Page last updated: 2024-11-04

aminopyrine

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

Description

Aminopyrine: A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

aminophenazone : A pyrazolone that is 1,2-dihydro-3H-pyrazol-3-one substituted by a dimethylamino group at position 4, methyl groups at positions 1 and 5 and a phenyl group at position 2. It exhibits analgesic, anti-inflammatory, and antipyretic properties. [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 CID6009
CHEMBL ID288470
CHEBI ID160246
SCHEMBL ID26293
MeSH IDM0000965

Synonyms (186)

Synonym
smr001216566
MLS002154195 ,
STL356033
BRD-K12568846-001-04-7
dimapyrin
pyramidone
4-dimethylamino-2,3-dimethyl-1-phenyl-5-pyrazolone
dimethylamino-analgesine
febrinina
brufaneuxol
amidazofen
amidopyrine
hyparon
1-phenyl-2,3-dimethyl-4-dimethylaminopyrazolone-5
novamidon
mamallet-a
piridol
itamidone
4-(dimethylamino)antipyrine
antipyrine, 4-(dimethylamino)-
piromidina
dimethylaminoantipyrine
dereuma
4-dimethylaminophenazone
3-keto-1,3-dihydropyrazole
wln: t5nnvj a1 br& dn1&1 e1
4-dimethylamino-1-phenyl-2,3-dimethylpyrazolone
(dimethylamino)phenazone
pyradone
eufibron
aminophenazon
nsc-4993
aminopyrin
3-pyrazolin-5-one,3-dimethyl-1-phenyl-
amidopyrazoline
4-dimethylamino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one
1,5-dimethyl-4-dimethylamino-2-phenyl-3-pyrazolone
dipirin
amidopyrin
dimethylaminoazophene
amidofen
polinalin
amidofebrin
pirazon
pyramidon
amidophen
aminophenazone
amidazophen
1-phenyl-2,3-dimethyl-4-dimethylaminopyrazol-5-one
anafebrina
amidazophene
dimethylaminophenazone
2,3-dimethyl-4-dimethylamino-1-phenyl-5-pyrazolone
febron
1-phenyl-2,3-dimethyl-4-(dimethylamino)-5-pyrazolone
dipyrin
amidophenazone
dimethylaminophenyldimethylpyrazolone
dipyrine
nsc4993
piramidon
3h-pyrazol-3-one, 4-(dimethylamino)-1,2-dihydro-1,5-dimethyl-2-phenyl-
4-(dimethylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one
TIMTEC1_000737
PRESTWICK_14
NCGC00016257-01
cas-58-15-1
PRESTWICK3_000088
BPBIO1_000018
PRESTWICK2_000088
BSPBIO_000016
OPREA1_080671
NCGC00090878-01
netsusarin
aminofenazona [inn-spanish]
aminopyrinum
nsc 4993
amidazophenum
einecs 200-365-8
dimethylaminophenazon [german]
dimethylaminophenyldimethylpyrazolin
ccris 2907
3-pyrazolin-5-one, 4-(dimethylamino)-2,3-dimethyl-1-phenyl-
aminopyrine [jan]
aminophenazon [german]
aminofenazone [italian]
aminophenazonum [inn-latin]
hsdb 2135
amidopyrinum
58-15-1
aminopyrine
4-dimethylaminoantipyrine
C07539
4-dimethylaminoantipyrine, reactive nitrogen species scavenger
4-(dimethylamino)-1,2-dihydro-1,5-dimethyl-2-phenyl-3h-pyrazol-3-one
DB01424
3-keto-1,5-dimethyl-4-dimethylamino-2-phenyl-2,3-dihydropyrazole
aminofenazone
aminophenazone (inn)
aminopyrine (jan)
D00556
NCGC00090878-02
NCGC00090878-03
PRESTWICK0_000088
PRESTWICK1_000088
SPBIO_001955
NCGC00175173-02
NCGC00175173-01
HMS1536B11
HMS2092E10
AC-12025
mamallet a
CHEMBL288470
AKOS001590378
aminophenazonum
dimethylaminophenazon
chebi:160246 ,
aminofenazona
HMS1568A18
4-(dimethylamino)-1,5-dimethyl-2-phenylpyrazol-3-one
NCGC00016257-04
HMS2095A18
HMS3039C06
tox21_302830
dtxcid70504
dtxsid7020504 ,
NCGC00256436-01
NCGC00259094-01
tox21_201544
nsc757388
nsc-757388
pharmakon1600-01500621
tox21_110333
S3209
CCG-103785
NCGC00016257-03
NCGC00016257-05
NCGC00016257-02
NCGC00016257-07
NCGC00016257-06
4-(dimethylamino)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one
aminopyrine [jan:nf]
unii-01704yp3mo
aminophenazone [inn]
01704yp3mo ,
metamizole sodium monohydrate impurity d [ep impurity]
aminopyrine [hsdb]
aminophenazone [who-dd]
4-dimethylamino-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one
aminophenazone [mart.]
aminopyrine [mi]
3h-pyrazol-3-one,4-(dimethylamino)-1,2-dihydro-1,5-dimethyl-2-phenyl-
HY-B0533
SCHEMBL26293
tox21_110333_1
NCGC00016257-10
4-(dimethylamino)-1,5-dimethyl-2-phenyl-pyrazol-3-one
dimethylaminophenyldimethylpyrazone
4-n,n-dimethylaminoantipyrine
piramidone
4-(dimethylamino)phenazone
4-(dimethylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one #
,3-dimethyl-4-dimethylamino-1-phenyl-3-pyrazolin-5-one
1,5-dimethyl-2-phenyl-4-dimethylamino-3-pyrazolone
bdbm74258
4-(dimethylamino)-1,5-dimethyl-2-phenyl-3-pyrazolin-3-one
cid_6009
4-(dimethylamino)-1,5-dimethyl-2-phenyl-3-pyrazolone
mfcd00003142
4-(dimethylamino)-1,5-dimethyl-2-phenyl-2,3-dihydro-1h-pyrazol-3-one
4-dimethylamino-2,3-dimethyl-1-phenylpyrazol-5-one
SR-05000001741-4
sr-05000001741
HMS3652G13
SR-05000001741-3
SR-05000001741-1
aminophenazone (4-dimethylamino-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one)
4-dimethylamino-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one (4,4-dimethylaminophenazone)
SBI-0207073.P001
HMS3712A18
SW196332-3
Q416503
4-(dimethylamino)-1,5-dimethyl-2-phenyl-1h-pyrazol-3(2h)-one
tocainidehydrochloride(125mg)
EN300-18532179
4-dimethylaminoantipyrine-d6

Research Excerpts

Overview

Aminopyrine is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties. It is weakly ulcerogenic, while indomethacin and aspirin are known to cause considerable ulcerogenesis.

ExcerptReferenceRelevance
"Aminopyrine breath test is a sensitive, non-invasive test and specific in liver function and therefore useful in the follow up of patients with known liver disease."( [The diagnostic relevance of the aminopyrine breath test in liver disease].
Stang, H; Wildgrube, HJ, 1982
)
1.27
"Aminopyrine is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties, but is weakly ulcerogenic, while indomethacin and aspirin are known to cause considerable ulcerogenesis."( Different modes of inhibition of rat gastric mucosal 6-keto-PGF1 alpha production by indomethacin, aspirin and aminopyrine.
Nishikawa, T; Shimizu, S; Tomori, Y; Yamashita, S, 1989
)
1.21
"The aminopyrine breath test is a valuable quantitative liver function test. "( Altered liver function in diabetes: model experiments with aminopyrine in the rat.
Tlach, C; Zysset, T, 1987
)
1.07

Effects

Aminopyrine has been reported to inhibit gluconeogenesis from fructose by 30% and from lactate by 85%. The aminopyrina breath test has been proposed as a quantitative test of hepatic function, but its long-term prognostic value has not been determined.

ExcerptReferenceRelevance
"Aminopyrine (AMP) has been frequently detected in the aquatic environment. "( Transformation of aminopyrine in the presence of free available chlorine: Kinetics, products, and reaction pathways.
Cai, MQ; Feng, L; Zhang, LQ, 2017
)
2.23
"The aminopyrine breath test has been performed on Day 1 and Day 7 in pigs following experimental liver allografting. "( The aminopyrine breath test predicts the outcome of hepatic transplantation in pigs.
Hickman, R; Oakland, CD; Terblanche, J, 1989
)
1.39
"4. Aminopyrine has been reported to inhibit gluconeogenesis from fructose by 30% and from lactate by 85%."( Interrelationship between drug oxidation ureogenesis and gluconeogenesis in isolated hepatocytes.
Antoni, F; Bánhegyi, G; Garzó, T; Mandl, J, 1988
)
0.79
"The aminopyrine breath test has been shown to be a sensitive noninvasive indicator of liver cell dysfunction. "( The aminopyrine breath test, an inadequate early indicator of methotrexate-induced liver disease in patients with psoriasis.
Malatjalian, DA; McCauley, D; Ross, JB; Turnbull, GK; Williams, CN, 1987
)
1.39
"The aminopyrine breath test has been proposed as a quantitative test of hepatic function, but its long-term prognostic value in patients with cirrhosis has not been determined. "( Prognostic value of the aminopyrine breath test in cirrhotic patients.
Ampelas, M; Huet, PM; Infante-Rivard, C; Marleau, D; Pomier-Layrargues, G; Villeneuve, JP,
)
1
"The aminopyrine breath test has been used in adults as a measure of hepatic N-demethylase activity. "( Effect of infant age on aminopyrine breath test results.
Boutton, TW; Irving, CS; Klein, PD; Nichols, BL; Shulman, RJ; Wong, WW, 1985
)
1.13

Actions

ExcerptReferenceRelevance
"Aminopyrine could inhibit MDA production by CsA, but CsA could not reduce the formation of formaldehyde by aminopyrine."( Generation of oxygen free radicals during the metabolism of cyclosporine A: a cause-effect relationship with metabolism inhibition.
Grevel, J; Kahan, BD; Napoli, KL; Serino, F; Strobel, HW, 1993
)
1.01

Toxicity

ExcerptReferenceRelevance
"The influence of LD50 of lidocain by preliminary treatment with pethidin, aminophenazone or diazepam, respectively, is examined at the mouse."( [Over-additive increase of the toxicity of lidocaine by pethidine].
Lampe, D; Lange, B; Mai, I, 1976
)
0.26
" It is concluded that UDCA appears to be safe only in stages I to III and that prognostic stratification based on bile acid levels or on the histological stage of the disease should be an important aspect of controlled clinical trials."( Ursodeoxycholic acid in primary biliary cirrhosis: no evidence for toxicity in the stages I to III.
Bircher, J; Foelsch, UR; Lotterer, E; Raedsch, R; Stiehl, A, 1990
)
0.28
"The role of S-oxidation in the toxic bioactivation of alpha-naphthylisothiocyanate (ANIT) was investigated."( Effect of inhibitors of alpha-naphthylisothiocyanate-induced hepatotoxicity on the in vitro metabolism of alpha-naphthylisothiocyanate.
Hanzlik, RP; Traiger, GJ; Vyas, KP, 1985
)
0.27
" Preadministration of thiamin and especially of thiamin diphosphate decreased the toxic effect of cyclophosphamide."( [Metabolism and toxicity of various xenobiotics in vitamin B1 deficiency and after administration of thiamine and thiamine diphosphate].
Lutsiuk, NB; Lychko, AP; Pentiuk, AA,
)
0.13
" Finally, the application of an acute toxicity test (Daphnia magna) showed an increase in toxicity during the photolytic process, a consequence of the formation of toxic photoproducts."( Photodegradation study of three dipyrone metabolites in various water systems: identification and toxicity of their photodegradation products.
Agüera, A; Fernández-Alba, AR; Gómez, MJ; Mezcua, M; Sirtori, C, 2008
)
0.35

Pharmacokinetics

ExcerptReferenceRelevance
" The mean Cmax of 4-MAA increased linearly with dose whereas its AUC was not proportional to dose after administration of 1500 and 3000 mg."( Pharmacokinetics of metamizol metabolites in healthy subjects after a single oral dose of metamizol sodium.
Bacracheva, N; Badian, M; Verho, M; Vlahov, V, 1990
)
0.28
" The pharmacokinetic characteristics of the drug that affect the usefulness of the carbon dioxide excretion as a measure of liver function were examined by means of computer simulations."( Drug pharmacokinetics and the carbon dioxide breath test.
Lane, EA; Parashos, I, 1986
)
0.27
" Plasma levels of the active dipyrone metabolite-Methylaminoantipyrine (MAA) were measured and the calculated pharmacokinetic parameters were compared."( Influence of food on the pharmacokinetics of dipyrone.
Flusser, D; Granit, L; Levy, M; Zylber-Katz, E, 1988
)
0.27
" Plasma pharmacokinetic data were first obtained from rabbits given 3 mg/kg doxorubicin."( The influence of ranitidine on the pharmacokinetics and toxicity of doxorubicin in rabbits.
Anthony, LB; Brenner, DE; Collins, JC; Halter, S; Hande, KR; Harris, NL, 1988
)
0.27
" VPA was excreted in the neonates with a mean half-life of 47 +/- 15 hr (n = 8) which is approximately 4 times the mean value found in adult epileptics."( Valproic acid and its metabolites: placental transfer, neonatal pharmacokinetics, transfer via mother's milk and clinical status in neonates of epileptic mothers.
Häuser, I; Helge, H; Koch, S; Nau, H; Rating, D, 1981
)
0.26
" The feasibility of the brain microdialysis method for direct measurement and pharmacokinetic study of imipramine (Imip) and its metabolite desipramine (DMI) was investigated in the rat brain."( Measurement and pharmacokinetic analysis of imipramine and its metabolite by brain microdialysis.
Ishikawa, K; Sato, Y; Shibanoki, S; Sugahara, M, 1994
)
0.29
" The elimination half-life of the final metabolites FAA and AAA can be equally evaluated from plasma and saliva data."( Validity of saliva samples for the estimation of dipyrone metabolites pharmacokinetics.
Caraco, Y; Granit, L; Levy, M; Zylber-Katz, E, 1993
)
0.29
" Additional pharmacokinetic investigations are recommended to optimise pharmacological outcomes in patients with severe head injury."( Pharmacokinetic alterations after severe head injury. Clinical relevance.
Boucher, BA; Hanes, SD, 1998
)
0.3

Compound-Compound Interactions

ExcerptReferenceRelevance
"Antitumor activity and lethality of cyclophosphamide alone and in combination with several drugs were investigated in male ddY mice."( [Drug interaction on antitumor drugs I. Antitumor activity of cyclophosphamide in mice consecutively administered aminopyrine, chlorpromazine, or morphine (author's transl)].
Saitoh, M; Sasaki, K; Takayanagi, G, 1979
)
0.47
"In the present study we investigated the antiinflammatory effect of pentosanpolysulfate (SP 54) in combination with metamizol using different forms of rat paw edema (induced by dextrane, hyaluronidase, trypsin, formaldehyde, carragenine or kaolin)."( [Pharmacological studies on the antiphlogistic effect of pentosanpolysulfate in combination with metamizol].
Kalbhen, DA; Smalla, HD, 1977
)
0.26
" Within each study, there is no significant difference between the elimination rate constants, areas under the plasma concentration/time curve and percentage excreted in urine for the three components administered alone or in any combination with the other components of Optalidon."( Drug interactions of the components of Optalidon after oral administration.
Guillaume, MF; Kiger, JL; Lavene, D; Longchampt, J, 1976
)
0.26
" Omeprazole contains a benzimidazole moiety and thus has the potential to interact with the cytochrome P-450 enzyme group."( Clinical implications of drug interactions with the cytochrome P-450 enzyme system associated with omeprazole.
Humphries, TJ, 1991
)
0.28

Bioavailability

ExcerptReferenceRelevance
" Based on a pharmacokinetic model, the following conclusions can be drawn: a) There is no change in bioavailability due to the combination of the three components in Optalidon in respect to their single administration."( Drug interactions of the components of Optalidon after oral administration.
Guillaume, MF; Kiger, JL; Lavene, D; Longchampt, J, 1976
)
0.26
" Maximal concentration, time to peak and absorption rate of MAA were similar for both groups."( Effect of age on the pharmacokinetics of dipyrone.
Granit, L; Levy, M; Stessman, J; Zylber-Katz, E, 1989
)
0.28
" The parent drug extraction ratio, fraction demethylated, volume of distribution, and absorption rate of an oral dosage form all contribute to the carbon dioxide breath test result."( Drug pharmacokinetics and the carbon dioxide breath test.
Lane, EA; Parashos, I, 1986
)
0.27
" Bioavailability of ASA at intramuscular administration to rabbits was close to that at intravenous injection and significantly higher as compared with intragastric administration."( [Analgesic action and pharmacokinetics of lysine acetylsalicylate administered intramuscularly].
Chaĭka, LA; Khadzhaĭ, IaI; Kosheleva, LP; Libina, VV; Pichugin, VV,
)
0.13
" A reduction of the mucosal unstirred layer thickness by means of the segmented-flow technique considerably increased the absorption rate without essentially changing the shape of the pH-absorption curves."( Drug absorption by the rat jejunum perfused in situ. Dissociation from the pH-partition theory and role of microclimate-pH and unstirred layer.
Högerle, ML; Winne, D, 1983
)
0.27
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described."( Importance of physicochemical properties for the design of new pesticides.
Akamatsu, M, 2011
)
0.37
"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

nitrazepam with other drugs exhibited an anticonvulsive pattern different from the case of dosing with either drug alone. Fragmentation of the intact DNA was observed significantly shortly after combined treatment with aminopyrine and nitrite when no liver necrosis occurred yet. The damaged DNA was found to be repaired in contrast to the increased activity of serum aminotransferase.

ExcerptRelevanceReference
" The histamine respiratory dose-response curve was shifted to the left in the presence of the phosphodiesterase inhibitor aminophylline."( Potentiation by carbachol and aminophylline of histamine- and db-cAMP-induced parietal cell activity in isolated gastric glands.
Berglindh, T, 1977
)
0.26
"Neuro-Demoplas was compared in a double blind trial on behalf of its analgesic properties to another antiphologistic containing high dosage of vitamin B complex and Metamizol."( [Analgesic effect of Neuro-Demoplas in a double-blind test].
Gabka, J, 1976
)
0.26
"A simple, rapid, specific and sensitive colorimetric method is proposed for the quantitative estimation of noramido-pyrine methanesulfonate sodium in different dosage forms as well as in blood and urine samples."( Colorimetric assay of noramidopyrine methanesulfonate sodium in formulations and in blood and urine samples.
Diab, AH, 1977
)
0.26
" Fragmentation of the intact DNA was observed significantly shortly after combined treatment with aminopyrine and nitrite when no liver necrosis occurred yet and the damaged DNA at the lower dosage level of aminopyrine with nitrite was found to be repaired in contrast to the increased activity of serum aminotransferase."( Damage and repair of rat liver DNA by simultaneous oral administration of amines and nitrite.
Hosokawa, S; Miyamoto, J, 1976
)
0.47
" The dosage causing a 50% inhibition culture growth (ID50) and minimum concentration, caused by the detachment of the cell from the vessel wall, were determined."( [Effects of drugs on cell culture (II)].
Kameyama, T; Mukaide, A, 1975
)
0.25
" Evaluation of dose-response curves revealed saturation phenomena."( Expiratory measurement of maximal amino-pyrine demethylation in vivo: effect of phenobarbital, partial hepatectomy, protacaval shunt and bile duct ligation in the rat.
Bircher, J; Lauterburg, BH, 1976
)
0.26
" There was a marked upward shift in the dose-response curve of histamine (HA; 10(-8) to 10(-3) M) in milk-fed rats, indicating enhanced sensitivity of parietal cell-H2 receptor to exogenous HA."( Milk-stimulated PGE2 production by isolated gastric cells: a possible role in the inhibition of histamine-induced acid secretion.
Brunel-Riveau, B; Ducroc, R; Garzon, B; Geloso, JP; Vilar, J; Wirbel, A, 1992
)
0.28
" The trial was open, randomized, and cross-over, with a one-week interval between dosing days."( Pharmacokinetics of metamizol metabolites in healthy subjects after a single oral dose of metamizol sodium.
Bacracheva, N; Badian, M; Verho, M; Vlahov, V, 1990
)
0.28
" Assuming that the binding of carbachol to one site (Site 1) increases [14C]aminopyrine accumulation but its binding to the other site (Site 2) reduces [14C]aminopyrine accumulation, we analysed the dose-response curves for the carbachol effects in the absence and presence of different concentrations of atropine, pirenzepine and AF-DX 116."( Carbachol-induced potentiation and inhibition of acid secretion by guinea pig gastric gland.
Haga, T; Honda, N; Ichiyama, A; Kajimura, M; Kaneko, E, 1990
)
0.51
" The dose-response curve for carbachol was biphasic."( Stimulation of acid formation by histamine, carbachol and pentagastrin in isolated pig parietal cells.
Ljungström, M; Mårdh, S; Norberg, L; Vega, FV, 1986
)
0.27
" Imipramine and nortriptyline also caused a rightward shift in the dose-response curve of histamine-induced cAMP generation."( Tricyclic antidepressants and acid secretory response of rabbit gastric cells.
Batzri, S, 1985
)
0.27
" The dose-response relations for the increase in inositol phosphates closely paralleled the binding of carbachol to muscarinic receptors with a Km of 17 microM."( Stimulation of acid secretion and phosphoinositol production by rat parietal cell muscarinic M2 receptors.
Herz, A; Paumgartner, G; Pfeiffer, A; Rochlitz, H, 1988
)
0.27
" Additional prior dosing with Opisthorchis viverrini metacercariae (100/animal) induced inflammatory and proliferative changes in the livers of infected hamsters and was associated with a significant increase in yields of hepatocellular and cholangiocellular preneoplastic and neoplastic lesions."( Generation of high yields of Syrian hamster cholangiocellular carcinomas and hepatocellular nodules by combined nitrite and aminopyrine administration and Opisthorchis viverrini infection.
Hiasa, Y; Ito, N; Moore, MA; Thamavit, W, 1988
)
0.48
" Elimination of these model drugs was studied before and during 8 days of famotidine dosing in 8 healthy volunteers."( Effect of famotidine on oxidative drug metabolism.
Kitchingman, GA; Langman, MJ; Somerville, KW, 1986
)
0.27
" The parent drug extraction ratio, fraction demethylated, volume of distribution, and absorption rate of an oral dosage form all contribute to the carbon dioxide breath test result."( Drug pharmacokinetics and the carbon dioxide breath test.
Lane, EA; Parashos, I, 1986
)
0.27
" On the other hand despite a relatively highly dosed one-week treatment propyphenazone did not lead to changes of the demethylation capacity of the liver in the majority of the patients."( [Effect of propyphenazone on drug biotransformation in the liver. A comparison with phenylbutazone using the aminopyrine breath test].
Clemens, M; Reinicke, C; Steiner, A; Stiller, KJ; Tanner, E; Wächter, G, 1988
)
0.49
" EGF (10(-7) M) significantly inhibited the histamine dose-response curve for [14C]AP and IF, but a relatively greater inhibition was observed at higher histamine concentration."( Epidermal growth factor (EGF) inhibits both intrinsic factor secretion and acid secretion in histamine-stimulated isolated gastric glands.
Modlin, IM; Rackoff, PJ; Tyshkov, M; Zdon, MJ, 1988
)
0.27
" Secretory mechanisms of this species were identified by establishment of a histamine dose-response curve and use of 8-bromo-cAMP."( Characteristics of the spontaneous gastric endocrine tumor of mastomys.
Adrian, TE; Modlin, IM; Sussman, J; Zdon, MJ; Zucker, KA, 1988
)
0.27
"5 g, the dose-response relationship of the analgesic effect has not been investigated in humans."( [Dose-dependence of the analgesic action of metamizol].
Neddermann, E; Rohdewald, P, 1988
)
0.27
"The histamine H2-receptor on the human parietal cell has been characterized by using dose-response curves and the negative logarithm of the molar concentration of an antagonist (pA2) analyses of cimetidine antagonism of betazole, histamine, and impromidine stimulation in isolated human and rabbit gastric glands."( Histamine H2-receptor of human and rabbit parietal cells.
Elander, B; Fellenius, E; Haglund, U; Leth, R; Olbe, L, 1987
)
0.27
" Alterations in L/P ratio preceded the release of cytosolic ALT and at 4 h a well defined dose-response relationship existed between the benoxaprofen concentration and the observed increases in the L/P ratio and ALT release."( Benoxaprofen induced toxicity in isolated rat hepatocytes.
Cassidy, MR; Drew, R; Knights, KM, 1986
)
0.27
" Time course experiments and dose-response experiments indicated that an increase in the microsomal oxidation of alcohols could be observed 24 hr after a single treatment with 200 mg/kg body weight of either pyrazole or 4-methylpyrazole, and after 2 or 3 days of treatment with 50 mg/kg of either of these compounds."( Interaction of pyrazole and 4-methylpyrazole with hepatic microsomes: effect on cytochrome P-450 content, microsomal oxidation of alcohols, and binding spectra.
Cederbaum, AI; Feierman, DE,
)
0.13
" The blocking factor was present in serum IgG fractions, and serum and IgG fractions gave parallel dose-response and dilution curves."( Serum from patients with pernicious anaemia blocks gastrin stimulation of acid secretion by parietal cells.
de Aizpurua, HJ; Toh, BH; Ungar, B, 1985
)
0.27
" Furthermore, chronic dosing with cimetidine does not result in tolerance to the inhibitory effect."( Inhibition of microsomal drug metabolism by histamine H2-receptor antagonists studied in vivo and in vitro in rodents.
Avant, GR; Mitchell, MC; Patwardhan, RV; Schenker, S; Speeg, KV, 1982
)
0.26
" Administration of nitrazepam with other drugs, except aminopyrine, or of estazolam together with haloperidol exhibited an anticonvulsive pattern different from the case of dosing with either drug alone."( [Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III). Behavioral study on interactions of 450191-S and other drugs in mice].
Horiuchi, M; Ibii, N; Yamamoto, K, 1984
)
0.51
" Complete dose-response curves of H+ secretion as a function of K+ concentration could now be obtained."( Cation effects on acid secretion in rabbit gastric glands.
Berglindh, T; Koelz, HR; Sachs, G, 1981
)
0.26
" In the case of secretagogue stimulation (1) benzotript slightly affected histamine-induced AP (15% inhibition at 5 X 10(-3) M), proglumide did not; (2) both proglumide and benzotript inhibited in a non-competitive manner acetylcholine-induced AP; (3) these isolated cells were sensitive to gastrin and the dose-response curve for the stimulant was biphasic (maximum for 1 X 10(-9) M), suggesting a desensitization mechanism."( Evidence that proglumide and benzotript antagonize secretagogue stimulation of isolated gastric parietal cells.
Bali, JP; Magous, R, 1983
)
0.27
" The procedure presented here provides possibilities for the assay of these compounds in various dosage forms."( [Gas chromatography determination of atropine, theophylline, phenobarbital and aminophenazone in tablets].
Majlát, P, 1984
)
0.27
" Moreover, based on these results an hypothesis is put forward in order to explain the phenomenon of product inhibition, which has been suggested to occur in man under chronic orphenadrine dosing conditions."( Effect of multiple administration of orphenadrine or mono-N-desmethylorphenadrine on cytochrome P-450 catalyzed reactions in the rat.
Bast, A; Noordhoek, J; Savenije-Chapel, EM; Scheefhals, LW; van Kemenade, FA, 1983
)
0.27
" Areas under the curves from 1 to 6 h after dosing indicated distinct interindividual differences in metabolite patterns even in the absence of disturbed liver function, whereas the intraindividual data were closely reproducible."( Plasma levels of parent drug and metabolites in the intravenous aminopyrine breath test.
Breyer-Pfaff, U; Egberts, EH; Harder, M, 1982
)
0.5
" Dose-response relationships provided security for the comparison of the activities of these two pharmaca."( [Antipyretic activity of 3-amino-4-mercapto-6-methylpyridazine and some standard pharmaca].
Bluth, R, 1982
)
0.26
" Cimetidine caused parallel displacement of the dose-response curve to histamine, but failed to alter the response to carbachol or gastrin."( Secretagogue stimulation of [14C]aminopyrine accumulation by isolated canine parietal cells.
Soll, AH, 1980
)
0.54
" Individual histamine dose-response curves were shifted to the right by increasing ranitidine and cimetidine concentrations (0."( Secretagogue-induced [14C]aminopyrine uptake in isolated equine parietal cells.
Campbell-Thompson, M, 1994
)
0.59
" However, the dose-response curve for pentagastrin in the presence of ranitidine plus IBMX was similar to that obtained in the absence of IBMX."( Gastrin action on aminopyrine accumulation in isolated pig parietal cells requires cAMP.
Cabero, JL; Li, ZQ; Mårdh, S, 1993
)
0.62
" These results should be taken into consideration to determine the optimal CCl4 dosing schedule in the rat CCl4-induced cirrhosis model."( Mechanism of carbon tetrachloride autoprotection: an in vivo study based on 13C-aminopyrine and 13C-galactose breath tests.
Brazier, JL; Géloën, A; Minaire, Y; Mion, F; Rousseau, M, 1994
)
0.52
"14 microM Ro 31-8220) and shifted the dose-response curve for the effect of carbachol concentration of aminopyrine accumulation downwards and to the right."( Inhibition by Ro 31-8220 of acid secretory activity induced by carbachol indicates a stimulatory role for protein kinase C in the action of muscarinic agonists on isolated rat parietal cells.
Hanson, PJ; McKenna, JP, 1993
)
0.5
" Comparison of the dose-response curves between TPA-induced hydrogen (H+) secretion, as measured by aminopyrine (AP) uptake, and the membrane-associated PKC-alpha suggests that translocation of PKC-alpha is not involved in the H+ secretory process in PC."( Expression and characterization of protein kinase C in isolated rabbit parietal cells.
Kim, SW; Levine, RA; Loo, A; Nandi, J, 1999
)
0.52
"1 mmol; a phosphodiasterase inhibitor) were added to the Eppendorf tubes containing the PPIs and AP and dose-response curves were done for each drug after incubating for 5, 10 and 20 min at 37 degrees C and AP accumulation was determined using a scintillation counter."( Comparison of five antisecretory agents acting via gastric H+/K+-ATPase.
Bastaki, SM; Chandranath, I; Garner, A,
)
0.13
"Oral dosing with DMP 777 caused a rapid increase in serum gastrin levels and severe hypochlorhydria."( Reversible drug-induced oxyntic atrophy in rats.
Barnes, TB; Car, BD; Coffey, RJ; Goldenring, JR; Haley, PJ; Meunier, PC; Ray, GS, 2000
)
0.31
"1 mM)-stimulated AP accumulation, which was dose-dependently inhibited by higher concentrations of TPA with corresponding shifts in the dose-response curve for carbachol-stimulated AP accumulation."( Effects of phorbol ester treatment on dibutyryl cyclic adenosine-5' monophosphate- and carbachol-stimulated aminopyrine accumulation in isolated rat parietal cells.
Kopp, R; Pfeiffer, A, 2000
)
0.52
" Treatment was successful with prednisone, started at a dosage of 1 mg/kg/d, for 5 months."( A case of linear immunoglobulin A bullous dermatosis in a patient exposed to sun and an analgesic.
Caldarola, G; Cozzani, E; Parodi, A; Pellicano, R, 2009
)
0.35
" Therefore, an appropriate dosage adjustments should be considered when high-hepatic-metabolism drugs are administered to HHT patients."( Liver involvement in hereditary hemorrhagic telangiectasia: can breath test unmask impaired hepatic first-pass effect?
Bosco, G; Candelli, M; Gasbarrini, A; Lenato, GM; Pompili, M; Rapaccini, GL; Sabbà, C; Scardapane, A; Suppressa, P, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
xenobioticA xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
[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 (2)

ClassDescription
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
pyrazoloneA member of the class of pyrazoles in which one of the carbons of the pyrazole ring is substituted by an oxo group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (39)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency0.31625.623417.292931.6228AID485281
LuciferasePhotinus pyralis (common eastern firefly)Potency72.19760.007215.758889.3584AID1224835
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
thioredoxin reductaseRattus norvegicus (Norway rat)Potency100.00000.100020.879379.4328AID588453
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
RAR-related orphan receptor gammaMus musculus (house mouse)Potency41.66030.006038.004119,952.5996AID1159521; AID1159523
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624170
GLI family zinc finger 3Homo sapiens (human)Potency39.23860.000714.592883.7951AID1259392
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926; AID938
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency55.42590.000657.913322,387.1992AID1259377
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency37.54590.001022.650876.6163AID1224838; AID1224839
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.37680.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency25.33090.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency32.26230.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency62.18890.001530.607315,848.9004AID1224841; AID1224842
pregnane X nuclear receptorHomo sapiens (human)Potency55.42590.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency46.59220.000229.305416,493.5996AID1259244; AID1259248; AID743075
GVesicular stomatitis virusPotency38.90180.01238.964839.8107AID1645842
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency4.73040.001024.504861.6448AID743215
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency8.70860.023723.228263.5986AID743223
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency69.77710.001723.839378.1014AID743083
activating transcription factor 6Homo sapiens (human)Potency0.87090.143427.612159.8106AID1159516
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency55.883419.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency47.09790.057821.109761.2679AID1159526; AID1159528
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency63.09570.010039.53711,122.0200AID1479
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency47.42830.000323.4451159.6830AID743065; AID743067
histone deacetylase 9 isoform 3Homo sapiens (human)Potency62.18890.037617.082361.1927AID1259364
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency47.30790.000627.21521,122.0200AID651741
gemininHomo sapiens (human)Potency0.32640.004611.374133.4983AID624297
lamin isoform A-delta10Homo sapiens (human)Potency0.06310.891312.067628.1838AID1487
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency69.77710.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency38.90180.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency38.90180.01238.964839.8107AID1645842
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency69.77710.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency38.90180.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency38.90180.01238.964839.8107AID1645842
[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)
Nicotinate phosphoribosyltransferaseHomo sapiens (human)Ki0.00100.00000.00060.0019AID1618606
[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)
ORF73Human gammaherpesvirus 8EC50 (µMol)75.00000.06008.134632.1400AID435023
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
response to oxidative stressNicotinate phosphoribosyltransferaseHomo sapiens (human)
NAD salvageNicotinate phosphoribosyltransferaseHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nicotinate phosphoribosyltransferase activityNicotinate phosphoribosyltransferaseHomo sapiens (human)
protein bindingNicotinate phosphoribosyltransferaseHomo sapiens (human)
transferase activityNicotinate phosphoribosyltransferaseHomo sapiens (human)
metal ion bindingNicotinate phosphoribosyltransferaseHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
extracellular regionNicotinate phosphoribosyltransferaseHomo sapiens (human)
cytosolNicotinate phosphoribosyltransferaseHomo sapiens (human)
azurophil granule lumenNicotinate phosphoribosyltransferaseHomo sapiens (human)
extracellular exosomeNicotinate phosphoribosyltransferaseHomo sapiens (human)
cytosolNicotinate phosphoribosyltransferaseHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (147)

Assay IDTitleYearJournalArticle
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID194642Neuronal protective effect of compound against ischemic brain damage in rat t-MCAO model2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.
AID486711Antioxidant activity assessed as hydroxyl radical scavenging activity at 10 mM at pH 7 by fenton reaction2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Scavenging activity of aminoantipyrines against hydroxyl radical.
AID1134606Et2O-water partition coefficient, log P of the compound1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Hydrogen-bonding parameter and its significance in quantitative structure--activity studies.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1145612Dissociation constant, pKa of the compound at pH 5.31977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1124469Antiinflammatory activity in po dosed CD1 mouse assessed as inhibition of carrageenan-induced paw edema administered 1 hr prior to carrageenan challenge measured after 3 hrs1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.
AID1123027Acute lethal toxicity in po dosed mouse measured after 1 week1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID1145613Drug absorption in rat small intestine1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID1145608Drug absorption in anesthetized rat colon at pH 6.81977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
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.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1223492Oral bioavailability in human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1123390Analgesic activity in sc dosed ddY mouse assessed as inhibition of acetic acid-induced abdominal stretching pretreated for 30 mins followed by acetic acid challenge measured for 5 to 20 mins1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds.
AID1123028Analgesic activity in sc dosed ddN mouse assessed as inhibition of light radiation-induced thermal pain by D'Amour-Smith method1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1123026Acute lethal toxicity in po dosed rat measured after 1 week1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1217729Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1124468Analgesic activity in po dosed CD1 mouse assessed as inhibition of acetic acid-induced writhing administered 30 mins prior to acetic acid challenge measured after 15 mins1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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.
AID1123021Toxicity in sc dosed ddN mouse light radiation-induced thermal pain model1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
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.
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.
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.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1123024Analgesic activity in po dosed ddN mouse assessed as inhibition of light radiation-induced thermal pain by D'Amour-Smith method1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1123020Analgesic activity in po dosed ddN mouse assessed as inhibition of phenylquinone-induced writhing1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
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.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1217709Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1123022Acute lethal toxicity in sc dosed rat measured after 1 week1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
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.
AID1124467Acute toxicity in po dosed CD1 mouse after 7 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1124470Analgesic activity in po dosed OF1 mouse assessed as dose required to double paw licking reaction time after 30 mins by hot plate test1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Synthesis and analgesic activities of some (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates.
AID1123029Toxicity in po dosed Wistar rat tail pressing-induced mechanical pain model1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1123391Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 100 mg/kg, po pretreated for 30 mins followed by carrageenan challenge measured after 3 hrs relative to control1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds.
AID1123393Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 25 mg/kg, po pretreated for 30 mins followed by carrageenan challenge measured after 3 hrs relative to control1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds.
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1145606Octanol-aqueous phase partition coefficient, log P of the compound1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID1145607Octanol-aqueous phase distribution coefficient, log D of the compound1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID1123394Acute toxicity in ip dosed ddY mouse measured after 72 hrs1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
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.
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1134605Oil-water partition coefficient, log P of the compound1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Hydrogen-bonding parameter and its significance in quantitative structure--activity studies.
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]
AID21086Lipid solubility measured as chloroform-water partition coefficient1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
1H-2-Benzopyran-1-one derivatives, microbial products with pharmacological activity. Conversion into orally active derivatives with antiinflammatory and antiulcer activities.
AID288194Intrinsic artificial membrane permeability coefficient, log P0 of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' 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]
AID1123392Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 50 mg/kg, po pretreated for 30 mins followed by carrageenan challenge measured after 3 hrs relative to control1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
A new nonsteroidal analgesic-antiinflammatory agent. Synthesis and activity of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone and related compounds.
AID28956Partition coefficient (logP) (dodecane)2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Rational determination of transfer free energies of small drugs across the water-oil interface.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1123023Analgesic activity in po dosed Wistar rat assessed as inhibition of tail pressing-induced mechanical pain by Haffner method1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID288190Permeability coefficient through artificial membrane in presence of stirred water layer at 100 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID28957Partition coefficient (logP)2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Rational determination of transfer free energies of small drugs across the water-oil interface.
AID182196Compound was tested for antiinflammatory activity and the % inhibition was reported 3 hr after carrageenan injection in the hind paw edema test in rats: dose=80 mg/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Studies on heterocyclic compounds. 6. Synthesis and analgesic and antiinflammatory activities of 3,4-dimethylpyrano[2,3-c]pyrazol-6-one derivatives.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID116720Acute lethal toxicity after oral administration was determined1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Studies on heterocyclic compounds. 6. Synthesis and analgesic and antiinflammatory activities of 3,4-dimethylpyrano[2,3-c]pyrazol-6-one derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
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]
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.
AID1145610Dissociation constant, pKa of the compound at pH 6.81977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Use of distribution coefficients in quantitative structure-activity relationships.
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID288187Permeability coefficient through artificial membrane in presence of stirred water layer at 250 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID681794TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Amimopyrine: 1000 uM) in Xenopus laevis oocytes1999Molecular pharmacology, May, Volume: 55, Issue:5
Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes.
AID1149365Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced hind paw edema at 100 mg/kg, po administered as gum arabic suspension 30 mins prior to carrageenin injection measured 3 hrs post-carrageenin injection1977Journal of medicinal chemistry, Jan, Volume: 20, Issue:1
Synthesis and antiinflammatory and hypnotic activity of 5-alkoxy-3-(N-substituted carbamoyl)-1-phenylpyrazoles.
AID288193Flux ionization constant, pKa of the membrane permeability coefficient of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
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.
AID1123025Acute lethal toxicity in sc dosed mouse measured after 1 week1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on analgesic agents. 1.1a Preparation of 1,2-diphenyl-2-(4-substituted 1-piperazinyl)ethanol derivatives and structure-activity relationships.
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]
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID112288Compound was tested for antianalgesic activity by phenylquinone writhing method in mice.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Studies on heterocyclic compounds. 6. Synthesis and analgesic and antiinflammatory activities of 3,4-dimethylpyrano[2,3-c]pyrazol-6-one derivatives.
AID288186Permeability coefficient through artificial membrane in presence of stirred water layer at 200 rpm stirring speed2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
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.
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.
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.
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.
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.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,909)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903369 (86.19)18.7374
1990's332 (8.49)18.2507
2000's123 (3.15)29.6817
2010's68 (1.74)24.3611
2020's17 (0.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.10

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 Index53.10 (24.57)
Research Supply Index8.40 (2.92)
Research Growth Index4.09 (4.65)
Search Engine Demand Index92.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials130 (3.01%)5.53%
Reviews93 (2.15%)6.00%
Case Studies167 (3.87%)4.05%
Observational0 (0.00%)0.25%
Other3,930 (90.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]