Page last updated: 2024-12-09

propylthiouracil

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Description

Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. [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 CID657298
CHEMBL ID1518
CHEBI ID8502
SCHEMBL ID41239
SCHEMBL ID17375339
MeSH IDM0017784

Synonyms (244)

Synonym
HMS1766D22
MLS002303010
BB 0242498
6-propyl-2-thioxo-2,3-dihydro-1h-pyrimidin-4 -one
BRD-K48168960-001-04-4
BRD-K48168960-001-05-1
nsc-6498
6-n-propylthiouracil
thiuragyl
propyl-thiorist
prothiurone
ptu (thyreostatic)
2-mercapto-6-propylpyrimid-4-one
prothyran
propylthiorit
2-thio-4-oxo-6-propyl-1,3-pyrimidine
6-propylthiouracil
protiural
propacil
2,3-dihydro-6-propyl-2-thioxo-4(1h)-pyrimidinone
6-thio-4-propyluracil
propycil
4-propyl-2-thiouracil
procasil
thyreostat ii
2-mercapto-4-hydroxy-6-n-propylpyrimidine
uracil, 6-propyl-2-thio-
6-n-propyl-2-thiouracil
2-thio-6-propyl-1,3-pyrimidin-4-one
2-mercapto-6-propyl-4-pyrimidone
propyl-thiorit
prothycil
6-propyl-2-thio-2,3h)-pyrimidinedione
prothiucil
wln: t6mymvj bus f3
6-propyl-2-thiouracil
nsc6498
propyl-thyracil
4(1h)-pyrimidinone,3-dihydro-6-propyl-2-thioxo-
4(1h)-pyrimidinone, 2,3-dihydro-6-propyl-2-thioxo-
6-(n-propyl)-2-thiouracil
6-propyl-2-thioxo-1h-pyrimidin-4-one
smr000058275
MLS000028494 ,
KBIO1_000268
DIVK1C_000268
inchi=1/c7h10n2os/c1-2-3-5-4-6(10)9-7(11)8-5/h4h,2-3h2,1h3,(h2,8,9,10,11
nsc70461
nsc-70461
SPECTRUM_000876
6-propyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1h)-one
PRESTWICK_810
propylthiouracile
propylthiouracilum
propiltiouracilo
6-propyl-2-thio-2,4(1h,3h)pyrimidinedione
6-propyl-2-thioxo-2,3-dihydropyrimidin-4(1h)-one
CHEBI:8502 ,
NCGC00016229-01
cas-51-52-5
IDI1_000268
SPECTRUM5_001815
BPBIO1_000427
PRESTWICK3_000494
PRESTWICK2_000494
NCGC00090881-01
propiltiouracilo [inn-spanish]
hsdb 3390
propilthiouracil
nsc 6498
ccris 544
einecs 200-103-2
propiltiouracile [dcit]
propyl thiouracil
propythiouracil
ai3-25477
4-hydroxy-2-mercapto-6-propylpyrimidine
6-propil-tiouracile [italian]
propylthiouracilum [inn-latin]
propylthiouracile [inn-french]
propylthiouracil
51-52-5
C07569
6-propyl-2-thiouracil, enzyme inhibitor
DB00550
propylthiouracil (tn)
D00562
propylthiouracil (jp17/usp/inn)
BSPBIO_000387
BSPBIO_003402
NCGC00090881-02
NCGC00090881-03
NCGC00022715-03
KBIOGR_001003
KBIO3_002622
KBIO2_006492
KBIO2_003924
KBIOSS_001356
KBIO2_001356
SPBIO_002308
SPECTRUM2_001302
NINDS_000268
PRESTWICK1_000494
SPECTRUM4_000492
PRESTWICK0_000494
SPECTRUM3_001731
SPBIO_001363
SPECTRUM1500515
NCGC00016229-02
NCGC00178089-01
NCGC00178089-02
6 propyl 2 thiouracil
6-propyl-2 thiouracil
NCGC00183321-01
AC-10795
HMS2092E03
CHEMBL1518
bdbm50133597
HMS500N10
2-mercapto-6-propylpyrimidin-4(3h)-one
FT-0695546
F2199-0035
2-mercapto-6-propylpyrimidin-4-ol
P0533
HMS1920L22
HMS1569D09
AKOS001053246
6-propyl-2-sulfanylidene-1h-pyrimidin-4-one
AKOS000120319
HMS2096D09
HMS3259M04
STL102645
propylthiouracil [usp:inn:ban:jan]
unii-721m9407iy
721m9407iy ,
propiltiouracile
6-propil-tiouracile
NCGC00259290-01
NCGC00254180-01
tox21_201741
tox21_300280
nsc-757302
nsc757302
pharmakon1600-01500515
tox21_110882
dtxsid5021209 ,
dtxcid101209
F1967-1318
HMS2230B22
CCG-39240
NCGC00016229-08
NCGC00016229-05
NCGC00016229-04
NCGC00016229-07
NCGC00016229-11
NCGC00016229-09
NCGC00016229-03
NCGC00016229-06
NCGC00016229-10
6-propyl-2-sulfanylpyrimidin-4-ol
500-50-5
6-propyl-2-thioxo-2, 3-dihydropyrimidin-4(1h)-one
FT-0621285
NCGC00016229-13
PS-3436
propylthiouracil [iarc]
propylthiouracil [mi]
propylthiouracil [who-dd]
propylthiouracil [inn]
propylthiouracil [mart.]
propylthiouracil [usp-rs]
propylthiouracil [ep impurity]
propylthiouracil [hsdb]
propylthiouracil [who-ip]
propylthiouracil [jan]
propylthiouracil [ep monograph]
propylthiouracil [vandf]
propylthiouracil [orange book]
propylthiouracil [usp monograph]
S1988
AKOS015892537
F3097-4245
HMS3371D17
gtpl6650
4-hydroxy-6-n-propylpyrimidine-2-thiol
2-mercapto-6-propyl-pyrimidin-4-ol
2-mercapto-4-hydroxy-6-propyl pyrimidine
HY-B0346
NC00533
SCHEMBL41239
tox21_110882_1
NCGC00016229-14
6-propyl-2-thio-2,4(1h,3h)-pyrimidinedione
6-propyl-2-sulfanyl-4-pyrimidinol #
MLS006011901
propylthiouracil / 6-propyl-2-thiouracil
smr003317355
W-105881
BS-3928
2-thio-4-hydroxy-6-n-propyl-pyrimidine
OPERA_ID_530
AB00052082_05
AB00052082_06
4(1h)-pyrimidinone,6-butyl-2,3-dihydro-2-thioxo-
mfcd00006041
SCHEMBL17375339
6-propyl-2-sulfanylidene-1,2,3,4-tetrahydropyrimidin-4-one
6-propyl-2-thiouracil, purum, >=98.0% (t)
nsc 70461
SR-05000001706-3
sr-05000001706
propylthiouracil, united states pharmacopeia (usp) reference standard
6-propyl-2-thiouracil, vetranal(tm), analytical standard
HMS3655J07
SR-05000001706-2
SR-05000001706-1
6-propyl-2-sulfanyl-3,4-dihydropyrimidin-4-one
EN300-35033
propylthiouracil, european pharmacopoeia (ep) reference standard
propylthiouracil; 2,3-dihydro-6-propyl-2-thioxopyrimidin-4(1h)-one
2,3-dihydro-6-propyl-2-thioxo-4(1h)pyrimidinone
SBI-0051497.P003
2-thio-4-hydroxy-6-n-propylpyrimidine
HMS3713D09
Z56922173
SW196944-3
3CJ ,
BCP22165
Q377342
SY038617
BRD-K48168960-001-08-5
6-n-propylthiouracil;6-propyl-2-thiouracil;ptu
AC8761
propylthiouracil (usp-rs)
propylthiouracil (ep monograph)
h03ba02
propylthiouracil (usp monograph)
propylthiouracil (iarc)
propylthiouracil (ep impurity)
propylthiouracile (inn-french)
propylthiouracil (usp:inn:ban:jan)
propiltiouracilo (inn-spanish)
propylthiouracil (mart.)
propylthiouracilum (inn-latin)

Research Excerpts

Overview

Propylthiouracil (PTU) is a common drug that is used in medicine for treating hyperthyroidism. It is a rare cause of the DRESS/DiHS syndrome, which typically consists of severe dermatitis.

ExcerptReferenceRelevance
"Propylthiouracil (PTU) is a common drug that is used in medicine for treating hyperthyroidism. "( Thymoquinone improved redox homeostasis in the heart and aorta of hypothyroid rats.
Baghcheghi, Y; Beheshti, F; Hedayati-Moghadam, M; Hosseini, M; Seyedi, F, 2022
)
2.16
"Propylthiouracil is a rare cause of the DRESS/DiHS syndrome, which typically consists of severe dermatitis and various degrees of internal organ involvement. "( DRESS/DiHS syndrome induced by Propylthiouracil: a case report.
Chen, L; Chen, X; Cong, X; Shen, Q; Wang, Q; Yu, L; Zang, H, 2023
)
2.64
"Propylthiouracil (PTU) is a synthetic antithyroid drug that can induce ANCA-associated vasculitis."( [Purpura in a young woman with hyperthyroidism].
Bernigaud, C; Charpentier, C; Droumaguet, C; Fardet, L; Giraud-Kerleroux, L; Helbert-Davidson, S; Hüe, S; Ingen-Housz-Oro, S; Marciano-Fellous, L; Thai, LH; Thomas, L, 2021
)
2.06
"6-Propylthiouracil, PTU, is a well-known antithyroid drug that has been the mainstay of treatment of Graves' disease. "( Electrochemical versus Enzymatic in Vitro Oxidations of 6-propyl-2-thiouracil: Identification, Detection, and Characterization of Metabolites.
Chipiso, K; Simoyi, RH, 2017
)
1.18
"Propylthiouracil (PTU) is a common antithyroid drug which can treat hyperthyroidism effectively. "( Propylthiouracil-induced organizing pneumonia: A case report.
An, J; Hu, CP; Luo, BL; Xiao, XW, 2019
)
3.4
"Propylthiouracil is a drug used to treat hyperthyroidism. "( Diffuse alveolar haemorrhage secondary to propylthiouracil-induced vasculitis.
Costa, T; Ferreira, C; Marques, AV, 2015
)
2.12
"Propylthiouracil (PTU) is a potent antithyroid drug that acts by inhibiting the function of TPO."( Mode of binding of the antithyroid drug propylthiouracil to mammalian haem peroxidases.
Kaur, P; Kushwaha, GS; Sharma, S; Singh, A; Singh, AK; Singh, RP; Singh, TP, 2015
)
1.41
"Propylthiouracil (PTU) is a medication commonly used to treat hyperthyroidism, but it is associated with various rare side effects, such as antineutrophil cytoplasm antibody-positive vasculitis."( Necrotizing vasculitis in a patient affected by autoimmune hyperthyroidism treated with propylthiouracil.
Antonucci, A; Bardazzi, F; Iozzo, I; Patrizi, A,
)
1.07
"Propylthiouracil (PTU) is a common and effective clinical medicine for the treatment of hyperthyroidism. "( Stimulatory effects of propylthiouracil on pregnenolone production through upregulation of steroidogenic acute regulatory protein expression in rat granulosa cells.
Chen, MC; Kan, SF; Tsai, SC; Wang, PS; Wang, SW; Wu, YC, 2010
)
2.11
"Propylthiouracil (PTU) is a drug used to treat hyperthyroidism. "( Propylthiouracil-induced nonspecific interstitial pneumonia.
Chung, JH; Kim, SY; Koo, HK; Lee, CT; Lee, JH; Lee, JY; Lee, YJ; Park, SS; Yoon, HI, 2011
)
3.25
"Propylthiouracil (PTU) is an effective drug for psoriasis treatment. "( Clinical efficacy of propylthiouracil and its influence on prolactin in psoriatic patients.
Dayalan, H; Elango, T; Gnanaraj, P; Malligarjunan, H; Subramanian, S, 2011
)
2.13
"Propylthiouracil (PTU) is an antithyroid drug which is known to cause drug-induced vasculitis. "( Propylthiouracil-induced anti-neutrophil cytoplasmic antibodies and agranulocytosis together with granulocyte colony-stimulating factor induced Sweet's syndrome in a patient with Graves' disease.
Cuyan, D; Deram, B; Ertugrul, T; Koray, T; Mustafa, S; Ozlem, C, 2011
)
3.25
"Propylthiouracil (PTU) is a thioamide drug used clinically to inhibit thyroid hormone production. "( Inhibition of testosterone production by propylthiouracil in rat Leydig cells.
Chiao, YC; Cho, WL; Wang, PS, 2002
)
2.02
"Propylthiouracil (PTU) is an anti-thyroid drug that reportedly can impair olfactory function in humans and mice. "( Propylthiouracil alters the expression and activity of glutathione-dependent enzymes in the mouse olfactory mucosa.
Etienne, LA; Maruniak, JA; Walters, E, 2003
)
3.2
"Propylthiouracil is a commonly used agent in the treatment of patients with Graves' hyperthyroidism, a condition associated with elevated levels of interleukin-12 (IL-12), which fall significantly after propylthiouracil treatment."( Effect of PTU on IL-12 and IL-10 in psoriasis.
Barr, RJ; Elias, AN; Nanda, VS, 2003
)
1.04
"Propylthiouracil is a commonly used medication for hyperthyroidism. "( Fulminant hepatic failure associated with propylthiouracil: a case report with treatment emphasis on the use of plasmapheresis.
Aydemir, S; Bayraktaroglu, T; Peksoy, I; Tekin, IO; Unal, AU; Ustundag, Y, 2005
)
2.04
"Propylthiouracil is a drug used in the treatment of hyperthyroidism for more than 60 years. "( Propylthiouracil-induced vasculitis associated with ANCA: a case report.
Atilgan, KG; Ayli, MD; Dede, F; Duranay, M; Guler, S; Memis, L; Yuksel, A; Yuksel, C, 2007
)
3.23
"Propylthiouracil (PTU) is a well known inhibitor of thyroxine (T(4)) to triiodothyronine (T(3)) conversion as evidenced by its effect in several in vitro systems and by the decrease in serum T(3) caused by this drug in either rats or man receiving T(4) replacement. "( Evidence for two tissue-specific pathways for in vivo thyroxine 5'-deiodination in the rat.
Crantz, FR; Larsen, PR; Leonard, JL; Silva, JE, 1982
)
1.71
"Propylthiouracil is a drug used commonly to treat hyperthyroidism. "( Hepatotoxicity from propylthiouracil.
Westphal, SA, 1994
)
2.05
"Propylthiouracil is an antithyroid drug which is carried by the blood, thanks to its binding with human seroalbumin (HSA), and induces a structural alteration in HSA that changes the binding capability of other ligands. "( Usefulness of difference spectroscopy in the study of the binding of uracil derivatives to human serum albumin.
Ochoa De Aspuru, E; Zatón, AM, 1993
)
1.73
"Propylthiouracil (PTU) is an antithyroid thioureylene that has immune modulatory and free radical scavenging abilities. "( Propylthiouracil in psoriasis: results of an open trial.
Barr, RJ; Elias, AN; Goodman, MM; Liem, WH, 1993
)
3.17
"Propylthiouracil (PTU) is an anti-thyroid drug. "( Direct effects of propylthiouracil on testosterone production in monkeys.
Chao, HL; Chiao, YC; Huang, SW; Wang, PS, 2000
)
2.08

Effects

Propylthiouracil (PROP) has been used to determine the genetic sensitivity to bitter taste in early childhood caries. It has been associated with drug-induced ANCA-associated vasculitis (AAV) It inhibits the enzyme 5'-deiodinase, which converts thyroxine to triiodothyronine.

ExcerptReferenceRelevance
"Propylthiouracil (PROP) has been used to determine the genetic sensitivity to bitter taste in early childhood caries."( Bitter Taste Perception and Dental Biofilm Cariogenicity in Orthodontics.
Koontongkaew, S; Luengthamchat, N; Utispan, K, 2022
)
1.44
"Propylthiouracil (PTU) has been associated with drug-induced ANCA-associated vasculitis (AAV), with antibodies against myeloperoxidase (MPO) and proteinase 3 (PR3) present individually and together having been recognised."( An unusual presentation of propylthiouracil-induced anti-MPO and PR3 positive ANCA vasculitis with associated anti-GBM antibodies, IgA nephropathy and an IgG4 interstitial infiltrate: a case report.
Bottomley, MJ; Daruwalla, CP; Galante, JR; Haynes, R; Roberts, ISD; Storey, BC, 2020
)
1.58
"Propylthiouracil has been in use for more than half a century for the treatment of hyperthyroidism. "( Aplastic anemia secondary to propylthiouracil: A rare and life-threatening adverse effect.
Kamran, A; Mewawalla, P; Shaikh, H; Shaikh, S, 2019
)
2.25
"Propylthiouracil (PTU) has been used for the treatment of hyperthyroidism since the 1940s, but over the years reports of significant hepatotoxicity have come forth, particularly in children. "( Propylthiouracil, and methimazole, and carbimazole-related hepatotoxicity.
Akmal, A; Kung, J, 2014
)
3.29
"Propylthiouracil exposure has not been associated with an increased risk of congenital malformations and is the recommended drug during the first trimester of pregnancy."( Pharmacologic treatment of hyperthyroidism during pregnancy.
Cassina, M; Clementi, M; Di Gianantonio, E; Donà, M, 2012
)
1.1
"Propylthiouracil (PTU) has been used in the treatment of hyperthyroidism for many years and inhibits the enzyme 5'-deiodinase, which converts thyroxine to triiodothyronine. "( Oral propylthiouracil for the treatment of resistant plaque psoriasis.
Chowdhury, MM; Marks, R, 2001
)
2.27
"Propylthiouracil has been shown to bind to the hepatic T 3 receptor and it is possible that propylthiouracil (6-n-propyl-2-thiouracil) binding to the ligand-binding site normally occupied by T 3 impairs transcription by inactivating the effect of T 3 as well as by squelching retinoic X receptor heterodimer formation with other receptors of the steroid receptor superfamily such as the peroxisome proliferator-activated receptor, retinoic acid receptor and vitamin D receptors."( Anti-thyroid thioureylenes in the treatment of psoriasis.
Elias, AN, 2004
)
1.04
"Propylthiouracil (PTU) has been shown to be protective against acetaminophen (APAP)-induced liver damage in rats; however, the nephroprotective effect of propylthiouracil has not been studied yet."( Propylthiouracil attenuates acetaminophen-induced renal damage in the rat.
Abraham, P; Dian, BJ; Kanakasabapathy, I, 2005
)
2.49
"Propylthiouracil (PTU) has been held responsible for diffuse alveolar hemorrhage (DAH) with positive antineutrophil cytoplasmic antibody (ANCA) and capillaritis. "( Propylthiouracil-related diffuse alveolar hemorrhage with negative serologies and without capillaritis.
Hadjiangelis, NP; Harkin, TJ, 2007
)
3.23
"Propylthiouracil (PTU) has been known to induce myeloperoxidase-antineutrophil cytoplasmic antibody (MPO-ANCA) positive vasculitis. "( Follow-up of avidity and titre of anti-myeloperoxidase antibodies in sera from patients with propylthiouracil-induced vasculitis.
Chen, M; Gao, Y; Guo, XH; Wang, HY; Ye, H; Zhao, MH, 2007
)
2
"2-Propylthiouracil has been reported as replacing glutathione as a substrate for the glutathione transferases of rat liver. "( 2-Propylthiouracil does not replace glutathione for the glutathione transferases.
Guthenberg, C; Habig, WH; Jakoby, WB; Mannervik, B; Vander Jagt, DL, 1984
)
1.71
"Propylthiouracil has been shown to have a protective effect against hypoxic necrosis in alcohol-fed animals and has been found to be most effective in accelerating the rate of recovery of alcoholics with active liver disease."( Hepatocyte demand and substrate supply as factors in the susceptibility to alcoholic liver injury: pathogenesis and prevention.
Israel, Y; Orrego, H, 1981
)
0.98
"Propylthiouracil (PTU) has recently been observed to be associated with antineutrophil cytoplasmic antibody (ANCA)-positive small vessel vasculitis, resulting in crescentic glomerulonephritis and, infrequently, diffuse alveolar hemorrhage (DAH). "( Diffuse alveolar hemorrhage and pulmonary capillaritis due to propylthiouracil.
Dhillon, SS; Doe, N; Qadri, AM; Ricciardi, S; Schwarz, MI; Singh, D, 1999
)
1.99
"Propylthiouracil use has been associated with ANCA positive pauci-immune glomerulonephritis, but not with IgA nephropathy."( ANCA-positive glomerulonephritis and IgA nephropathy in a patient on propylthiouracil.
Hurley, RM; Lirenman, DS; Winters, MJ, 2002
)
1.27
"Propylthiouracil (PTU) has been demonstrated to reduce alcohol-induced hepatocyte damage and severe alcoholic liver disease. "( Antioxidant activity of propylthiouracil.
Day, RO; Hicks, M; Wong, LS, 1992
)
2.03
"Propylthiouracil has been shown experimentally to protect against alcohol-induced hepatocellular necrosis in hypoxic conditions. "( Long-term treatment of alcoholic liver disease with propylthiouracil.
Blake, JE; Blendis, LM; Compton, KV; Israel, Y; Orrego, H, 1987
)
1.97

Actions

Propylthiouracil is a rare cause of the DRESS/DiHS syndrome. The syndrome typically consists of severe dermatitis and various degrees of internal organ involvement. It can cause severe liver failure, leading to liver transplantation or death.

ExcerptReferenceRelevance
"Propylthiouracil is a rare cause of the DRESS/DiHS syndrome, which typically consists of severe dermatitis and various degrees of internal organ involvement. "( DRESS/DiHS syndrome induced by Propylthiouracil: a case report.
Chen, L; Chen, X; Cong, X; Shen, Q; Wang, Q; Yu, L; Zang, H, 2023
)
2.64
"Propylthiouracil promotes VSMC differentiation, at lest in part, via induction of the PTEN-mediated pathway."( Propylthiouracil, independent of its antithyroid effect, promotes vascular smooth muscle cells differentiation via PTEN induction.
Chen, WJ; Hsu, LA; Kuo, CT; Lee, DY; Lin, KH; Pang, JH, 2010
)
2.52
"Propylthiouracil can cause severe liver failure, leading to liver transplantation or death."( [Update hyperthyreoidism].
Mann, K; Möller, L, 2010
)
1.08
"Propylthiouracil did not inhibit PT4ase at 10 mM DTT, but when the DTT concentration was lowered to 0.25 mM, up to 71% inhibition was noted."( The effects of propylthiouracil, iodothyronines, and other agents on thyroid hormone metabolism in human placenta.
Braverman, LE; Emerson, CH; Fang, SL; Fay, M; Roti, E; Wright, G, 1984
)
1.34
"Propylthiouracil may cause lethal hepatic damage."( Propylthiouracil hepatotoxicity: two pediatric cases and review of the literature.
Eidson, MS; Jonas, MM,
)
2.3

Treatment

Propylthiouracil-treated animals showed decreased cellular and nuclear areas when compared with the control animals, except for the 180-day-old animals, whose pericentral cells and nuclei were greater than those of the controls.

ExcerptReferenceRelevance
"Propylthiouracil treatment of Graves' disease has been postulated to provoke antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis. "( Propylthiouracil and carbimazole associated-antineutrophil cytoplasmic antibodies (ANCA) in patients with Graves' disease.
Allahabadia, A; Chin, L; Daykin, J; Franklyn, JA; Gough, SC; Harper, L; Heward, J; Savage, CO, 2004
)
3.21
"Propylthiouracil treatment was followed by a statistically significant decrease in thyroid gland volume and circumference of neck (p< 0.001 and p< 0.001, respectively)."( Effects of antithyroid medication on the flow-volume loop in patients with hyperthyroidism.
Arbak, P; Bicik, Z; Cinar, Y; Safak, A; Ulger, F, 2004
)
1.04
"Propylthiouracil-treated portal hypertensive rats had a lower portal pressure (12.4 +/- 1.9 versus 16.3 +/- 0.7 mmHg; p < 0.05) and portal blood flow (11.6 +/- 0.7 versus 13.2 +/- 1.3 ml/min/100 g; p < 0.05) than non-treated animals. "( Chronic administration of propylthiouracil ameliorates hyperdynamic circulation in portal hypertensive rats.
Albornoz, L; Bandi, JC; Bildózola, M; de las Heras, M; Mastai, RC, 2005
)
2.07
"Propylthiouracil pretreatment significantly reduced APAP-induced nephrotoxicity in a dose-dependant manner, as evidenced by reduction in plasma creatinine and by amelioration of renal pathology (interstitial congestion, tubular cell degeneration and necrosis)."( Propylthiouracil attenuates acetaminophen-induced renal damage in the rat.
Abraham, P; Dian, BJ; Kanakasabapathy, I, 2005
)
3.21
"Propylthiouracil treatment (PTU) of rats led to thyroid hypertrophy and hyperplasia by TSH-induced activation of the mitogen-activated protein kinase (MAPK) pathway."( HMG-CoA reductase inhibitors inhibit rat propylthiouracil-induced goiter by modulating the ras-MAPK pathway.
Bifulco, M; Carella, C; Fiorentino, L; Gazzerro, P; Gerbasio, D; Laezza, C; Matarese, G; Mazziotti, G; Portella, G, 2006
)
1.32
"Propylthiouracil treatment of rats is associated with a decrease in anterior pituitary neurotensin content, an increase in hypothalamic content and an impaired release of peptide from hypothalami in vitro."( Neurotensin regulation of TSH secretion in the rat.
Askew, RD; Franks, S; Ramsden, DB; Shennan, KI; Sheppard, MC, 1983
)
0.99
"Propylthiouracil treatment had no beneficial or protective effect in alcohol-fed rats in this animal model of hepatitis."( Potentiation of hepatotoxicity by ethanol in galactosamine-induced hepatitis in rats: role of propylthiouracil protection.
Ganatra, RD; Nadkarni, GD; Naik, SB; Soman, CS; Talavdekar, RV; Talwalkar, GV, 1983
)
1.21
"Propylthiouracil treatment did not reduce the frequency and incidence of complications in alcoholic hepatitis, but induced hypothyroidism in 4 patients."( Double-blind, controlled trial of propylthiouracil in patients with severe acute alcoholic hepatitis.
Hallé, P; Kanel, G; Kaptein, E; Paré, P; Redeker, AG; Reynolds, TB, 1982
)
1.26
"Propylthiouracil treatment reduced the mean plasma T4 concentration to 9 ng/ml and the mean plasma CBA to 39% of normal, while following recovery from PTU, the mean values for plasma T4 and CBA were 56 ng/ml and 108%, respectively."( Correlation between plasma thyroxine levels and corticosterone-binding activity in intact, ovariectomized, and ovariectomized estrogen-treated rats.
Calvano, SE; Carlisle, HJ; Ladenslager, ML; Reynolds, RW, 1981
)
0.98
"The propylthiouracil treatment caused a marked increase in the number of round, peroxidase-positive vesicles in the apical and middle regions of cytoplasm, and brought about a formation of granular reaction products in the colloid lumen adjacent to the elongated microvilli."( Thyrotropin-dependence of the distribution of peroxidase in rat thyroid gland.
Hosoya, T; Matsukawa, S; Mihara, S, 1981
)
0.74
"Propylthiouracil treatment (0.05% PTU in the drinking water for 21 days) led to a marked increase in thyroid gland weight (550% of control) but had no significant effect on NGF concentration in any of the organs studied with the exception of kidney where a 75% reduction in NGF concentration was observed."( Radioimmunoassay for mouse nerve growth factor (NGF). Effects of thyroxine administration on tissue NGF levels.
Fisher, DA; Guo, SM; Walker, P; Weichsel, ME, 1980
)
0.98
"In propylthiouracil-treated rats, the complete endocytic removal of the luminal content coincided with the pronounced visualization of APP/APLP in the extrafollicular space, where it was associated with proliferating endothelial cells and fibroblasts."( Localization and regulated release of Alzheimer amyloid precursor-like protein in thyrocytes.
Graebert, KS; Herzog, V; Kehle, T; Lemansky, P, 1995
)
0.81
"Propylthiouracil treatment also attenuated the increase in portal tributary blood flow after the administration of a single dose of ethanol."( Effect of propylthiouracil on the ethanol-induced increase in liver oxygen consumption in awake rats.
Carmichael, FJ; Israel, Y; Orrego, H; Saldivia, V, 1993
)
1.41
"Propylthiouracil (PTU) treatment caused stimulation of the synaptosomal Na(+)-K(+)-ATPase activity in comparison to the untreated control animals."( Synaptosomal action of thyroid hormone: changes in Na(+)-K(+)-ATPase activity in adult rat cerebral cortex.
Ray, AK; Sarkar, PK, 1993
)
1.01
"Propylthiouracil pretreatment for 12 days enhanced the concentration of the following metabolites in the liver: ATP (1.5 fold), ATPase inhibitor protein (IF1) (4.5 fold), and reduced glutathione (1.3 fold), while the activity of the inhibitor protein increased 2 fold."( Induction of an ATPase inhibitor protein by propylthiouracil and protection against paracetamol (acetaminophen) hepatotoxicity in the rat.
Banerjee, A; Chan, SH; Chiji, H; Cho, C; Linscheer, WG; Murthy, UK; Nandi, J, 1998
)
1.28
"Propylthiouracil treatment lowered the level of alpha receptors in heart by 30% as measured by [3H]dihydroergocryptine binding, but increased the affinity about 2.5-fold."( Hormone action at the membrane level. VIII. Adrenergic receptors in rat heart and adipocytes and their modulation by thyroxine.
Ciaraldi, TP; Marinetti, GV, 1978
)
0.98
"Propylthiouracil (PTU) treatment of thyroidectomized rats maintained on T4, 2 mug/100 g BW per day resulted in increased NE125I from [125E]T3 in plasma, kidney, and liver."( Thyroid hormone regulation of extrathyroidal iodoproteins.
Balsam, A; Sexton, FC, 1976
)
0.98
"Propylthiouracil treatment produced an increase in hexokinase activity in the hypothalamus and septum, and a decrease in the anterior cortex, while phosphofructokinase decreased significantly in the hippocampus."( Effect of low-iodine diet and propylthiouracil on glycolytic enzymes in brain areas of adult rats.
Alonso, A; Morata, P; Morell, M; Quesada, J; Sabell, I, 1989
)
1.29
"Propylthiouracil treatment produced a reduction (P less than .01) in body weight and an increase (P less than .01) in thyroid weight."( Effects of antithyroid drug on the rectal temperature and metabolic parameters of ducks (Cairina moschata).
Artoni, SM; Macari, M; Zuim, SM, 1989
)
1
"Propylthiouracil (PTU) treatment raised LSH levels but 131I treatment produced no significant change."( Free radicals and Graves' disease: the effects of therapy.
Bradley, H; Chopra, M; McKillop, JH; Smith, WE; Thomson, JA; Wilson, R, 1989
)
1
"Propylthiouracil-treated rats also had increased phosphoprotein phosphatase activities towards phosphorylase and glycogen synthase and decreased activity of phosphatase inhibitor 1."( Effects of altered thyroid status on beta-adrenergic actions on skeletal muscle glycogen metabolism.
Chu, DT; Exton, JH; Khatra, BS; Shikama, H, 1985
)
0.99
"Propylthiouracil-treated animals showed decreased cellular and nuclear areas when compared with the control animals, except for the 180-day-old animals, whose pericentral cells and nuclei were greater than those of the controls and exhibited fatty infiltration."( Effect of propylthiouracil on liver cell development in the male albino mouse: protective effect against ethanol-induced alterations.
Batista-López, N; Ferres-Torres, R; Gómez-Sirvent, JL; González-Hernández, T; González-Reimers, CE; Pérez-Delgado, MM; Santolaria-Fernández, FJ, 1988
)
1.4
"Treatment with propylthiouracil, iodide potassium (KI), and prednisolone (PSL) was started, which resulted in improvement of the general condition."( Glucose variability before and after treatment of a patient with Graves' disease complicated by diabetes mellitus: assessment by continuous glucose monitoring.
Arao, T; Kurozumi, A; Mori, H; Narisawa, M; Okada, Y; Tanaka, Y; Torimoto, K; Yamamoto, S, 2014
)
0.74
"Treatment with propylthiouracil attenuated these increments after 1 month."( The effect of hypothyroidism, hyperthyroidism, and their treatment on parameters of oxidative stress and antioxidant status.
Biberoğlu, G; Demirci, H; Elbeg, S; Erbil, MK; Erdamar, H; Sancak, B; Yakar, T; Yaman, H; Yetkin, I, 2008
)
0.69
"On treatment with propylthiouracil and a beta-blocking agent, her symptoms resolved within one day, even though her free thyroxine level was still high."( Hyperthyroidism as a cause of persistent vomiting.
Cools, BM; Hoogendoorn, EH, 2004
)
0.65
"Treatment with propylthiouracil for 5 days resulted in complete suppression of the increase in liver oxygen consumption induced by long-term ethanol administration."( Effect of propylthiouracil on the ethanol-induced increase in liver oxygen consumption in awake rats.
Carmichael, FJ; Israel, Y; Orrego, H; Saldivia, V, 1993
)
1.03
"Treatment with propylthiouracil, 300 mg/d for 2 months followed by 100 to 150 mg/d for 3 months and a subsequent maintenance dose of 100 mg/d."( Hepatic injury during propylthiouracil therapy in patients with hyperthyroidism. A cohort study.
Chen, TJ; Fan, KD; Huang, MJ; Li, KL; Liaw, YF; Wu, SS, 1993
)
0.95
"Treatment with propylthiouracil produced a decline in serum T3 plasma appearance rate T3 PAR (-55%; P < 0.02) in the T4-replaced lean rat but no alteration in T3 metabolism in the fatty Zucker rat."( Impaired peripheral thyroid hormone metabolism in genetic obesity.
Katzeff, HL; Selgrad, C, 1993
)
0.63
"The treatment with propylthiouracil induces the normalization of thyroid hormone status and consequently of OCTT with the disappearance of gastrointestinal symptoms, such as diarrhea and steatorrhea, with a better efficacy if compared to other drugs utilized in the treatment of hyperthyroidism."( Effects of propylthiouracil on intestinal transit time and symptoms in hyperthyroid patients.
Cammarota, G; Capelli, G; Certo, M; Cuoco, L; de Rosa, G; Fedeli, G; Gasbarrini, G; Montalto, M; Papa, A; Tursi, A,
)
0.85
"Treatment with propylthiouracil (PTU) resulted in a significant decrease in azoxymethane-induced intestinal tumors, total concentration of fecal bile acids as well as the fecal neutral steroids, cholesterol and coprostanol. "( Effect of propylthiouracil on intestinal tumor formation by azoxymethane in rats.
Campbell, RL; Lin, YN; Nigro, ND; Singh, DV, 1977
)
1.01
"Treatment with propylthiouracil (PTU; 0.1% in drinking water), which inhibits thyroidal T4 production and peripheral conversion of T4 to T3, resulted in a more rapid reduction in serum T3 levels and increase in serum TSH than those in rats treated with 0.1% MMI."( Effects of hypothyroidism on hypothalamic release of thyrotropin-releasing hormone in rats.
de Greef, WJ; Klootwijk, W; Rondeel, JM; Visser, TJ, 1992
)
0.62
"Treatment with propylthiouracil caused a significant fall in Na+K(+)-ATPase activity of liver and muscle and the normal value was restored in the two organs after three consecutive injections of T4 at the dose of 1 microgram/g."( Thyroid hormone effects upon Na+K+ dependent adenosine triphosphatase activity of microsomal fraction of liver, muscle and brain of toad Bufo melanostictus.
Dey, SS; Medda, AK, 1990
)
0.62
"Treatment with propylthiouracil and insulin and glucagon infusions has also shown promising results in controlled studies but there is still no general agreement on their value."( Treatment of advanced alcoholic liver disease.
Bird, GL; Williams, R, 1990
)
0.62
"Treatment with propylthiouracil was associated with small elevations of serum total protein, urea nitrogen, and creatine concentrations regardless of the method of administration of this agent."( Induction of experimental thyroid dysfunction in rats with implantable pellets of thyroxine or propylthiouracil.
Levy, G; Walker, JS, 1989
)
0.84

Toxicity

The authors studied 389 Graves' hyperthyroid patients receiving either high propylthiouracil (PTU) or methimazole (MMI) daily doses or low doses to evaluate whether adverse effects were related to the thionamide drugs.

ExcerptReferenceRelevance
" Only those rats which received ETU at 125 or 625 ppm and those ingesting PTU or amitrole demonstrated a measurable toxic response."( Dietary subacute toxicity of ethylene thiourea in the laboratory rat.
Baron, RL; Freudenthal, RI; Kerchner, G; Persing, R,
)
0.13
"The authors studied 389 Graves' hyperthyroid patients receiving either high propylthiouracil (PTU) or methimazole (MMI) daily doses or low doses to evaluate whether adverse effects were related to the thionamide drugs or its daily dose regimen."( Adverse effects related to thionamide drugs and their dose regimen.
Bromberg, N; Farah, CS; Romaldini, JH; Werner, MC; Werner, RS, 1989
)
0.51
" It is demonstrated that propylthiouracil-induced hypothyroid-hyperlipidemic chick develops severe toxic manifestations following clofibrate administration."( Propylthiouracil-induced hypothyroid hyperlipidemic chick: a model for clofibrate-induced toxicity.
Cho, C; Linscheer, WG; Raheja, KL, 1986
)
2.02
"Mice given propylthiouracil, a thyroid inhibitor, and fed a diet containing a nontoxic level of rac-1(3)-palmitoyl glycerol showed the hypothermia and mortality expected for a toxic dose, but did not show these signs when linoleate or oleate was added to the diet."( Toxicity of palmitoyl glycerol to mice: depression of thyroid function.
King, MW; Meuten, DJ; Tove, SB; Trumbo, PR, 1987
)
0.66
" Also, the effect of food deprivation of both the euthyroid and PTU-induced hypothyroid rats for 24 h, as well as forced feeding of the euthyroid rats after a toxic dose of APAP, was determined."( Effect of nutritional status on propylthiouracil-induced protection against acetaminophen hepatotoxicity in the rat.
Cho, CD; Hirose, N; Raheja, KL, 1987
)
0.56
" Whereas a toxic dose of acetaminophen administration did not effect SGOT and SGPT levels after 30 hr in PTU pretreated rats given either a single or multiple injections of DEM, the same dose of acetaminophen in the control rats raised these transaminases to a very high level."( Prevention of acetaminophen hepatotoxicity by propylthiouracil in the glutathione depleted rat.
Cho, C; Linscheer, WG; Raheja, KL, 1983
)
0.52
"The aims of the present study were to investigate the incidence of adverse effects of thioureylene antithyroid drugs and to see if there were any factors related to the development of the adverse effects."( [The adverse effects of thioureylene antithyroid drugs (author's transl)].
Inoue, K; Nakashima, T; Nishitani, H; Okabe, N; Okamura, K; Omae, T; Shiroozu, A; Yoshinari, M, 1982
)
0.26
" Provided the results obtained from these animal experiments can be applied to the situation in man, the inhibition of peripheral deiodination could have an adverse effect at least in the treatment of T3-thyrotoxicosis."( Inhibition of peripheral deiodination of 3, 5, 3'-triiodothyronine: an adverse effect of propylthiouracil in the treatment of T3-thyrotoxicosis.
Heinen, E; Herrmann, J; Krüskemper, HL; Moreno, F; Mosny, D; Teschke, R,
)
0.35
" In rare cases, this drug has been found to have severe toxic effects on the liver."( Propylthiouracil hepatotoxicity. A review and case presentation.
Levy, M, 1993
)
1.73
" Possible adverse effects of this therapy include cardiovascular changes (shortening of systolic time intervals, increased frequency of atrial premature beats and, possibly, left ventricular hypertrophy) and bone changes (reduced bone density and bone mass), but the risk of these adverse effects can be minimised by carefully monitoring serum free thyroxine and free liothyronine (triiodothyronine) measurements and adjusting the dosage accordingly."( Adverse effects of thyroid hormone preparations and antithyroid drugs.
Bartalena, L; Bogazzi, F; Martino, E, 1996
)
0.29
" The PTU-induced elevated baseline levels of this inhibitor protein inactivated m-ATPase, and prevented hepatotoxicity by a toxic dose of acetaminophen (AAP) (paracetamol), by maintaining hepatic adenosine 5'-triphosphate (ATP) levels."( Induction of an ATPase inhibitor protein by propylthiouracil and protection against paracetamol (acetaminophen) hepatotoxicity in the rat.
Banerjee, A; Chan, SH; Chiji, H; Cho, C; Linscheer, WG; Murthy, UK; Nandi, J, 1998
)
0.56
"Antithyroid drugs adverse effects are varied and rare."( Systemic adverse effect of antithyroid drugs.
Fain, O; Mathieu, E; Sitbon, M; Thomas, M, 1999
)
0.3
" Further studies of the effectiveness of continuous thionamide therapy in patients with thyrotoxicosis need to be designed and implemented to determine indications for such therapy in children, adolescents and adults with diffuse toxic goiter, in particular, in those who have had recurrence of hyperthyroidism after discontinuation of one complete course of treatment."( The safety and efficacy of antithyroid drugs.
Azizi, F, 2006
)
0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Phenobarbital, Aroclor 1254 and beta-naphthoflavone (indirect toxic mechanism) enhanced thyroidal radioiodide accumulation, and the administration of potassium perchlorate had no effect on thyroid: blood (125)I ratio."( Standardization of the perchlorate discharge assay for thyroid toxicity testing in rats.
Coelho-Palermo Cunha, G; van Ravenzwaay, B, 2007
)
0.34
" Recent studies, indicating that even small changes in the mother's thyroid hormone status early in pregnancy may cause adverse effects on her child, have lead to increased concern for thyroid hormone disrupting chemicals in the environment."( Developmental neurotoxicity of propylthiouracil (PTU) in rats: relationship between transient hypothyroxinemia during development and long-lasting behavioural and functional changes.
Axelstad, M; Boberg, J; Bonnichsen, M; Hansen, PR; Hass, U; Hougaard, KS; Lund, SP; Nellemann, C, 2008
)
0.63
" Over the years that these medications have been used, reports of adverse events involving hepatotoxicity have appeared."( Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children.
Rivkees, SA; Szarfman, A, 2010
)
0.63
" Food and Drug Administration's Adverse Event Reporting System (AERS)."( Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children.
Rivkees, SA; Szarfman, A, 2010
)
0.63
" Hence, there is a constant need to explore newer, effective, orally administered, and cost-effective drugs with minimal adverse effects."( Therapeutic efficacy and safety of propylthiouracil in psoriasis: an open-label study.
Dayalan, H; Gnanaraj, P; Karthikeyan, S; Malligarjunan, H; Narasimhan, M,
)
0.41
"PTU significantly clears the lesions in psoriasis with minimal adverse effects."( Therapeutic efficacy and safety of propylthiouracil in psoriasis: an open-label study.
Dayalan, H; Gnanaraj, P; Karthikeyan, S; Malligarjunan, H; Narasimhan, M,
)
0.41
"Agranulocytosis is a serious adverse effect of antithyroid drugs (ATDs) and mainly develops within three months after the start of uninterrupted ATD treatment."( Characteristics of agranulocytosis as an adverse effect of antithyroid drugs in the second or later course of treatment.
Ito, K; Iwaku, K; Kobayashi, S; Kunii, Y; Matsumoto, M; Mukasa, K; Noh, JY; Ohye, H; Sugino, K; Suzuki, M; Watanabe, N; Yoshihara, A, 2014
)
0.4
"In mice treated with PTU or MMI, no significant histopathological abnormalities or external gross malformations, and no adverse effects on placental weight, litter size, resorption rates, or fetal weight were observed at GD 18."( Evaluation of developmental toxicity of propylthiouracil and methimazole.
Booth, CJ; Mallela, MK; Poulsen, RR; Rivkees, SA; Strobl, M; Wendler, CC, 2014
)
0.67
" The secondary outcomes were liver function indexes and adverse reactions in MMI and PTU groups."( The efficiency and safety of methimazole and propylthiouracil in hyperthyroidism: A meta-analysis of randomized controlled trials.
Chen, L; Fu, X; Jin, L; Tan, S, 2021
)
0.88
" Leukocytoclastic vasculitis is described among dermatologic adverse effects of PTU."( [Leukocytoclastic vasculitis as an adverse effect of propylthiouracil. A case report].
Cortés-Guzmán, JS; Domínguez, JD; Pinzón-Tovar, A; Veloza, KT, 2023
)
1.16

Pharmacokinetics

ExcerptReferenceRelevance
"A pharmacokinetic analysis of propylthiouracil (PTU) plasma concentration versus time data for twelve euthyroid subjects was performed using the NONLIN computer program."( Pharmacokinetics of propylthiouracil upon p.o. administration in man.
Hardt, T; Meyer, MC; Ringhand, HP; Ritschel, WA; Straughn, AB, 1980
)
0.87
" Comparisons of the pharmacokinetic parameters obtained for the euthyroid beagle dog to those reported for euthyroid man12 indicated that the beagle dog is an adequate model for PTU disposition in man."( Effects of thyroid status and choice of USP preparation on the pharmacokinetics of propylthiouracil in the beagle dog.
Bauman, DH; Chen, IW; Maxon, HR; Ringhand, P; Ritschel, WA,
)
0.36
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

Group A patients (n = 31) received either methimazole (40-100 mg daily) or propylthiouracil (400-900mg daily) combined with T3 daily throughout treatment.

ExcerptReferenceRelevance
" Group A patients (n = 31) received either methimazole (40-100 mg daily) or propylthiouracil (400-900 mg daily) combined with T3 daily throughout treatment."( The evolution of Graves' ophthalmopathy during treatment with antithyroid drug alone and combined with triiodothyronine.
Bromberg, N; Romaldini, JH; Sgarbi, JA; Werner, MC; Werner, RS, 1992
)
0.51
" The present preliminary investigation served to assess the effects of oral consumption of perchlorate, alone and in combination with ethanol, on thyroid hormone and brain catecholamine concentrations in female rats of gestational age."( The effect of oral consumption of perchlorate, alone and in combination with ethanol, on plasma thyroid hormone and brain catecholamine concentrations in the rat.
James-Walke, NL; McMillen, BA; Taylor, DA; Williams, HL, 2006
)
0.33
"Carrier-mediated three-phase hollow fiber microextraction combined with high-performance liquid chromatography-ultra violet detection (HPLC-UV) was applied for the extraction and determination of propylthiouracil in biological samples."( Optimization of carrier-mediated three-phase hollow fiber microextraction combined with HPLC-UV for determination of propylthiouracil in biological samples.
Abedi, H; Asgharinezhad, AA; Ebrahimzadeh, H; Kamarei, F, 2011
)
0.77

Bioavailability

The bioavailability of propylthiouracil (about 80%) was unchanged by the surgical procedure. The fraction of ampicillin (given as pivampicillin) absorbed decreased from a preoperative value of 109 +/- 44% to 44 +/- 30%.

ExcerptReferenceRelevance
" While no significant differences could be demonstrated between the two age groups concerning volumes of distribution, clearance and extent of absorption, a large difference was found with regard to the absorption rate constant ka, which was about 3 times higher in the younger than in the elderly subjects, presumably due a reduced gastric emptying time."( Kinetics of propylthiouracil in the elderly.
Bach, B; Hansen, JM; Kampmann, JP; Kristensen, MB; Mortensen, HB; Waldorff, S, 1979
)
0.64
" The method is sufficiently sensitive for most bioavailability and pharmacokinetic studies."( High-pressure liquid chromatographic determination of propylthiouracil in human plasma.
Ringhand, HP; Ritschel, WA, 1979
)
0.51
"The bioavailability of 6-propylthiouracil (PTU) has been examined in eight healthy volunteers, with respect to interindividual variation and influence of food intake."( Bioavailability of propylthiouracil: Interindividual variation and influence of food intake.
Danielson, K; Hanson, A; Melander, A; Wåhlin, E, 1977
)
0.89
" Following oral administration, both the bioavailability (59."( Altered disposition of propylthiouracil in cats with hyperthyroidism.
Aucoin, DP; Davis, CA; Graves, TK; Peterson, ME, 1988
)
0.59
" The bioavailability of propylthiouracil (about 80%) was unchanged by the surgical procedure but the fraction of ampicillin (given as pivampicillin) absorbed decreased from a preoperative value of 109 +/- 44% to 44 +/- 30% 12 months after the bypass operation."( Ampicillin and propylthiouracil pharmacokinetics in intestinal bypass patients followed up to a year after operation.
Kampmann, JP; Klein, H; Lumholtz, B; Mølholm Hansen, JE,
)
0.79
" Bioavailability data from euthyroid, hyperthyroid, and hypothyroid beagle dogs indicated that the rate of PTU absorption varied appreciably between the two generic products studied."( Effects of thyroid status and choice of USP preparation on the pharmacokinetics of propylthiouracil in the beagle dog.
Bauman, DH; Chen, IW; Maxon, HR; Ringhand, P; Ritschel, WA,
)
0.36
" The bioavailability of propylthiouracil in dogs from the hydrophilic matrices investigated was low, because of the short gastro-intestinal transit times of the matrix tablets in the dogs."( In vitro and in vivo evaluation in dogs and pigs of a hydrophilic matrix containing propylthiouracil.
Kabanda, L; Lefebvre, RA; Remon, JP; Van Bree, HJ, 1994
)
0.82
" Measurement of 24-h urinary-free iodide indicated that the bioavailability of potassium iodide delivered by retention enema was at least 40%."( Rectal administration of iodide and propylthiouracil in the treatment of thyroid storm.
Balasubramanyam, A; Go, R; Yeung, SC, 1995
)
0.57
"To reduce the number of administrations of propylthiouracil required to treat hyperthyroidism, the bioavailability and sustained-release characteristics of 300 mg propylthiouracil formulated in hydrophilic matrix tablets were evaluated after single oral administration in healthy male volunteers."( In-vivo evaluation in man of a hydrophilic matrix containing propylthiouracil.
Kabanda, L; Lefebvre, RA; Remon, JP, 1996
)
0.8
" In constant oxidative stress (ageing and liver regeneration after partial hepatectomy), high liver Zn-MTs, low zinc ion bioavailability and depressed TTA efficiency appear."( Metallothioneins (I+II) and thyroid-thymus axis efficiency in old mice: role of corticosterone and zinc supply.
Carpenè, E; Cipriano, C; Gasparini, N; Giacconi, R; Isani, G; Mocchegiani, E; Muzzioli, M; Orlando, F; Stecconi, R, 2002
)
0.31
" The enema form appeared to provide better bioavailability than the suppository form."( Rectal administration of propylthiouracil in hyperthyroid patients: comparison of suspension enema and suppository form.
Akarawut, W; Chailurkit, L; Chantasart, D; Jongjaroenprasert, W; Rajatanavin, R, 2002
)
0.62
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" The authors also extensively discuss the details regarding the pharmacology, bioactivation, biodisposition, bioavailability and pharmacokinetic properties of the two main ATD (MMI and PTU)."( Toxicological considerations for antithyroid drugs in children.
Karras, S; Krassas, GE; Tzotzas, T, 2011
)
0.37
" Food administration increased the Tmax and decreased the bioavailability (Cmax and AUC)."( Propylthiouracil quantification in human plasma by high-performance liquid chromatography coupled with electrospray tandem mass spectrometry: application in a bioequivalence study.
Arruda, AM; Babadópulos, T; Bittencourt, S; De Nucci, G; Frecentese, F; Gagliano-Jucá, T; Mendes, GD; Perissutti, E; Vespasiano, CF, 2014
)
1.85
" Moreover, we found that ZINC39395747 significantly increased NO bioavailability in renal vascular cells, augmented renal blood flow, and decreased systemic blood pressure in response to vasoconstrictors in spontaneously hypertensive rats."( Structure Guided Chemical Modifications of Propylthiouracil Reveal Novel Small Molecule Inhibitors of Cytochrome b5 Reductase 3 That Increase Nitric Oxide Bioavailability.
Alvarez, RA; Camacho, CJ; Chen, BB; Cheng, D; Jackson, EK; Koes, D; Miller, MP; Mutchler, SM; Nguyen, AT; Rahaman, MM; Reinders, FG; Sparacino-Watkins, C; Straub, AC, 2015
)
0.68
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A 49-year-old woman treated with increasing dosage of propylthiouracil (PTU) in order to control hyperthyroidism developed progressive necrotic ulcers in the oral cavity, oropharynx and rhinopharynx.

ExcerptRelevanceReference
" The response to the divided dosage schedule was prompt and predictable, and by ten weeks all but one patient had achieved remission."( Prospective randomized comparison of propylthiouracil.
Gwinup, G, 1978
)
0.53
" Similarly, injection of PTU in rats in a dosage of 5 microgram/100 g BW or greater significantly impaired T4 5'-deiodination in subsequently isolated kidney microsomal preparations."( Thyroxine 5'-deiodinase activity of rat kidney: observations on activation by thiols and inhibition by propylthiouracil.
Leonard, JL; Rosenberg, IN, 1978
)
0.47
" Two features of the previously proposed scheme were tested:1) the effects of drug dosage and 2) the effects of iodine deficiency."( Mechanism of action of thioureylene antithyroid drugs: factors affecting intrathyroidal metabolism of propylthiouracil and methimazole in rats.
Nakashima, T; Riesco, G; Taurog, A, 1978
)
0.47
" After the addition of increasing doses of PTU (40--400 ng/ml) a linear increase of FT4 was found in human serum, while in rat serum a nonlinear dose-response relationship was observed."( Increase of serum free thyroxine after propylthiouracil in vitro or its peroral administration to rats.
Michajlovskij, N; Stastná, M, 1976
)
0.52
" Rat liver and kidney microsomes produced dose-response curves that were essentially parallel to that of LAP-744."( A radioimmunoassay of rat type I iodothyronine 5'-monodeiodinase.
Chopra, IJ; Santini, F, 1992
)
0.28
" Patient 3 fell into hypothyroidism when receiving a small dosage of methimazole."( Three patients who spontaneously developed persistent hypothyroidism during or following treatment with antithyroid drugs for Graves' hyperthyroidism.
Adachi, T; Mashiba, H; Mitani, Y; Miyazaki, S; Shigemasa, C; Tanaka, T; Taniguchi, S; Ueta, Y; Urabe, K; Yoshida, A, 1990
)
0.28
" The aim of the present study was to examine the apparently very steep dose-response relationship between elevated plasma TSH and thyroid vascular C/mass."( Thyroid vascular conductance: differential effects of elevated plasma thyrotropin (TSH) induced by treatment with thioamides or TSH-releasing hormone.
Chang, BS; Connors, JM; Dey, RD; Hedge, GA; Huffman, LJ; Michalkiewicz, M, 1991
)
0.28
" The dose-response curves for both agonists were shifted to the left in the hypothyroid rats compared to water-treated controls."( The hypothyroid rat as a model of increased sensitivity to dopamine receptor agonists.
Cameron, DL; Crocker, AD, 1990
)
0.28
" One hundred and eighty-six were given a dose adjusted for thyroid size and radioactive iodine uptake (Protocol 1), and a second group received the same dosage followed by antithyroid drug therapy plus potassium iodide for 15 days (Protocol 2)."( Comparison of RA 131I treatment protocols for Graves' disease.
DeGroot, LJ; Mangklabruks, A; McCormick, M, 1990
)
0.28
" These findings indicate that high free thyroxine levels and the presence of antibodies that inhibit binding of thyrotropin are useful indexes of the fetal need for antithyroid treatment, and that the thionamide dosage that maintains maternal free thyroxine levels in a mildly thyrotoxic range seems appropriate for maintaining euthyroid status in the fetus."( Antithyroid drug therapy for Graves' disease during pregnancy. Optimal regimen for fetal thyroid status.
Ishikawa, N; Ito, K; Momotani, N; Noh, J; Oyanagi, H, 1986
)
0.27
" Although most side effects were not dangerous, in normal instances the lowest possible dosage should be administered to control hyperthyroid metabolism."( [Side effects of antithyroid therapy of hyperthyroidism. A study of 1256 continuously treated patients].
Benker, G; Cissewski, K; Meyer-Gessner, M; Olbricht, T; Reiners, C; Reinwein, D; Windeck, R, 1989
)
0.28
" Thus, studies of altered thyroid status in the rat reveal dose-response and time-course variability in the pretranslational control of TSH beta, alpha-subunit, GH, and PRL by thyroid hormone."( The effect of altered thyroid status on pituitary hormone messenger ribonucleic acid concentrations in the rat.
Ridgway, EC; Samuels, MH; Wang, C; Wierman, ME, 1989
)
0.28
" Pregnant rats were dosed with PTU during gestation and/or lactation, and on postnatal day 28, auditory startle responses were measured to determine if PTU altered functional development."( Relative cerebellar weight: a potential indicator of developmental neurotoxicity.
Guerriero, FJ; Toscano, TV; Walker, RF; Weideman, CA,
)
0.13
" At the higher dosage used bovine GH appeared to stimulate the accumulation of creatine kinase."( The postnatal development of sarcoplasmic reticulum Ca2+ transport activity in skeletal muscle of the rat is critically dependent on thyroid hormone.
Simonides, WS; van Hardeveld, C, 1989
)
0.28
"Thyrotrophin-releasing hormone (TRH) occurs in high concentrations in the rat ventral prostate and its concentrations is regulated in a positive dose-response manner by testosterone in castrated rats."( Thyroid hormone modulation of thyrotrophin-releasing hormone (TRH) and TRH-Gly levels in the male rat reproductive system.
Bhasin, S; Hershman, JM; Pekary, AE; Smith, V; Sugawara, M; Swerdloff, RS, 1987
)
0.27
" Elevated plasma reverse T3 levels were demonstrated after each treatment, however, suggesting a desirable therapeutic effect at this dosage level for all preparations."( Rectal absorption of propylthiouracil.
Bartle, WR; Silverberg, JD; Walker, SE, 1988
)
0.59
"2% solution of PTU was administered at a dosage of 2 microliter/gm embryo weight on embryonic day nine (E9)."( Neuronal development in the trigeminal mesencephalic nucleus of the duck under normal and hypothyroid states: I. A light microscopic morphometric analysis.
Narayanan, CH; Narayanan, Y, 1987
)
0.27
" No specific clinical subgroup at high risk can be identified, and manifestations may occur at any dosage and at any time during therapy."( Adverse immunologic effects of antithyroid drugs.
Fantus, IG; Wing, SS, 1987
)
0.27
"2% PTU diets, and a dose-response relationship was established."( Propylthiouracil causes phase delays and circadian period lengthening in male and female hamsters.
Gavin, ML; Morin, LP; Ottenweller, JE, 1986
)
1.71
" The mean daily dosage of PTU was 827 (n=11) and of MMI was 88 (n=8)."( Triiodothyronine and thyroxine in hyperthyroidism. Comparison of the acute changes during therapy with antithyroid agents.
Abuid, J; Larsen, PR, 1974
)
0.25
" No detectable change in T(4) deiodination rate was observed with these agents in the dosage ranges employed in this study."( A new method for the measurement of acute alterations in thyroxine deiodination rate in man.
Nicoloff, JT, 1970
)
0.25
" Some dosage schedules of antithyroid drugs are considered, and some techniques for predicting remission status and relapse of disease are reported."( [Hyperthyroidism in children (author's transl)].
Bozzola, M; Cisternino, M; Larizza, D; Livieri, C; Lorini, R; Salvatoni, A; Severi, F,
)
0.13
"Appropriate dosage of levothyroxine for the treatment of hypothyroidism is assessed by determining the serum thyroxine (T4) concentration in secondary and tertiary types."( Laboratory tests for evaluating thyroid therapy.
Kabadi, UM, 1982
)
0.26
" These results support the hypothesis that large antithyroid drug doses may have greater immunosuppressive effects than low dosage regimens."( Comparison of effects of high and low dosage regimens of antithyroid drugs in the management of Graves' hyperthyroidism.
Bromberg, N; Farah, CS; Reis, LC; Rodrigues, HF; Romaldini, JH; Tanaka, LM; Werner, MC; Werner, RS, 1983
)
0.27
" A dose-response relationship existed between the hTSH dose injected and the duration and magnitude of suppression of rabbit TSH."( Autoregulatory control of thyrotropin in rabbits.
Kakita, T; Laborde, NP; Odell, WD, 1984
)
0.27
" These results indicate that short-term ethanol dosing does not affect PTU disposition and therefore dosage adjustment is not necessary in patients who drink alcohol."( Effect of alcohol on propylthiouracil disposition.
Bennett, J; Dorian, P; Giles, HG; Long, JP; Orrego, H; Sellers, EM; Thiessen, JJ, 1983
)
0.58
" The clinical implications of our findings are discussed with relation to the dosage schedule commonly employed in the treatment of Graves' disease with antithyroid drugs."( Mechanism of action of thioureylene antithyroid drugs in the rat: possible inactivation of thyroid peroxidase by propylthiouracil.
Dorris, ML; Engler, H; Shiroozu, A; Taurog, A, 1983
)
0.48
"Intramuscular injection of staphylococcal enterotoxin B (SEB) at a dosage level of 50 microgram/kg of body weight caused death in Dutch rabbits."( Modification of lethality induced by staphylococcal enterotoxin B in Dutch rabbits.
Liu, CT; Sanders, RP, 1980
)
0.26
" In the management of hypothyroidism during pregnancy thyroxine dose may require to be increased but excess dosage should be avoided because of its unwanted effects on foetal cerebral maturation."( Thyroxine excess and pregnancy.
Lazarus, JH, 1994
)
0.29
" Furthermore, the shrinkage of thyroid glands may further decrease the radioiodine dosage in patients with Graves' disease."( Therapeutic 131I dose in hyperthyroidism: role of pretreatment with thionamide.
Cech, R; Kabadi, U, 1994
)
0.29
" Ethanol stimulated iodide uptake in a dose-response manner in TSH-free medium."( Ethanol has thyrotropin-like activity in cultured porcine thyroid follicles.
Nasu, M; Sugawara, M, 1993
)
0.29
" Possible adverse effects of this therapy include cardiovascular changes (shortening of systolic time intervals, increased frequency of atrial premature beats and, possibly, left ventricular hypertrophy) and bone changes (reduced bone density and bone mass), but the risk of these adverse effects can be minimised by carefully monitoring serum free thyroxine and free liothyronine (triiodothyronine) measurements and adjusting the dosage accordingly."( Adverse effects of thyroid hormone preparations and antithyroid drugs.
Bartalena, L; Bogazzi, F; Martino, E, 1996
)
0.29
"Propylthiouracil discontinued 4-7 days before radioiodine dosing is associated with a significant increase in the failure rate of a single dose of radioiodine."( The effect of propylthiouracil on subsequent radioactive iodine therapy in Graves' disease.
Bauman, J; Hancock, LD; LeMar, H; Patience, T; Tuttle, RM, 1997
)
2.1
" In a dose-response study half-maximal stimulation by T4 was achieved at a concentration of 100 nM, whereas 50% of maximal induction was produced by 1 nM T3 and 6 nM triiodothyroacetic acid (TRIAC)."( L-thyroxine directly affects expression of thyroid hormone-sensitive genes: regulatory effect of RXRbeta.
Bartalena, L; Bogazzi, F; Brogioni, S; Burelli, A; Dell'Unto, E; Grasso, L; Manetti, L; Martino, E, 1997
)
0.3
" The patients were under propylthiouracil (PTU) therapy at a dosage of 3 x 100 mg/day for one month."( The impact of propylthiouracil therapy on lipid peroxidation and antioxidant status parameters in hyperthyroid patients.
Burcak, G; Hatemi, H; Seven, A; Tasan, E, 1999
)
0.97
"A 49-year-old woman treated with increasing dosage of propylthiouracil (PTU) in order to control hyperthyroidism, developed progressive necrotic ulcers in the oral cavity, oropharynx and rhinopharynx and vasculitic ulcers on both auricular pinnae after a few days."( Anti-neutrophil cytoplasmic antibody-associated mucocutaneous allergic vasculitis with oral manifestations caused by propylthiouracil.
Sorribes, MM; Stangerup, SE; Welinder, NR, 1999
)
0.76
" In two similar experiments, weanling female rats were dosed for 20 days by gavage with vehicle (0."( Evaluation of the EDSTAC female pubertal assay in CD rats using 17beta-estradiol, steroid biosynthesis inhibitors, and a thyroid inhibitor.
Carney, EW; Crissman, JW; Marty, MS, 1999
)
0.3
" The lytic activity of serum from animals treated with a single PTU dose of 50 mg/200 g body weight and sacrificed 1-48 h after dosing did not differ from controls."( The effect of the antithyroid drug propylthiouracil on the alternative pathway of complement in rats.
Azzolini, AE; de Assis Pandochi, AI; dos Santos, GL; Duarte, CG, 2000
)
0.58
" The fetal thyroid status, investigated by percutaneous fetal umbilical cord blood sampling, was normal and the reduction of PTU dosage was sufficient to decrease goitre volume."( [Treatment of maternal hyperthyroidism and fetal goiter].
Andreotti, C; Arreghini, A; Bellini, P; Kirm, V; Marinetti, E; Roncaglia, N,
)
0.13
" Weanling male CD rats (21 days old) were dosed for 30 d by gavage with vehicle (0."( Evaluation of the male pubertal assay's ability to detect thyroid inhibitors and dopaminergic agents.
Carney, EW; Crissman, JW; Marty, MS, 2001
)
0.31
" In the case of a pre-existing hypothyroidism a 25-50% increase in the levothyroxine dosage is often needed during the first trimester of pregnancy."( [Pregnancy (conception) in hyper- or hypothyroidism].
Boer, K; Corssmit, EP; Prummel, MF; Wiersinga, WM, 2001
)
0.31
" Excipients present in the dosage forms did not interfere with the analysis, and the recovery of PTU from each dosage form was quantitative."( Development and validation of a high-performance liquid chromatographic method for the analysis of propylthiouracil in pharmaceuticals.
Abdul-Fattah, AM; Bhargava, HN, 2001
)
0.53
" There remains, however, significant variability among (131)I dosing regimens, and it is clear that most patients ultimately develop hypothyroidism after therapy."( High dose of (131)I therapy for the treatment of hyperthyroidism caused by Graves' disease.
Alexander, EK; Larsen, PR, 2002
)
0.31
" There were no significant differences in age, duration, or dosage between the MPO-ANCA positive and negative patients."( Prevalence of serum anti-myeloperoxidase antineutrophil cytoplasmic antibodies (MPO-ANCA) in patients with Graves' disease treated with propylthiouracil and thiamazole.
Ito, T; Kohno, M; Mukai, M; Notoya, A; Wada, N; Yoshioka, N, 2002
)
0.52
" For the current studies, male rats were dosed for 15 days via oral gavage and euthanized on the morning of test day 15."( Evaluation of a 15-day screening assay using intact male rats for identifying steroid biosynthesis inhibitors and thyroid modulators.
Frame, SR; Ladics, GS; O'Connor, JC, 2002
)
0.31
" When a dosage reduction does not cause a decrease in fetal thyroid size, transplacental passage of thyroid-stimulating antibodies causing fetal thyrotoxicosis should be suspected."( Serial in utero ultrasonographic measurements of the fetal thyroid: a new complementary tool in the management of maternal hyperthyroidism in pregnancy.
Achiron, R; Cohen, O; Dolitski, M; Lipitz, S; Pinhas-Hamiel, O; Sivan, E, 2003
)
0.32
" CPI was studied in relation to the cytologic parameters of the smears; clinical parameters, such as Wayne's Clinical Index (WCI) and time without treatment; laboratory parameters, such as 131I uptake and dosage of serum free thyroxin and thyroid-stimulating hormone; and thyroid ultrasound."( Thyroid cell proliferation in Graves' disease. Use of MIB-1 monoclonal antibody.
Aragon, FF; Mazeto, GM; Montenegro, MR; Oliveira, ML; Padovani, CR; Schmitt, FC,
)
0.13
" Based on the above findings, the mother's PTU dosage was reduced to 50 mg daily from a total of 150 mg and weekly ultrasonographic examinations were performed."( Non-invasive management of fetal goiter during maternal treatment of hyperthyroidism in Grave's disease.
Eroglu, D; Gurakan, B; Kinik, ST; Kuscu, E; Lembet, A,
)
0.13
" The present study was performed to examine the dose-response relationships of moderate levels of hormone disruption on synaptic function in the dentate gyrus in an in vivo preparation and to determine the effects on spatial learning."( Dose-dependent reductions in spatial learning and synaptic function in the dentate gyrus of adult rats following developmental thyroid hormone insufficiency.
Gilbert, ME; Sui, L, 2006
)
0.33
" The PTU dosage was first decreased but pericardial, dermal and joint involvement ascribed to PTU developed later and the drug was discontinued."( Propylthiouracil-induced hypersensitivity syndrome.
Arhan, E; Aycan, Z; Cakar, N; Cetinkaya, E; Menekşe, N; Vidinlisan, S; Yücel, H,
)
1.57
" Using stepwise multivariate logistic regression, the authors could not identify any factors (including age, gender, family history of thyroid diseases, size of goiter, level of free T4, dosage and duration of antithyroid drugs) that would predict the remission of thyrotoxicosis with antithyroid drugs."( Thyrotoxicosis in children: treatment and outcome.
Jaruratanasirikul, S; Leethanaporn, K; Sriplung, H, 2006
)
0.33
" After 15 days, the 40 mg dosage was decreased to 20mg/kg body weight for an additional 20 days (35 days of PTU)."( Serum thyroid hormones and performance of offspring in ewes receiving propylthiouracil with or without melatonin.
Duffey, JL; Gifford, CA; Hallford, DM; Knight, RL, 2007
)
0.57
" Failure to recommend increased thyroxine dosage early in pregnancy (thus placing the offspring of women being treated for hypothyroidism at risk of impaired fetal brain development)."( Barriers in the quest for quality drug information: salutary lessons from TGA-approved sources for thyroid-related medications.
Stockigt, JR, 2007
)
0.34
" The histological measurements revealed clear dose-response relationships in both follicular cross-section area and epithelial cell height, with lowest observed effect concentrations (LOECs) recorded at 2 and 5mg/L, respectively."( The impact of the goitrogen 6-propylthiouracil (PTU) on West-African clawed frog (Xenopus tropicalis) exposed during metamorphosis.
Carlsson, G; Norrgren, L, 2007
)
0.63
" Plasma was collected for free T4 dosage and the spleen for histomorphometry analysis, apoptosis index and the immunohistochemistry expression of caspase 3 and CDC47."( [Apoptosis, proliferation and spleen histomorphometry of adult female rats with thyroid and ovarian hypofunction].
Gomes, MG; Moro, L; Ocarino, NM; Ribeiro, AF; Serakides, R; Silva, CM; Vasconcelos, AC, 2008
)
0.35
" Sprague-Dawley rat dams were dosed from the first day of gestation until weaning with methylmercury (MeHg), polychlorinated biphenyls (PCBs) or organochlorines pesticides (OCs) administered either separately or together in the NCM."( Contribution of methylmercury, polychlorinated biphenyls and organochlorine pesticides to the toxicity of a contaminant mixture based on Canadian Arctic population blood profiles.
Alwis, R; Black, P; Bowers, WJ; Chu, I; Kumarathasan, P; Masson, S; Mohottalage, S; Nakai, J; Pelletier, G; Vincent, R; Wade, MJ, 2009
)
0.35
"04), but there were no significant differences in age, gender, duration of PTU therapy or dosage of PTU."( A long-term follow-up of serum myeloperoxidase antineutrophil cytoplasmic antibodies (MPO-ANCA) in patients with Graves disease treated with propylthiouracil.
Ando, T; Ashizawa, K; Eguchi, K; Ejima, E; Horie, I; Ide, A; Imaizumi, M; Ishii, R; Sera, N; Ueki, I; Usa, T, 2010
)
0.56
" The propylthiouracil dosage was not necessary high."( Clinical features and outcomes in patient with antineutrophil cytoplasmic autoantibody-positive glomerulonephritis associated with propylthiouracil treatment in Siriraj Hospital.
Chanchairujuira, T; Choensuchon, B; Ong-Ajyooth, L; Parichatikanond, P; Visavachaipan, N, 2010
)
1.08
" Males were more affected by PTU than females, BDNF levels in hippocampus and cortex were altered but not those in cerebellum, and biphasic dose-response functions were detected in both sexes."( Developmental thyroid hormone insufficiency reduces expression of brain-derived neurotrophic factor (BDNF) in adults but not in neonates.
Gilbert, ME; Lasley, SM,
)
0.13
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Biphasic dose-response profiles were evident in some measures (trace fear conditioning and LTP) but not others and serve to exemplify the complexity of the role of TH in brain development and its consequences for brain function."( Impact of low-level thyroid hormone disruption induced by propylthiouracil on brain development and function.
Gilbert, ME, 2011
)
0.61
" To monitor dosage of antithyroid drugs, approximately 73% of responders used TSH and free T4 (FT4) levels without free T3 (FT3) (53%) or with FT3 (20%)."( Management of hyperthyroidism during pregnancy in Asia.
Akamizu, T; Alamdari, S; Amouzegar, A; Azizi, F; Mehran, L; Poppe, K; San Luis, T; Sarvghadi, F; Subekti, I; Vaidya, B, 2014
)
0.4
" In the present study, we report the dose-response characteristics of this developmental malformation and the connectivity of heterotopic neurones with other brain regions, as well as their functionality."( Subcortical band heterotopia in rat offspring following maternal hypothyroxinaemia: structural and functional characteristics.
Gilbert, ME; Goodman, JH; McCloskey, DP; Ramos, RL, 2014
)
0.4
"Recommended dosage of oral nicotine replacement therapy (NRT) product is often not achieved in smoking cessation attempts."( Relationships of PROP Taste Phenotype, Taste Receptor Genotype, and Oral Nicotine Replacement Use.
Ahijevych, K; Graham, MC; Holloman, C; Matcham, WA; Tepper, BJ, 2015
)
0.42
" SBH increased with increasing dosage of PTU, but counter to our hypothesis, no SBH was detected in the offspring of FeD dams."( Thyroid hormone-dependent formation of a subcortical band heterotopia (SBH) in the neonatal brain is not exacerbated under conditions of low dietary iron (FeD).
Anderson, GW; Bastian, TW; Gilbert, ME; Kosian, P; Spring, SR; Wang, Y,
)
0.13
" The goal of the current experiments was to explore dose-response relations between graded levels of TH insufficiency during development and the visual function of adult offspring."( Moderate perinatal thyroid hormone insufficiency alters visual system function in adult rats.
Boyes, WK; Degn, L; George, BJ; Gilbert, ME, 2018
)
0.48
" Timed-pregnant National Center for Toxicological Research Sprague-Dawley rats (strain code 23) were dosed by gavage with vehicle control (0."( CLARITY-BPA: Bisphenol A or Propylthiouracil on Thyroid Function and Effects in the Developing Male and Female Rat Brain.
Bansal, R; Zoeller, RT, 2019
)
0.81
" A quantitative model was constructed by contrasting in vitro and ex vivo AUR-TPO results and the in vivo time-course and dose-response analysis."( Extrapolating In Vitro Screening Assay Data for Thyroperoxidase Inhibition to Predict Serum Thyroid Hormones in the Rat.
Brennan, A; El-Masri, H; Ford, J; Gilbert, ME; Handa, S; Hassan, I; Paul Friedman, K, 2020
)
0.56
" Methimazole is usually the preferred thionamide for the treatment of hyperthyroidism if the patient is not planning to conceive or not in the first trimester of pregnancy, given the less frequent dosing and lower risk of hepatotoxicity."( Desensitization to Methimazole.
Emanuele, MA; Espiritu, B; Mazhari, A, 2021
)
0.62
" This paper presents the data of the study where 6-propylthiouracil (6-PTU, 10 ppm) and sodium phenobarbital (NaPB, 1000 ppm) were dosed by feeding from gestational days (GD)6-20, and from GD6 to lactation day 21."( Feasibility study for a downsized comparative thyroid assay with measurement of brain thyroid hormones and histopathology in rats: Case study with 6-propylthiouracil and sodium phenobarbital at high dose.
Aoyama, H; Fukuda, T; Hojo, H; Iwashita, K; Kosaka, T; Minami, K; Ogata, K; Sato, A; Suto, H; Takahashi, N; Tomiyama, N; Yamada, T, 2023
)
1.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
antithyroid drugA drug used to treat hyperthyroidism by reducing the excessive production of thyroid hormones.
carcinogenic agentA role played by a chemical compound which is known to induce a process of carcinogenesis by corrupting normal cellular pathways, leading to the acquistion of tumoral capabilities.
antimetaboliteA substance which is structurally similar to a metabolite but which competes with it or replaces it, and so prevents or reduces its normal utilization.
hormone antagonistA chemical substance which inhibits the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
EC 1.14.13.39 (nitric oxide synthase) inhibitorAn EC 1.14.13.* (oxidoreductase acting on paired donors, incorporating 1 atom of oxygen, with NADH or NADPH as one donor) inhibitor that interferes with the action of nitric oxide synthase (EC 1.14.13.39).
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
antidote to paracetamol poisoningA role borne by a molecule that acts to counteract or neutralize the deleterious effects of paracetamol (acetaminophen).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
pyrimidinethione
[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
thyroid hormone metabolism II (via conjugation and/or degradation)632
thyroid hormone metabolism I (via deiodination)414

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.74070.140911.194039.8107AID2451
interleukin 8Homo sapiens (human)Potency74.97800.047349.480674.9780AID651758
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency20.59620.000811.382244.6684AID686979
thyroid stimulating hormone receptorHomo sapiens (human)Potency10.00000.001318.074339.8107AID926; AID938
EWS/FLI fusion proteinHomo sapiens (human)Potency35.19730.001310.157742.8575AID1259255; AID1259256
pregnane X nuclear receptorHomo sapiens (human)Potency70.75760.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency24.04200.000229.305416,493.5996AID743075; AID743079
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency63.62610.001024.504861.6448AID743212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency44.66840.001019.414170.9645AID588537
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency0.00160.023723.228263.5986AID588543
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency3.16230.00255.840031.6228AID899
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency42.16320.000627.21521,122.0200AID651741
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency50.11870.425612.059128.1838AID504891
gemininHomo sapiens (human)Potency2.27700.004611.374133.4983AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency0.00090.891312.067628.1838AID1487
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
NADH-cytochrome b5 reductase 3 Homo sapiens (human)IC50 (µMol)279.40008.20008.20008.2000AID1639923
MyeloperoxidaseHomo sapiens (human)IC50 (µMol)2.81000.02001.88117.6800AID1256926
Thyroid peroxidaseHomo sapiens (human)IC50 (µMol)3.38000.40001.69253.3800AID1256929
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Taste receptor type 2 member 38Homo sapiens (human)EC50 (µMol)2.00000.00491.36102.3000AID1619468
[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)
Taste receptor type 2 member 38Homo sapiens (human)Activity0.30000.15003.256310.0000AID1619467
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cholesterol biosynthetic processNADH-cytochrome b5 reductase 3 Homo sapiens (human)
nitric oxide biosynthetic processNADH-cytochrome b5 reductase 3 Homo sapiens (human)
blood circulationNADH-cytochrome b5 reductase 3 Homo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
response to yeastMyeloperoxidaseHomo sapiens (human)
hypochlorous acid biosynthetic processMyeloperoxidaseHomo sapiens (human)
respiratory burst involved in defense responseMyeloperoxidaseHomo sapiens (human)
defense responseMyeloperoxidaseHomo sapiens (human)
response to oxidative stressMyeloperoxidaseHomo sapiens (human)
response to mechanical stimulusMyeloperoxidaseHomo sapiens (human)
removal of superoxide radicalsMyeloperoxidaseHomo sapiens (human)
response to foodMyeloperoxidaseHomo sapiens (human)
response to lipopolysaccharideMyeloperoxidaseHomo sapiens (human)
low-density lipoprotein particle remodelingMyeloperoxidaseHomo sapiens (human)
hydrogen peroxide catabolic processMyeloperoxidaseHomo sapiens (human)
negative regulation of apoptotic processMyeloperoxidaseHomo sapiens (human)
defense response to fungusMyeloperoxidaseHomo sapiens (human)
response to gold nanoparticleMyeloperoxidaseHomo sapiens (human)
defense response to bacteriumMyeloperoxidaseHomo sapiens (human)
thyroid hormone generationThyroid peroxidaseHomo sapiens (human)
response to oxidative stressThyroid peroxidaseHomo sapiens (human)
embryonic hemopoiesisThyroid peroxidaseHomo sapiens (human)
hormone biosynthetic processThyroid peroxidaseHomo sapiens (human)
hydrogen peroxide catabolic processThyroid peroxidaseHomo sapiens (human)
cellular oxidant detoxificationThyroid peroxidaseHomo sapiens (human)
detection of chemical stimulus involved in sensory perception of bitter tasteTaste receptor type 2 member 38Homo sapiens (human)
G protein-coupled receptor signaling pathwayTaste receptor type 2 member 38Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
nitrite reductase (NO-forming) activityNADH-cytochrome b5 reductase 3 Homo sapiens (human)
cytochrome-b5 reductase activity, acting on NAD(P)HNADH-cytochrome b5 reductase 3 Homo sapiens (human)
protein bindingNADH-cytochrome b5 reductase 3 Homo sapiens (human)
AMP bindingNADH-cytochrome b5 reductase 3 Homo sapiens (human)
ADP bindingNADH-cytochrome b5 reductase 3 Homo sapiens (human)
NAD bindingNADH-cytochrome b5 reductase 3 Homo sapiens (human)
FAD bindingNADH-cytochrome b5 reductase 3 Homo sapiens (human)
chromatin bindingMyeloperoxidaseHomo sapiens (human)
peroxidase activityMyeloperoxidaseHomo sapiens (human)
protein bindingMyeloperoxidaseHomo sapiens (human)
heparin bindingMyeloperoxidaseHomo sapiens (human)
heme bindingMyeloperoxidaseHomo sapiens (human)
metal ion bindingMyeloperoxidaseHomo sapiens (human)
iodide peroxidase activityThyroid peroxidaseHomo sapiens (human)
peroxidase activityThyroid peroxidaseHomo sapiens (human)
calcium ion bindingThyroid peroxidaseHomo sapiens (human)
heme bindingThyroid peroxidaseHomo sapiens (human)
G protein-coupled receptor activityTaste receptor type 2 member 38Homo sapiens (human)
bitter taste receptor activityTaste receptor type 2 member 38Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
endoplasmic reticulum membraneNADH-cytochrome b5 reductase 3 Homo sapiens (human)
extracellular regionNADH-cytochrome b5 reductase 3 Homo sapiens (human)
cytoplasmNADH-cytochrome b5 reductase 3 Homo sapiens (human)
mitochondrionNADH-cytochrome b5 reductase 3 Homo sapiens (human)
mitochondrial outer membraneNADH-cytochrome b5 reductase 3 Homo sapiens (human)
endoplasmic reticulumNADH-cytochrome b5 reductase 3 Homo sapiens (human)
endoplasmic reticulum membraneNADH-cytochrome b5 reductase 3 Homo sapiens (human)
lipid dropletNADH-cytochrome b5 reductase 3 Homo sapiens (human)
membraneNADH-cytochrome b5 reductase 3 Homo sapiens (human)
mitochondrial membraneNADH-cytochrome b5 reductase 3 Homo sapiens (human)
azurophil granule lumenNADH-cytochrome b5 reductase 3 Homo sapiens (human)
hemoglobin complexNADH-cytochrome b5 reductase 3 Homo sapiens (human)
nitric-oxide synthase complexNADH-cytochrome b5 reductase 3 Homo sapiens (human)
mitochondrionNADH-cytochrome b5 reductase 3 Homo sapiens (human)
extracellular regionMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
nucleusMyeloperoxidaseHomo sapiens (human)
nucleoplasmMyeloperoxidaseHomo sapiens (human)
lysosomeMyeloperoxidaseHomo sapiens (human)
secretory granuleMyeloperoxidaseHomo sapiens (human)
azurophil granule lumenMyeloperoxidaseHomo sapiens (human)
azurophil granuleMyeloperoxidaseHomo sapiens (human)
intracellular membrane-bounded organelleMyeloperoxidaseHomo sapiens (human)
extracellular exosomeMyeloperoxidaseHomo sapiens (human)
phagocytic vesicle lumenMyeloperoxidaseHomo sapiens (human)
extracellular spaceMyeloperoxidaseHomo sapiens (human)
extracellular spaceThyroid peroxidaseHomo sapiens (human)
plasma membraneThyroid peroxidaseHomo sapiens (human)
cell surfaceThyroid peroxidaseHomo sapiens (human)
extracellular spaceThyroid peroxidaseHomo sapiens (human)
plasma membraneTaste receptor type 2 member 38Homo sapiens (human)
membraneTaste receptor type 2 member 38Homo sapiens (human)
membraneTaste receptor type 2 member 38Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (169)

Assay IDTitleYearJournalArticle
AID1256932Lipophilicity, log D of the compound at pH 7.4 by shake-flask method2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1256938Drug metabolism assessed as formation of human MPO-mediated PTU-SO3- at 10 uM after 60 mins by LC-MS/MS analysis in presence of H2O2/Cl-2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1262534Inhibition of L-T4-induced decrease in high-density lipoprotein cholesterol in albino Wistar rat at 10 mg/kg/day, po cotreated with 0.5 mg/kg L-T4 for 15 days (Rvb = 20.18 +/- 2.32 mg/dl)2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.
AID1256936Drug metabolism assessed as formation of human MPO-mediated PTU-disulfide at 10 uM after 60 mins by LC-MS/MS analysis in presence of H2O2/Cl-2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1256926Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin after 300 secs by spectrophotometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID92035Inhibition of Human placenta inner-ring Iodothyronine 5-deiodinase activity measured as rT3 production in presence of DTT concentrations of 0.2 mM1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1262541Inhibition of L-T4-induced decrease in total cholesterol level in albino Wistar rat at 10 mg/kg/day, po cotreated with 0.5 mg/kg L-T4 for 15 days (Rvb = 58.77 +/- 3.95 mg/dl)2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.
AID1256930Inhibition of TPO (unknown origin) using Amplex Red as substrate assessed as formation of resorufin by measuring ratio of Kinact to Ki measured every 20 secs by spectrophotometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678718Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID92038Inhibition of Human placenta inner-ring Iodothyronine 5-deiodinase activity measured as rT3 production in presence of DTT concentrations of 12.5 mM1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID92034Inhibition of Human Placenta Inner-Ring Iodothyronine 5-deiodinase at the compound concentration of 5 mM1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1262536Inhibition of L-T4-induced decrease in very low-density lipoprotein cholesterol in albino Wistar rat at 10 mg/kg/day, po cotreated with 0.5 mg/kg L-T4 for 15 days (Rvb = 8.65 +/- 2.76 mg/dl)2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.
AID92036Inhibition of Human placenta inner-ring Iodothyronine 5-deiodinase activity measured as rT3 production in presence of DTT concentrations of 1.56 mM1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1256931Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as partition ratio preincubated for 15 mins with H2O2 followed by 300 fold dilution measured immediately post dilution by spectropho2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1256937Drug metabolism assessed as formation of human MPO-mediated PTU-SO2- at 10 uM after 60 mins by LC-MS/MS analysis in presence of H2O2/Cl-2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID92037Inhibition of Human placenta inner-ring Iodothyronine 5-deiodinase activity measured as rT3 production in presence of DTT concentrations of 100 mM1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis of 6-anilino-2-thiouracils and their inhibition of human placenta iodothyronine deiodinase.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1256928Irreversible inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin at 24 uM preincubated for 15 mins without H2O2 followed by 300 fold dilution measured immedia2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1256927Irreversible inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin at 24 uM preincubated for 15 mins with H2O2 followed by 300 fold dilution measured immediatel2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1632598Antithyroid activity in L-T4-induced Wistar albino rat model of hyperthyroidism assessed as inhibition of hepatic 5'-monodeiodinase 1 activity by measuring reduction in T3 level using T4 as substrate at 10 mg/kg, po qd post 12 days of L-T4 challenge measu2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Role of a gitogenin-type steroidal saponin (3-O-β-d-glucopyranosyl (1→2)-β-d-glucopyranosyl (1→4)-β-d-galactopyranoside-25R,5α-spirostane-2α,3β-diol), isolated from the leaves of Malvastrum coromandelianum in regulating thyrotoxicosis in rats.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1262537Inhibition of L-T4-induced decrease in low-density lipoprotein cholesterol in albino Wistar rat at 10 mg/kg/day, po cotreated with 0.5 mg/kg L-T4 for 15 days (Rvb = 31.68 +/- 4.25 mg/dl)2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.
AID1256929Inhibition of TPO (unknown origin) using Amplex Red as substrate assessed as formation of resorufin measured every 20 secs by spectrophotometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1632596Antithyroid activity in L-T4-induced Wistar albino rat model of hyperthyroidism assessed as reduction in T3 level at 10 mg/kg, po qd post 12 days of L-T4 challenge measured after 15 days in presence of [125I]-T3 by RIA2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Role of a gitogenin-type steroidal saponin (3-O-β-d-glucopyranosyl (1→2)-β-d-glucopyranosyl (1→4)-β-d-galactopyranoside-25R,5α-spirostane-2α,3β-diol), isolated from the leaves of Malvastrum coromandelianum in regulating thyrotoxicosis in rats.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1256925Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin at 0.47 to 30 uM by spectrophotometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1256934Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin by measuring ratio of Kinact to Ki measured every 20 secs by spectrophotometric analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1632597Antithyroid activity in L-T4-induced Wistar albino rat model of hyperthyroidism assessed as reduction in T4 level at 10 mg/kg, po qd post 12 days of L-T4 challenge measured after 15 days in presence of [125I]-T4 by RIA2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Role of a gitogenin-type steroidal saponin (3-O-β-d-glucopyranosyl (1→2)-β-d-glucopyranosyl (1→4)-β-d-galactopyranoside-25R,5α-spirostane-2α,3β-diol), isolated from the leaves of Malvastrum coromandelianum in regulating thyrotoxicosis in rats.
AID1262539Inhibition of L-T4-induced decrease in triglyceride level in albino Wistar rat at 10 mg/kg/day, po cotreated with 0.5 mg/kg L-T4 for 15 days (Rvb = 42.15 +/- 3.23 mg/dl)2015Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24
Protective effects of 5,7,4'-trihydroxy-6,3'dimethoxy-flavone 5-O-α-l-rhamnopyranoside, isolated from Annona squamosa leaves in thyrotoxicosis and in hepatic lipid peroxidation in rats.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID1256935Irreversible inhibition of MPO in LPS-stimulated human whole blood after 4 hrs by Amplex Red/H2O2-based fluorescence plate reader analysis2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,147)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902124 (51.22)18.7374
1990's674 (16.25)18.2507
2000's684 (16.49)29.6817
2010's550 (13.26)24.3611
2020's115 (2.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 85.95

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 Index85.95 (24.57)
Research Supply Index8.41 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index158.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (85.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials120 (2.75%)5.53%
Reviews229 (5.25%)6.00%
Case Studies621 (14.25%)4.05%
Observational3 (0.07%)0.25%
Other3,386 (77.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (10)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT01056419]Phase 440 participants (Anticipated)Interventional2009-01-31Recruiting
Clinical Evaluation in Healthy Volunteers of Potential syneRgistic Vascular Effects of PrOpylthiouracil, Riociguat, and Perphenazine a Possible STROKE Medication [NCT04776499]Phase 18 participants (Actual)Interventional2021-03-18Completed
The Oral Microbiota in Autoimmune Thyroiditis is Distinctive And Predictive [NCT03447093]120 participants (Anticipated)Observational2017-12-23Recruiting
Networked Drug REpurposing for Mechanism-based neuroPrOtection in Ischaemic STROKE (REPO-STROKE IIa) [NCT05762146]Phase 228 participants (Anticipated)Interventional2022-09-05Recruiting
Prospective Randomized Clinical Trial of Total Thyroidectomy (Tx) Versus Thionamides (Anti-Thyroid Drugs) in Patients With Moderate-to-Severe Graves' Ophthalmopathy - a 1-year Follow-up [NCT03066076]Phase 360 participants (Anticipated)Interventional2017-03-01Recruiting
The Effect of Intestinal Microbiota on Treatment Sensitivity and Prognosis of Methimazole for GD [NCT03433352]90 participants (Anticipated)Observational2017-12-23Recruiting
Effect of Hyperthyroidism and Its Treatment in Graves' Disease to Early Marker of Atherosclerosis: Review on the Pathway of Insulin Resistance, Lipid, Inflammation, and Endothelial Dysfunction to Pulse Wave Velocity and Carotid Intima-Media Thickness [NCT05118542]Phase 336 participants (Actual)Interventional2019-01-01Completed
Serum Betatrophin Levels and Its Influencing Factors in Patients With Hyperthyroidism [NCT02812888]240 participants (Anticipated)Observational [Patient Registry]2016-07-31Recruiting
Impact of Treating Thyroid Hormone Dysfunction During Pregnancy: A Randomized Controlled Trial of Universal Screening Versus Case Finding [NCT00846755]4,657 participants (Actual)Interventional2005-03-31Completed
A Randomised Study of Two Anti-thyroid Drug Treatment Regimens in Young People [NCT01436994]Phase 381 participants (Actual)Interventional2004-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]