, 1982
)
0.26
" The H1-antagonist chlorpheniramine shifted to the right the dose-response curves to histamine and to 2-aminoethylthiazole with the kinetics of the competitive antagonism."( Histamine receptors in the human ureter.
Bertaccini, G; Bezzi, E; Potenzoni, D; Zappia, L, 1983
)
0.27
" The dose-response curves of inhibition of mitogen-induced lymphocyte activation for chloroquine and methylamine are very steep and are similar to the dose-response curves obtained with dimaprit and nordimaprit, but very different from the flat dose-response curves previously described for histamine."( A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen-induced lymphocyte activation.
Dale, MM; Ladd, R, 1984
)
0.27
" Dose and dosing regimen dependent changes in tissue distribution are evident for most tissues with the thyroid gland, lung, stomach and fat being the most affected."( Effects of dose and dosing regimen on tissue distribution and elimination kinetics of [14C] dithiobiuret in rats.
Atchison, WD; Dickins, J; Peterson, RE; Porter, WR, 1983
)
0.27
" TSH administration to embryos and chicks resulted in similar time-course and dose-response characteristics, as judged by the thyroid 32P uptake response."( Responses to thyrotropin during development in Japanese quail.
Hughes, TE; McNabb, FM; Stanton, FW; Weirich, RT, 1984
)
0.27
" The dose-response curve to histamine was displaced to the right by mepyramine and further to the right by mepyramine plus cimetidine."( Evidence for both histamine H1- and H2-receptors in the gastric vasculature of the cat.
Harvey, CA; Owen, DA; Shaw, KD, 1980
)
0.26
" The dose-response curves for respective components of the salivary and vasodilator responses to PEA were parallel with the corresponding curves for histamine and in producing these responses PEA was about 40 times less potent than histamine on a molar basis."( Characterization of neuronal and vascular histamine receptors mediating the salivary and vasodilator responses to histamine of the dog submandibular gland.
Nunoki, K; Shimizu, T; Taira, N, 1981
)
0.26
" If the mice were dosed daily (i."( Effect of histamine agonists and antagonists on the production of murine reaginic antibodies.
Baker, AP; Chakrin, LW; Holden, DA; Smith, WJ; Sung, CP, 1981
)
0.26
"The present work investigates (a) the modification by pretreatment with selective H1- and H2-receptor antagonists on the dose-response curves (DRC) to histamine for heart rate, blood pressure, renal arterial blood flow and renal vascular resistance in anesthetized dogs, and (b) the characteristics of the DRC to histamine in canine isolated renal artery."( Histamine H1- and H2-receptors in canine renal artery in vivo and in vitro.
Bedate, H; Esplugues, J; Moragues, A; Morcillo, E, 1981
)
0.26
" These women may require a greater dosage of thyroid hormone during pregnancy."( Thyroid disease in pregnancy. ACOG Technical Bulletin Number 181--June 1993.
, 1993
)
0.29
" SMTC did not modify the NaCN dose-response curve."( Nitric oxide synthase isoforms and peripheral chemoreceptor stimulation in conscious rats.
Gozal, D; Gozal, E; Gozal, YM; Torres, JE, 1996
)
0.29
" The results indicate that dimaprit, an H2 agonist, facilitated retention (25 and 50 pg) with a U-shaped dose-response curve typical of drugs acting at postsynaptic receptors."( Effect of histamine H2 and H3 receptor modulation in the septum on post-training memory processing.
Flood, JF; Morley, JE; Uezu, K, 1998
)
0.3
"DNA single-strand breaks (and/or alkali-labile sites) induced by Cr(VI) were evaluated with the alkaline single cell gel electrophoresis (SCG) (Comet) assay in five organs (liver, kidney, spleen, lung, and brain) of male mice dosed with K(2)Cr(2)O(7) (20 mg Cr/kg) by a single ip injection in vivo, and the formation of paramagnetic Cr(V) in these organs was investigated by electron spin resonance (ESR) spectrometry."( Detection of dichromate (VI)-induced DNA strand breaks and formation of paramagnetic chromium in multiple mouse organs.
Furukawa, Y; Ishii, M; Kashimoto, T; Nishimura, Y; Sasaki, YF; Sugiyama, M; Susa, N; Ueda, J; Ueno, S; Yasuno, M; Yokoi, K, 2001
)
0.31
" Placebo control and PHI-346 dosed female CD-1 mice were mated with untreated males in order to evaluate if PHI-346 has any deleterious effects on the reproductive performance."( A 13-week subchronic intravaginal toxicity study of the novel broad-spectrum anti-HIV and spermicidal agent, N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (PHI-346) in mice.
D'Cruz, OJ; Uckun, FM; Waurzyniak, B,
)
0.33
" The pharmacokinetics of 17 different novel oral formulations of HI-443 were compared in an attempt to identify the most suitable dosage form for clinical use in HIV-infected persons."( In vivo pharmacokinetics and toxicity of a novel hydrophilic oral formulation of the potent non-nucleoside reverse transcriptase inhibitor compound N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (HI-443).
Erbeck, D; Qazi, S; Tibbles, H; Uckun, FM; Venkatachalam, TK, 2007
)
0.53
"To investigate the neuroprotective effects and dose-response relation by combining JAK-STAT signal pathway inhibitor (AG490) with free radical scavenger dimethylthiourea (DMTU) in rats subjected to focal cerebral ischemia/reperfusion (I/R) injury."( [Neuroprotective effects of combined application of JAK-STAT signal pathway inhibitor and free radical scavenger on focal cerebral ischemia/reperfusion injury in rats].
Lei, C; Lu, ZH; Wang, BR; Xiong, LZ; Yang, QZ, 2008
)
0.54
" Results obtained showed that, at appropriate concentrations, H(2)O(2) accelerates MNZ degradation by generating additional HO(); however, when the dosage of H(2)O(2) exceeds the optimal concentration, the efficacy of MNZ degradation is reduced."( Gamma irradiation of pharmaceutical compounds, nitroimidazoles, as a new alternative for water treatment.
Ferro-García, MA; López-Peñalver, J; Prados-Joya, G; Rivera-Utrilla, J; Sánchez-Polo, M, 2009
)
0.35
" The thermal dose-response curve for the fluorescence intensity of gammaH2AX appearance in DNA-PKcs-/- cells during the heating period was similar to that observed in DNA-PKcs+/+ cells."( ATM is the predominant kinase involved in the phosphorylation of histone H2AX after heating.
Chen, DJ; Ejima, Y; Kondo, N; Mori, E; Nakagawa, Y; Noda, T; Ohnishi, K; Ohnishi, T; Okamoto, N; Su, X; Takahashi, A; Toki, A; Uemura, H, 2010
)
0.36
" HI-443 exhibited a favorable toxicity and pharmacokinetics profile following oral, intraperitoneal or intravenous administration in rodents and a favorable safety profile after repeated intravaginal dosing via a gel formulation in rabbits and pigs."( A novel vaginal microbicide containing the rationally designed anti-HIV compound HI-443 (N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea]).
D'Cruz, OJ; Qazi, S; Uckun, FM; Yiv, S, 2012
)
0.58
" Dosage studies revealed that the frequency of primary root curvature was significantly enhanced with increased H(2)O(2) concentrations."( Exogenous hydrogen peroxide reversibly inhibits root gravitropism and induces horizontal curvature of primary root during grass pea germination.
Cheng, W; Jiang, J; Jiao, C; Li, F; Su, M; Sun, Z; Wang, C; Wang, L, 2012
)
0.38
" Among several factors, time (B), Tween 80 (C), ISSD dosage (D) and silver(I) concentration (F) were found to be most significant."( Sunlight mediated diesel degradation under saline conditions using ionic silver coated sand via nanoreduction: use of impregnated form of thiourea modified chitosan membranes for ex situ application.
Das, D; Das, N, 2014
)
0.6
"25mg/L) with a dosage of 10%."( Stabilization/solidification of lead in MSWI fly ash with mercapto functionalized dendrimer Chelator.
Li, F; Tian, Z; Wu, Y; Zhang, B; Zhao, H; Zhou, W, 2016
)
0.43
" The fact that concomitant dosing of sunitinib (VEGFRs/FMS inhibition) with crizotinib (MET inhibition) exerted comparable inhibitory efficacy for bone destruction to TAS-115 also supports this notion."( High Potency VEGFRs/MET/FMS Triple Blockade by TAS-115 Concomitantly Suppresses Tumor Progression and Bone Destruction in Tumor-Induced Bone Disease Model with Lung Carcinoma Cells.
Fujioka, Y; Fujita, H; Gomori, A; Harada, N; Haruma, T; Hashimoto, A; Inada, M; Ito, K; Kataoka, Y; Matsuo, K; Oda, N; Sakuragi, M; Suzuki, T; Tanaka, K; Yamamoto-Yokoi, H; Yonekura, K, 2016
)
0.43
" Fish with a low dosage of exogenous triiodothyronine and those treated with thiourea exhibited retarded development of bony plates compared to both control fish and those treated with higher a triiodothyronine dosage."( Heterochronic development of lateral plates in the three-spined stickleback induced by thyroid hormone level alterations.
Bolotovskiy, AA; DeFaveri, J; Levin, BA; Levina, MA; Merilä, J, 2018
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
chromophoreThe part (atom or group of atoms) of a molecular entity in which the electronic transition responsible for a given spectral band is approximately localized.
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
[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 (3)

ClassDescription
ureas
thioureasCompounds of general formula RR'NC(=S)NR''R'''.
one-carbon compoundAn organic molecular entity containing a single carbon atom (C1).
[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]

Pathways (2)

PathwayProteinsCompounds
protein citrullination57
thyroid hormone biosynthesis524

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency47.44360.003245.467312,589.2998AID2517
GLI family zinc finger 3Homo sapiens (human)Potency60.22430.000714.592883.7951AID1259369; AID1259392
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.39810.001318.074339.8107AID926; AID938
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency44.66846.309627.099079.4328AID602179
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency13.39370.001530.607315,848.9004AID1224841; AID1259401
estrogen nuclear receptor alphaHomo sapiens (human)Potency16.44420.000229.305416,493.5996AID743069; AID743079
aryl hydrocarbon receptorHomo sapiens (human)Potency24.39100.000723.06741,258.9301AID743085; AID743122
serine-protein kinase ATM isoform aHomo sapiens (human)Potency2.23870.707925.111941.2351AID485349
Nuclear receptor ROR-gammaHomo sapiens (human)Potency74.97800.026622.448266.8242AID651802
[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)
Alcohol dehydrogenase E chainEquus caballus (horse)Ki42,000.00000.14122.89278.7000AID33720
Alcohol dehydrogenase S chainEquus caballus (horse)Ki42,000.00000.14122.89278.7000AID33720
UreaseCanavalia ensiformis (jack bean)IC50 (µMol)20.07600.45703.20238.5900AID1055728; AID1071693; AID1168622; AID1238151; AID1238205; AID1250319; AID1254245; AID1312220; AID1368418; AID1453672; AID1673891; AID1799725; AID1799731; AID1801079; AID1801564; AID1801646; AID1802938; AID1802943; AID1802995; AID1803386; AID1882614; AID1882616; AID1882617; AID625341
UreaseCanavalia ensiformis (jack bean)Ki19.87330.40700.40700.4070AID1071692; AID1801532; AID625341
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)21.00000.00040.908610.0000AID1071693
Urease subunit alphaHelicobacter pylori 26695IC50 (µMol)23.00000.29003.87606.7000AID1882622
D(3) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)21.00000.00030.39075.4000AID1071693
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)21.00000.00031.38338.4000AID1071693
Urease subunit betaHelicobacter pylori 26695IC50 (µMol)23.00000.29003.87606.7000AID1882622
Serine-protein kinase ATMHomo sapiens (human)IC50 (µMol)0.20000.00200.29173.4200AID325749
Serine/threonine-protein kinase ATRHomo sapiens (human)IC50 (µMol)0.20000.00301.29487.3000AID325750
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (99)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
regulation of telomerase activitySerine-protein kinase ATMHomo sapiens (human)
DNA damage responseSerine-protein kinase ATMHomo sapiens (human)
peptidyl-serine autophosphorylationSerine-protein kinase ATMHomo sapiens (human)
DNA damage checkpoint signalingSerine-protein kinase ATMHomo sapiens (human)
pexophagySerine-protein kinase ATMHomo sapiens (human)
double-strand break repair via homologous recombinationSerine-protein kinase ATMHomo sapiens (human)
DNA double-strand break processingSerine-protein kinase ATMHomo sapiens (human)
ovarian follicle developmentSerine-protein kinase ATMHomo sapiens (human)
response to hypoxiaSerine-protein kinase ATMHomo sapiens (human)
somitogenesisSerine-protein kinase ATMHomo sapiens (human)
pre-B cell allelic exclusionSerine-protein kinase ATMHomo sapiens (human)
double-strand break repairSerine-protein kinase ATMHomo sapiens (human)
double-strand break repair via nonhomologous end joiningSerine-protein kinase ATMHomo sapiens (human)
chromatin remodelingSerine-protein kinase ATMHomo sapiens (human)
protein phosphorylationSerine-protein kinase ATMHomo sapiens (human)
DNA damage responseSerine-protein kinase ATMHomo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestSerine-protein kinase ATMHomo sapiens (human)
mitotic spindle assembly checkpoint signalingSerine-protein kinase ATMHomo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine-protein kinase ATMHomo sapiens (human)
reciprocal meiotic recombinationSerine-protein kinase ATMHomo sapiens (human)
male meiotic nuclear divisionSerine-protein kinase ATMHomo sapiens (human)
female meiotic nuclear divisionSerine-protein kinase ATMHomo sapiens (human)
signal transductionSerine-protein kinase ATMHomo sapiens (human)
brain developmentSerine-protein kinase ATMHomo sapiens (human)
heart developmentSerine-protein kinase ATMHomo sapiens (human)
determination of adult lifespanSerine-protein kinase ATMHomo sapiens (human)
post-embryonic developmentSerine-protein kinase ATMHomo sapiens (human)
response to ionizing radiationSerine-protein kinase ATMHomo sapiens (human)
regulation of autophagySerine-protein kinase ATMHomo sapiens (human)
positive regulation of gene expressionSerine-protein kinase ATMHomo sapiens (human)
peptidyl-serine phosphorylationSerine-protein kinase ATMHomo sapiens (human)
positive regulation of cell migrationSerine-protein kinase ATMHomo sapiens (human)
negative regulation of B cell proliferationSerine-protein kinase ATMHomo sapiens (human)
regulation of telomere maintenance via telomeraseSerine-protein kinase ATMHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseSerine-protein kinase ATMHomo sapiens (human)
V(D)J recombinationSerine-protein kinase ATMHomo sapiens (human)
cellular response to reactive oxygen speciesSerine-protein kinase ATMHomo sapiens (human)
multicellular organism growthSerine-protein kinase ATMHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processSerine-protein kinase ATMHomo sapiens (human)
lipoprotein catabolic processSerine-protein kinase ATMHomo sapiens (human)
signal transduction in response to DNA damageSerine-protein kinase ATMHomo sapiens (human)
regulation of apoptotic processSerine-protein kinase ATMHomo sapiens (human)
positive regulation of apoptotic processSerine-protein kinase ATMHomo sapiens (human)
positive regulation of DNA damage response, signal transduction by p53 class mediatorSerine-protein kinase ATMHomo sapiens (human)
positive regulation of neuron apoptotic processSerine-protein kinase ATMHomo sapiens (human)
meiotic telomere clusteringSerine-protein kinase ATMHomo sapiens (human)
positive regulation of cell adhesionSerine-protein kinase ATMHomo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine-protein kinase ATMHomo sapiens (human)
protein autophosphorylationSerine-protein kinase ATMHomo sapiens (human)
thymus developmentSerine-protein kinase ATMHomo sapiens (human)
oocyte developmentSerine-protein kinase ATMHomo sapiens (human)
neuron apoptotic processSerine-protein kinase ATMHomo sapiens (human)
regulation of cell cycleSerine-protein kinase ATMHomo sapiens (human)
histone mRNA catabolic processSerine-protein kinase ATMHomo sapiens (human)
cellular response to retinoic acidSerine-protein kinase ATMHomo sapiens (human)
cellular response to gamma radiationSerine-protein kinase ATMHomo sapiens (human)
cellular response to X-raySerine-protein kinase ATMHomo sapiens (human)
cellular response to nitrosative stressSerine-protein kinase ATMHomo sapiens (human)
cellular senescenceSerine-protein kinase ATMHomo sapiens (human)
replicative senescenceSerine-protein kinase ATMHomo sapiens (human)
establishment of RNA localization to telomereSerine-protein kinase ATMHomo sapiens (human)
establishment of protein-containing complex localization to telomereSerine-protein kinase ATMHomo sapiens (human)
regulation of cellular response to heatSerine-protein kinase ATMHomo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine-protein kinase ATMHomo sapiens (human)
positive regulation of DNA catabolic processSerine-protein kinase ATMHomo sapiens (human)
regulation of microglial cell activationSerine-protein kinase ATMHomo sapiens (human)
negative regulation of TORC1 signalingSerine-protein kinase ATMHomo sapiens (human)
negative regulation of telomere cappingSerine-protein kinase ATMHomo sapiens (human)
positive regulation of telomere maintenance via telomere lengtheningSerine-protein kinase ATMHomo sapiens (human)
positive regulation of telomerase catalytic core complex assemblySerine-protein kinase ATMHomo sapiens (human)
regulation of autophagosome assemblySerine-protein kinase ATMHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageSerine-protein kinase ATMHomo sapiens (human)
telomere maintenanceSerine-protein kinase ATMHomo sapiens (human)
nuclear membrane disassemblySerine/threonine-protein kinase ATRHomo sapiens (human)
DNA damage checkpoint signalingSerine/threonine-protein kinase ATRHomo sapiens (human)
nucleobase-containing compound metabolic processSerine/threonine-protein kinase ATRHomo sapiens (human)
DNA replicationSerine/threonine-protein kinase ATRHomo sapiens (human)
double-strand break repairSerine/threonine-protein kinase ATRHomo sapiens (human)
chromatin remodelingSerine/threonine-protein kinase ATRHomo sapiens (human)
DNA damage responseSerine/threonine-protein kinase ATRHomo sapiens (human)
negative regulation of DNA replicationSerine/threonine-protein kinase ATRHomo sapiens (human)
response to xenobiotic stimulusSerine/threonine-protein kinase ATRHomo sapiens (human)
response to mechanical stimulusSerine/threonine-protein kinase ATRHomo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase ATRHomo sapiens (human)
replication fork processingSerine/threonine-protein kinase ATRHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseSerine/threonine-protein kinase ATRHomo sapiens (human)
cellular response to UVSerine/threonine-protein kinase ATRHomo sapiens (human)
interstrand cross-link repairSerine/threonine-protein kinase ATRHomo sapiens (human)
positive regulation of DNA damage response, signal transduction by p53 class mediatorSerine/threonine-protein kinase ATRHomo sapiens (human)
mitotic G2/M transition checkpointSerine/threonine-protein kinase ATRHomo sapiens (human)
response to arsenic-containing substanceSerine/threonine-protein kinase ATRHomo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase ATRHomo sapiens (human)
protein localization to chromosome, telomeric regionSerine/threonine-protein kinase ATRHomo sapiens (human)
cellular response to gamma radiationSerine/threonine-protein kinase ATRHomo sapiens (human)
replicative senescenceSerine/threonine-protein kinase ATRHomo sapiens (human)
establishment of RNA localization to telomereSerine/threonine-protein kinase ATRHomo sapiens (human)
establishment of protein-containing complex localization to telomereSerine/threonine-protein kinase ATRHomo sapiens (human)
regulation of cellular response to heatSerine/threonine-protein kinase ATRHomo sapiens (human)
positive regulation of telomerase catalytic core complex assemblySerine/threonine-protein kinase ATRHomo sapiens (human)
regulation of double-strand break repairSerine/threonine-protein kinase ATRHomo sapiens (human)
DNA repairSerine/threonine-protein kinase ATRHomo sapiens (human)
telomere maintenanceSerine/threonine-protein kinase ATRHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
DNA bindingSerine-protein kinase ATMHomo sapiens (human)
protein serine/threonine kinase activitySerine-protein kinase ATMHomo sapiens (human)
DNA-dependent protein kinase activitySerine-protein kinase ATMHomo sapiens (human)
protein bindingSerine-protein kinase ATMHomo sapiens (human)
ATP bindingSerine-protein kinase ATMHomo sapiens (human)
1-phosphatidylinositol-3-kinase activitySerine-protein kinase ATMHomo sapiens (human)
histone H2AXS139 kinase activitySerine-protein kinase ATMHomo sapiens (human)
identical protein bindingSerine-protein kinase ATMHomo sapiens (human)
protein-containing complex bindingSerine-protein kinase ATMHomo sapiens (human)
protein serine kinase activitySerine-protein kinase ATMHomo sapiens (human)
DNA bindingSerine/threonine-protein kinase ATRHomo sapiens (human)
protein kinase activitySerine/threonine-protein kinase ATRHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase ATRHomo sapiens (human)
protein bindingSerine/threonine-protein kinase ATRHomo sapiens (human)
ATP bindingSerine/threonine-protein kinase ATRHomo sapiens (human)
MutLalpha complex bindingSerine/threonine-protein kinase ATRHomo sapiens (human)
MutSalpha complex bindingSerine/threonine-protein kinase ATRHomo sapiens (human)
histone H2AXS139 kinase activitySerine/threonine-protein kinase ATRHomo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase ATRHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
chromosome, telomeric regionSerine-protein kinase ATMHomo sapiens (human)
peroxisomal matrixSerine-protein kinase ATMHomo sapiens (human)
site of double-strand breakSerine-protein kinase ATMHomo sapiens (human)
nucleusSerine-protein kinase ATMHomo sapiens (human)
nucleoplasmSerine-protein kinase ATMHomo sapiens (human)
nucleolusSerine-protein kinase ATMHomo sapiens (human)
cytoplasmSerine-protein kinase ATMHomo sapiens (human)
peroxisomal matrixSerine-protein kinase ATMHomo sapiens (human)
centrosomeSerine-protein kinase ATMHomo sapiens (human)
spindleSerine-protein kinase ATMHomo sapiens (human)
cytosolSerine-protein kinase ATMHomo sapiens (human)
cytoplasmic vesicleSerine-protein kinase ATMHomo sapiens (human)
intracellular membrane-bounded organelleSerine-protein kinase ATMHomo sapiens (human)
DNA repair complexSerine-protein kinase ATMHomo sapiens (human)
cytoplasmSerine-protein kinase ATMHomo sapiens (human)
nucleusSerine-protein kinase ATMHomo sapiens (human)
chromosome, telomeric regionSerine/threonine-protein kinase ATRHomo sapiens (human)
nuclear envelopeSerine/threonine-protein kinase ATRHomo sapiens (human)
site of DNA damageSerine/threonine-protein kinase ATRHomo sapiens (human)
nucleusSerine/threonine-protein kinase ATRHomo sapiens (human)
nucleoplasmSerine/threonine-protein kinase ATRHomo sapiens (human)
chromosomeSerine/threonine-protein kinase ATRHomo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase ATRHomo sapiens (human)
PML bodySerine/threonine-protein kinase ATRHomo sapiens (human)
ATR-ATRIP complexSerine/threonine-protein kinase ATRHomo sapiens (human)
nucleusSerine/threonine-protein kinase ATRHomo sapiens (human)
chromosomeSerine/threonine-protein kinase ATRHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (80)

Assay IDTitleYearJournalArticle
AID1498567Inhibition of Campylobacter pylori urease preincubated for 5 mins followed by urea addition measured after 10 mins by Berthelot assay2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Synthesis, in vitro and in silico studies of novel potent urease inhibitors: N-[4-({5-[(3-Un/substituted-anilino-3-oxopropyl)sulfanyl]-1,3,4-oxadiazol-2-yl}methyl)-1,3-thiazol-2-yl]benzamides.
AID1312220Inhibition of jack bean urease using urea as substrate assessed as reduction in ammonia production after 30 mins by indophenol method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Solution-phase microwave assisted parallel synthesis, biological evaluation and in silico docking studies of N,N'-disubstituted thioureas derived from 3-chlorobenzoic acid.
AID1250318Inhibition of jack beans urease assessed as hydrolysis of urea into ammonia at 0.5 mM preincubated for 10 mins followed by urea addition measured after 10 mins by Berthelot assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.
AID1250317Inhibition of soybean LOX using linoleic acid as substrate preincubated for 10 mins followed by substrate addition measured after 6 mins by spectrophotometric analysis2015European journal of medicinal chemistry, Sep-18, Volume: 102Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.
AID625341Inhibition of jack bean urease assessed as ammonia production after 30 mins by indophenol method2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors.
AID1055728Inhibition of jack bean urease assessed as ammonia production after 30 mins by indophenol method2013European journal of medicinal chemistry, , Volume: 70Solution-phase microwave assisted parallel synthesis of N,N'-disubstituted thioureas derived from benzoic acid: biological evaluation and molecular docking studies.
AID776454Inhibition of jack bean urease using urea as substrate assessed as ammonia production at 250 ug/ml after 15 mins relative to control2013European journal of medicinal chemistry, Nov, Volume: 69Design, synthesis and biological activities of some 7-aminocephalosporanic acid derivatives.
AID1238205Inhibition of jack bean Urease assessed as ammonia production after 15 mins by indophenol method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design and synthesis of new barbituric- and thiobarbituric acid derivatives as potent urease inhibitors: Structure activity relationship and molecular modeling studies.
AID1135359Ionization constant, pKa of the compound1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID1250319Inhibition of jack beans urease assessed as hydrolysis of urea into ammonia preincubated for 10 mins followed by urea addition measured after 10 mins by Berthelot assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.
AID556560Antimicrobial activity against Escherichia coli K-12 BW25113 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID1368418Inhibition of jack bean urease assessed as reduction in ammonia production using urea as substrate after 15 mins by indophenol method2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Bisindolylmethane thiosemicarbazides as potential inhibitors of urease: Synthesis and molecular modeling studies.
AID71868Antiviral activity was evaluated in vitro against human poliovirus as toxicity zone in agar-diffusion plaque-inhibition test1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Structure-activity relationship of diphenylthiourea antivirals.
AID325749Inhibition of ATM2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
AID556566Antimicrobial activity against ahpC gene-deficient Escherichia coli K-12 3200 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID1673891Inhibition of jack bean urease assessed as reduction in ammonia production using urea as substrate incubated for 15 mins by indophenol method2019Bioorganic & medicinal chemistry, 11-15, Volume: 27, Issue:22
Developing new hybrid scaffold for urease inhibition based on carbazole-chalcone conjugates: Synthesis, assessment of therapeutic potential and computational docking analysis.
AID1168622Inhibition of jack bean urease assessed as reduction in ammonia production incubated at 30 degC for 15 mins by indophenol method2014European journal of medicinal chemistry, Nov-24, Volume: 87Implications of N-capped urea/thiourea and C-capped 3-(1-piperazinyl)-1,2-benzisothiazole with bridging Gly-Val/Phe-Gly-Val-Pro as therapeutic targets.
AID536655Inhibition of jack bean urease assessed as ammonia production after 15 mins by indophenol method2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives.
AID1673890Inhibition of jack bean urease assessed as reduction in ammonia production at 0.5 mM using urea as substrate incubated for 15 mins by indophenol method2019Bioorganic & medicinal chemistry, 11-15, Volume: 27, Issue:22
Developing new hybrid scaffold for urease inhibition based on carbazole-chalcone conjugates: Synthesis, assessment of therapeutic potential and computational docking analysis.
AID776453Inhibition of jack bean urease using urea as substrate assessed as ammonia production after 15 mins2013European journal of medicinal chemistry, Nov, Volume: 69Design, synthesis and biological activities of some 7-aminocephalosporanic acid derivatives.
AID1498919Inhibition of bacterial urease assessed as reduction in ammonia liberation using urea as substrate after 30 mins2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery.
AID1135361Octanol-water partition coefficient, log P of the compound at 37 degC1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine.
AID33720In vitro inhibition against horse liver alcohol dehydrogenase1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
Inhibition by carboxamides and sulfoxides of liver alcohol dehydrogenase and ethanol metabolism.
AID71864Antiviral activity was evaluated in vitro against human poliovirus as antiviral affect in agar-diffusion plaque-inhibition test - => inhibition diameter < = 5 mm1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Structure-activity relationship of diphenylthiourea antivirals.
AID1882622Inhibition of Helicobacter pylori urease2022European journal of medicinal chemistry, Apr-15, Volume: 234An overview on the synthetic urease inhibitors with structure-activity relationship and molecular docking.
AID765551Inhibition of Jack bean urease using urea as substrate assessed as production of ammonia after 15 mins2013European journal of medicinal chemistry, Sep, Volume: 67Microwave assisted synthesis of some hybrid molecules derived from norfloxacin and investigation of their biological activities.
AID1071692Competitive inhibition of jack bean urease using urea as substrate assessed as ammonia production after 15 mins by Lineweaver-Burk/Dixon plot analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas.
AID69276Antiviral activity was evaluated in vitro against human poliovirus as inhibition zone in agar-diffusion plaque-inhibition test1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Structure-activity relationship of diphenylthiourea antivirals.
AID1882614Inhibition of jack bean urease assessed as reduction on ammonia production using urea as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by indophenol method2022European journal of medicinal chemistry, Apr-15, Volume: 234An overview on the synthetic urease inhibitors with structure-activity relationship and molecular docking.
AID556562Antimicrobial activity against sodA gene-deficient Escherichia coli K-12 3144 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID114585Hydroxyl radical scavenging activity by chemiluminescence technique in mouse thymus cells2004Bioorganic & medicinal chemistry letters, Apr-05, Volume: 14, Issue:7
Different hydroxyl radical scavenging activity of water-soluble beta-alanine C60 adducts.
AID1071693Inhibition of jack bean urease using urea as substrate assessed as ammonia production after 15 mins by indophenol method2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas.
AID1498566Inhibition of Campylobacter pylori urease preincubated for 5 mins followed by urea addition measured after 10 mins by Berthelot assay relative to control2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
Synthesis, in vitro and in silico studies of novel potent urease inhibitors: N-[4-({5-[(3-Un/substituted-anilino-3-oxopropyl)sulfanyl]-1,3,4-oxadiazol-2-yl}methyl)-1,3-thiazol-2-yl]benzamides.
AID556565Antimicrobial activity against katG gene-deficient Escherichia coli K-12 3157 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID556568Antimicrobial activity against katE gene-deficient Escherichia coli K-12 3202 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID1403742Inhibition of Bacillus pasteurii urease using urea as substrate measured after 20 mins by phenol reagent based assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Amino acid conjugated antimicrobial drugs: Synthesis, lipophilicity- activity relationship, antibacterial and urease inhibition activity.
AID1250316Inhibition of soybean LOX using linoleic acid as substrate at 0.5 mM preincubated for 10 mins followed by substrate addition measured after 6 mins by spectrophotometric analysis2015European journal of medicinal chemistry, Sep-18, Volume: 102Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.
AID1882616Inhibition of jack bean urease2022European journal of medicinal chemistry, Apr-15, Volume: 234An overview on the synthetic urease inhibitors with structure-activity relationship and molecular docking.
AID23443Partition coefficient (logP)1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
Use of physicochemical parameters in distance geometry and related three-dimensional quantitative structure-activity relationships: a demonstration using Escherichia coli dihydrofolate reductase inhibitors.
AID1181957Inhibition of Bacillus pasteurii urease using urea substrate assessed as reduction in ammonia production after 15 mins by indophenol's method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis and structure-activity relationship of thiobarbituric acid derivatives as potent inhibitors of urease.
AID1453672Inhibition of jack bean urease using urea as substrate pretreated for 15 mins followed by substrate addition by phenol red based spectrophotometric method2017Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13
Synthesis and molecular docking study of some 5,6-dichloro-2-cyclopropyl-1H-benzimidazole derivatives bearing triazole, oxadiazole, and imine functionalities as potent inhibitors of urease.
AID776455Inhibition of jack bean urease using urea as substrate assessed as ammonia production at 100 ug/ml after 15 mins relative to control2013European journal of medicinal chemistry, Nov, Volume: 69Design, synthesis and biological activities of some 7-aminocephalosporanic acid derivatives.
AID1882617Inhibition of jack bean urease assessed as reduction on ammonia production using urea as substrate incubated for 30 mins by indophenol method2022European journal of medicinal chemistry, Apr-15, Volume: 234An overview on the synthetic urease inhibitors with structure-activity relationship and molecular docking.
AID765552Inhibition of Jack bean urease using urea as substrate assessed as production of ammonia at 100 ug/ml after 15 mins2013European journal of medicinal chemistry, Sep, Volume: 67Microwave assisted synthesis of some hybrid molecules derived from norfloxacin and investigation of their biological activities.
AID556564Antimicrobial activity against sodA, sodB gene-deficient Escherichia coli K-12 3156 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID1254245Inhibition of jack bean urease using urea as substrate assessed as ammonia production incubated for 15 mins by indophenol method2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Synthesis of potent urease inhibitors based on disulfide scaffold and their molecular docking studies.
AID1179091Retention time of the compound in 75% MeOH by HPLC analysis2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
Sulfur, selenium and tellurium pseudopeptides: synthesis and biological evaluation.
AID556561Antimicrobial activity against sodB gene-deficient Escherichia coli K-12 DKsodB by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID23734Micelle/water partition coefficient (Pmic) of the compound was determined1996Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13
Thermodynamic aspects of hydrophobicity and the blood-brain barrier permeability studied with a gel filtration chromatography.
AID674462Dissociation constant, pKa of the compound in DMSO at 25 degC2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
RCAI-84, 91, and 105-108, ureido and thioureido analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce Th1-biased cytokines.
AID69151Compound was tested for its ability to inhibit DNA strand scission induced by resveratrol and Cu2+, at concentration 50 mM1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
Resveratrol as a new type of DNA-cleaving agent.
AID556567Antimicrobial activity against katG,katE gene-deficient Escherichia coli K-12 3201 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID556563Antimicrobial activity against sodB gene-deficient Escherichia coli K-12 3145 by broth dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Contribution of oxidative damage to antimicrobial lethality.
AID1238151Inhibition of jack bean urease using urea as substrate assessed as ammonia production after 15 mins by Weatherburn assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis of novel derivatives of oxindole, their urease inhibition and molecular docking studies.
AID325750Inhibition of ATR2007Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1802943Urease Inhibition Assay from Article 10.3109/14756360903389864: \\Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.\\2010Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 25, Issue:4
Design, synthesis, and urease inhibition studies of some 1,3,4-oxadiazoles and 1,2,4-triazoles derived from mandelic acid.
AID1801079In vitro Urease Inhibition Assay from Article 10.1111/cbdd.12379: \\2-(Hetero(aryl)methylene)hydrazine-1-carbothioamides as potent urease inhibitors.\\2015Chemical biology & drug design, Feb, Volume: 85, Issue:2
2-(Hetero(aryl)methylene)hydrazine-1-carbothioamides as potent urease inhibitors.
AID1801646Urease Inhibition Assay from Article 10.1016/j.bioorg.2016.03.010: \\Hybrid benzothiazole analogs as antiurease agent: Synthesis and molecular docking studies.\\2016Bioorganic chemistry, 06, Volume: 66Hybrid benzothiazole analogs as antiurease agent: Synthesis and molecular docking studies.
AID1803386Urease Inhibition Assay from Article 10.3109/14756366.2012.740477: \\Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.\\2013Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 28, Issue:6
Synthesis and biological evaluation of novel series of aminopyrimidine derivatives as urease inhibitors and antimicrobial agents.
AID1801487Urease Inhibition Assay from Article 10.1016/j.bioorg.2015.10.005: \\Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.\\2015Bioorganic chemistry, Dec, Volume: 63Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.
AID1799725Inhibition Assay from Article 10.1080/14756360801945598: \\In silico studies of urease inhibitors to explore ligand-enzyme interactions.\\2009Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 24, Issue:1
In silico studies of urease inhibitors to explore ligand-enzyme interactions.
AID1799731Inhibition Assay from Article 10.1080/14756360802188420: \\Synthesis and biological evaluation of some new N(4)-substituted isatin-3-thiosemicarbazones.\\2009Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 24, Issue:2
Synthesis and biological evaluation of some new N(4)-substituted isatin-3-thiosemicarbazones.
AID1801564Urease Inhibition Assay from Article 10.1111/cbdd.12675: \\Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling.\\2016Chemical biology & drug design, Mar, Volume: 87, Issue:3
Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling.
AID1801532Urease Inhibition Assay from Article 10.1016/j.bioorg.2015.12.007: \\Dihydropyrimidine based hydrazine dihydrochloride derivatives as potent urease inhibitors.\\2016Bioorganic chemistry, Feb, Volume: 64Dihydropyrimidine based hydrazine dihydrochloride derivatives as potent urease inhibitors.
AID1802995Urease Inhibition Assay from Article 10.3109/14756366.2010.528415: \\Urease inhibitors from Indigofera gerardiana Wall.\\2011Journal of enzyme inhibition and medicinal chemistry, Aug, Volume: 26, Issue:4
Urease inhibitors from Indigofera gerardiana Wall.
AID1802938Urease Inhibition Assay from Article 10.3109/14756360903179385: \\Urease inhibitors from Hypericum oblongifolium WALL.\\2010Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 25, Issue:2
Urease inhibitors from Hypericum oblongifolium WALL.
AID1801648Urease Inhibition Assay from Article 10.1016/j.bioorg.2016.04.005: \\Synthesis of 2-acylated and sulfonated 4-hydroxycoumarins: In vitro urease inhibition and molecular docking studies.\\2016Bioorganic chemistry, 06, Volume: 66Synthesis of 2-acylated and sulfonated 4-hydroxycoumarins: In vitro urease inhibition and molecular docking studies.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,629)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902856 (43.08)18.7374
1990's625 (9.43)18.2507
2000's1235 (18.63)29.6817
2010's1563 (23.58)24.3611
2020's350 (5.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.82

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 Index64.82 (24.57)
Research Supply Index8.85 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index118.39 (26.88)
Search Engine Supply Index2.02 (0.95)

This Compound (64.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials46 (0.66%)5.53%
Reviews138 (1.98%)6.00%
Case Studies82 (1.18%)4.05%
Observational1 (0.01%)0.25%
Other6,692 (96.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]