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sulfisoxazole

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Description

Sulfisoxazole is a sulfonamide antibiotic that was first synthesized in the 1940s. It acts by inhibiting the synthesis of dihydrofolic acid, a key precursor in the biosynthesis of purines and pyrimidines, which are essential for DNA and RNA synthesis. Sulfisoxazole was widely used to treat a range of bacterial infections, including urinary tract infections, pneumonia, and meningitis. However, its use has declined in recent years due to the emergence of antibiotic resistance and the availability of newer, more effective antibiotics. Sulfisoxazole is still used in some cases, particularly for the treatment of certain types of urinary tract infections and for the prevention of recurrent urinary tract infections. It is available in oral and intravenous formulations. The compound is still studied today for its potential use in the treatment of other conditions, such as cancer and inflammatory bowel disease. '

Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms. [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 CID5344
CHEMBL ID453
CHEBI ID102484
SCHEMBL ID23467
MeSH IDM0020779

Synonyms (325)

Synonym
BIDD:GT0322
AC-1941
bdbm50034452
HMS3266N17
BB 0259593
AB00052104-14
BRD-K50859149-001-05-4
nsc-683536
4-amino-n-(3,4-dimethyl-isoxazol-5-yl)-benzenesulfonamide
nsc-38588
nsc38588
smr000037657
MLS000037737
MLS000028495
nsc33807
nsc-33807
DIVK1C_000579
KBIO1_000579
MLS000563718
SPECTRUM_001024
OPREA1_680668
OPREA1_828173
component of azo gantrisin
5-(p-aminobenzenesulfonamido)-3,4-dimethylisoxazole
benzenesulfonamide,4-dimethyl-5-isoxazolyl)-
sulfizin
nsc-13120
sulfazin
sulfisoxazole dialamine
sulfanilamide,4-dimethyl-5-isoxazolyl)-
component of azo-sulfizin
renosulfan
v-sul
nsc13120
5-sulfanilamido-3,4-dimethylisoxazole
soxomide
neoxazol
3,4-dimethylisoxale-5-sulfanilamide
entusil
soxisol
entusul
sulfisonazole
sulfaisoxazole
sulfalar
gantrosan
alphazole
wln: t5noj cmswr dz& d1 e1
sk-soxazole
sulbio
accuzole
cosoxazole
sulsoxin
sulfafurazol
uritrisin
chemouag
neazolin
g-sox
sulfadimethylisoxazole
isoxamin
thiasin
5-(4-aminophenylsulfonamido)-3,4-dimethylisoxazole
gantrisin
stansin
pancid
5-(p-aminobenzenesulphonamido)-3,4-dimethylisoxazole
roxosul tablets
sulfasoxazole
unisulf
sulfafurazole
soxo
sulfofurazole
amidoxal
n(sup1)-(3,4-dimethyl-5-isoxazolyl)sulfanilamide
sulfagan
sulfisoxasole
3,4-dimethyl-5-sulfonamidoisoxazole
sosol
sulfisoxazol
sulphafurazole
nci-c50022
gantrisona
norilgan-s
sulfoxol
5-(p-aminobenzenesulfonamido)-3,4-dimethylisooxale
sulfasol
3,4-dimethyl-5-sulfanilamidoisoxazole
dorsulfan warthausen
PRESTWICK_726
NCGC00016384-01
NCGC00023116-02
tocris-0731
cas-127-69-5
BSPBIO_000367
component of azo gantrisin accuzole
4-amino-n-(3,4-dimethyl-5-isoxazolyl)benzenesulfonamide
benzenesulfonamide, 4-amino-n-(3,4-dimethyl-5-isoxazolyl)-
nsc683536
4-amino-n-(3,4-dimethylisoxazol-5-yl)benzenesulfonamide
BPBIO1_000405
PRESTWICK3_000334
BSPBIO_003376
PRESTWICK2_000334
SPECTRUM5_001222
NCGC00023116-05
UPCMLD00X127-69-5:001
AB00052104
sulfanilamide, n(sup 1)-(3,4-dimethyl-5-isoxazolyl)-
j-sul
sulfapolar
sulfanilamide, n1-(3,4-dimethyl-5-isoxazolyl)-
solfafurazolo [dcit]
einecs 204-858-9
sulfazin (van)
ccris 568
ai3-24003
n(sup 1)-(3,4-dimethyl-5-isoxazolyl)-sulfanilamide
n(sup 1)-(3,4-dimethyl-5-isoxazolyl)sulphanilamide
sulphisoxazole
us-67
dorsulfan
soxamide
nu 445
gantrisine
koro-sulf
sulfizole
soxitabs
tl-azole
roxosul
nsc 683536
soxazole
urogan
sulfasoxizole
sulfisin
novosaxazole
u.s.-67
sulfizol
saxosozine
novazolo
nsc 13120
sulfisoxazolum
brn 0263871
hsdb 797
n(sup 1)-(3,4-dimethyl-5-isoxazolyl)sulfanilamide
sodizole
sulphafurazolum
sulfafurazolum [inn-latin]
urisoxin
sulfisoxazole
127-69-5
C07318
inchi=1/c11h13n3o3s/c1-7-8(2)13-17-11(7)14-18(15,16)10-5-3-9(12)4-6-10/h3-6,14h,12h2,1-2h
sulfisoxazole, >=99.0%
sulphadimethylisoxazole
DB00263
3,4-dimethylisoxazole-5-sulphanilamide
sulphofurazole
n1-(3,4-dimethyl-5-isoxazolyl)sulfanilamide
sulphaisoxazole
3,4-dimethyl-5-sulphonamidoisoxazole
4-amino-n-(3,4-dimethyl-5-isoxazolyl)benzenesulphonamide
3,4-dimethylisoxazole-5-sulfanilamide
5-sulphanilamido-3,4-dimethyl-isoxazole
sulphafurazol
n'-(3,4)dimethylisoxazol-5-yl-sulphanilamide
n1-(3,4-dimethyl-5-isoxazolyl)sulphanilamide
sulphisoxazol
3,4-dimethyl-5-sulphanilamidoisoxazole
sulfisoxazole (jp17/usp)
sulfafurazole (inn)
D00450
NCGC00023116-07
NCGC00023116-06
pediazole
vagilia
azo gantrisin
KBIO3_002596
KBIO2_001504
KBIO2_004072
KBIO2_006640
KBIOSS_001504
KBIOGR_000757
PRESTWICK0_000334
PRESTWICK1_000334
SPBIO_002288
SPBIO_001449
SPECTRUM4_000349
NINDS_000579
SPECTRUM2_001325
SPECTRUM3_001728
SPECTRUM1500555
IDI1_000579
NCGC00023116-08
NCGC00016384-02
STK400452
4-amino-n-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide
n(1)-(3,4-dimethyl-5-isoxazolyl)sulphanilamide
HMS2092K13
AKOS000310021
CHEMBL453 ,
HMS501M21
HMS1569C09
CHEBI:102484 ,
sulfafurazolum
n(1)-(3,4-dimethyl-5-isoxazolyl)sulfanilamide
NCGC00016384-10
AKOS000119074
HMS2096C09
HMS3259C06
[(4-aminophenyl)sulfonyl](3,4-dimethylisoxazol-5-yl)amine
solfafurazolo
740t4c525w ,
4-27-00-04747 (beilstein handbook reference)
sulfisoxazole [usp:jan]
unii-740t4c525w
sulfafurazole [inn]
tox21_302851
NCGC00256605-01
dtxcid001292
dtxsid6021292 ,
tox21_202265
NCGC00259814-01
tox21_112958
nsc-757343
pharmakon1600-01500555
nsc757343
tox21_110409
astrazolo
resoxol
ganda
roxoxol
azosulfizin
barazae
sulphafuraz
sulfagen
bactesulf
suloxsol
HMS2233G23
CCG-39263
NCGC00016384-07
NCGC00016384-12
NCGC00016384-05
NCGC00016384-11
NCGC00016384-04
NCGC00016384-09
NCGC00016384-06
NCGC00016384-08
NCGC00016384-03
FT-0631743
NCGC00016384-14
sulfisoxazole [jan]
sulfisoxazole component of azo gantrisin
sulfisoxazole [hsdb]
sulfisoxazole [orange book]
sulfafurazole [ep monograph]
sulfafurazole [iarc]
sulfisoxazole [vandf]
sulfafurazole [mart.]
sulfisoxazole [usp monograph]
sulfafurazole [who-dd]
azo gantrisin component sulfisoxazole
sulfisoxazole [usp-rs]
sulfisoxazole [mi]
sulfisoxazole [green book]
EPITOPE ID:122240
S1916
F0848-0391
HMS3374K11
HY-B0323
NC00536
4-amino-n-(3,4-dimethylisoxazol-5-yl)-benzenesulfonamide
SCHEMBL23467
NCGC00016384-15
tox21_110409_1
4-amino-n-(3,4-dimethyl-5-isoxazolyl)benzene-sulfonamide
gantrizin
5-(4-aminophenylsulphonamido)-3,4-dimethylisoxazole
4-amino-n-(3,4-dimethyl-5-isoxazolyl)benzenesulfonamide #
sulfanilamide, n(sup1)-(3,4-dimethyl-5-isoxazolyl)-
5-(p-aminobenzenesulphonamide)-3,4-dimethylisoxazole
azo-sulfizin (salt/mix)
sulfanilamide, n.sup1.-(3,4-dimethyl-5-isoxazolyl)-
azo gantrisin (salt/mix)
AB00052104_15
AB00052104_16
mfcd00003150
4-amino-n-(dimethyl-1,2-oxazol-5-yl)benzene-1-sulfonamide
J-005528
sr-01000003085
SR-01000003085-5
sulfisoxazole, united states pharmacopeia (usp) reference standard
sulfisoxazole, vetranal(tm), analytical standard
HMS3655B03
sulfafurazole, european pharmacopoeia (ep) reference standard
SR-01000003085-2
SR-01000003085-6
SBI-0051529.P003
HMS3713C09
SW196872-3
Q372598
gtpl12700
HMS3675F03
U0098
HMS3411F03
BRD-K50859149-001-10-4
STR04988
4-amino-n-(3,4-dimethyl-1,2-oxazol-5-yl)benzene-1-sulfonamide
H10712
4-amino-n-(3,4-dimethyl-5-isoxazolyl)benzenesulfonamid
nu445
sulfisoxazole 1000 microg/ml in acetonitrile
4-amino-n-(3,4-dimethyl-isoxazol-5-yl) benzene-13c6-sulfonamide
EN300-35024
4-amino-n-(3,4-dimethyl-2,5-dihydro-1,2-oxazol-5-ylidene)benzene-1-sulfonamide
Z90124784
sulfisoxazole (usp-rs)
sulfafurazole (ep monograph)
sulfafurazole (iarc)
soxisol tablets
3,4-dimethylisoaxazole-5-sulphanilimide
sulfafurazole (mart.)
sulfanilamide, n(sup 1)-(3,4-dimethyl-5-isoxazolyl)
sulfanilamide, n(1)-(3,4-dimethyl-5-isoxazolyl)-
sulfafurazolum (inn-latin)
sulfisoxazole (usp monograph)
sulfisoxazole (usp:jan)

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Pretreatment with sulfisoxazole produced an important enhancement in the effect of propofol in both tests."( Interaction between propofol and sulfisoxazole in mice an in vivo and in vitro study.
Calvo, R; Carlos, R; Costela, JL; Jiménez, R; Zamacona, MK, 1996
)
0.9

Pharmacokinetics

The pharmacokinetic profile of sulfisoxazole was studied and compared in dogs, swine, and humans. The loss of weight up to 44 per cent within an individual over a year's time had no significant effect.

ExcerptReferenceRelevance
" During the exponential postabsorption phase the relative error is only a function of the ratio (n) of the time interval over the half-life of the two plasma data points in the interval."( Critical evaluation of the potential error in pharmacokinetic studies of using the linear trapezoidal rule method for the calculation of the area under the plasma level--time curve.
Chiou, WL, 1978
)
0.26
" These results are consistent with recently developed pharmacokinetic theory according to which the plasma clearance of total bilirubin should increase upon administration of a displacing agent while the plasma clearance of free bilirubin should remain unchanged."( Effect of sulfisoxazole on pharmacokinetics of free and plasma protein-bound bilirubin in experimental unconjugated hyperbilirubinemia.
Levy, G; Oie, S, 1979
)
0.66
"In the analysis of individual pharmacokinetic data by nonlinear regression it is important to allow for possible heterogeneity of variance in the response."( Fitting heteroscedastic regression models to individual pharmacokinetic data using standard statistical software.
Giltinan, DM; Ruppert, D, 1989
)
0.28
" Pharmacokinetic absorption behavior of a sustained-release preparation of theophylline after repetitive oral administration was adequately evaluated using MFA-MULTI."( Pharmacokinetic analysis of single- or multiple-dose plasma drug concentration data with a microcomputer using multi-fraction absorption models.
Murata, K; Noda, K; Samejima, M; Tagawa, K, 1989
)
0.28
" The pharmacokinetic absorption behavior of a sustained-release preparation of diltiazem hydrochloride was studied using a multi-fraction absorption model."( Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multi-fraction absorption models.
Kohno, K; Murata, K; Noda, K; Samejima, M, 1987
)
0.27
"The pharmacokinetic profile of sulfisoxazole was studied and compared in dogs, swine, and humans."( Pharmacokinetics of sulfisoxazole compared in humans and two monogastric animal species.
Edds, GT; Lee, C; Suber, RL; Torosian, G, 1981
)
0.87
" The tmax value and plasma half-life of sulfisoxazole were significantly longer, and the total body and renal clearances of the drug decreased in the elderly subjects."( Pharmacokinetics of sulfisoxazole in young and elderly subjects.
Barbeau, G; Bélanger, PM; Boisvert, A, 1984
)
0.86
" However, its biological half-life and the apparent distribution volume of the central compartment were significantly lower and the intercompartmental transport rate constants and the urinary excretion rate constant were significantly greater, in phenobarbital treated rats than in control rats."( Effects of phenobarbital on the distribution pharmacokinetics and biological half-lives of model nonmicrosomal enzyme metabolizable sulfonamides in rats.
Kundu, S; Nagwekar, JB, 1982
)
0.26
" The loss of weight up to 44 per cent within an individual over a year's time had no significant effect on the apparent volumes of distribution or other pharmacokinetic parameters of sulfisoxazole and its N4-acetylsulfisoxazole metabolite."( Surgically affected sulfisoxazole pharmacokinetics in the morbidly obese.
Eberst, K; Garrett, ER; O'Leary, JP; Süverkrup, RS; Yost, RL,
)
0.65
" 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
"This study was undertaken to evaluate the ocular pharmacokinetic of sulfisoxazole."( Pharmacokinetic of sulfisoxazole in aqueous humor after topical and subconjunctival application in dogs.
Eraslan, G; Essiz, D; Kibar, M; Liman, BC; Sahindokuyucu, F, 2007
)
0.9
" Pharmacokinetic (PK) parameters along with liver and muscle tissue levels were collected, and their contributions to total V(ss) were calculated."( The impact of hepatic uptake on the pharmacokinetics of organic anions.
Gardiner, P; Paine, SW, 2011
)
0.37

Bioavailability

The effects of hexadecane, oleyl alcohol, polysorbate 80, trioctanoin, and triolein on the bioavailability of sulfisoxazole N1-acetyl, dicumarol, and griseofulvin were investigated. There was no significant variation between the two groups of volunteers in the absorption rate constant, Cmax, bioavailability.

ExcerptReferenceRelevance
" In contrast to these results, compounds such as urea and amitrole, which remain completely nonionized over the pH range studied, showed no change in absorption rate when the pH was varied."( Lung pH and pulmonary absorption of nonvolatile drugs in the rat.
Less, MJ; Schanker, LS,
)
0.13
" This pH-dependent release characteristic may not correspond to a change in bioavailability in all cases, but it represents a potential problem which should be considered by the formulator."( PH-dependent drug release from certain commercial tablets.
Lach, JL; Sutton, JE; Wagner, RS, 1977
)
0.26
"The effects of hexadecane, oleyl alcohol, polysorbate 80, trioctanoin, and triolein on the bioavailability of sulfisoxazole N1-acetyl, dicumarol, and griseofulvin were investigated."( Effects of lipids on bioavailability of sulfisoxazole acetyl, dicumarol, and griseofulvin in rats.
Bloedow, DC; Hayton, WL, 1976
)
0.74
" When the absorption rate constant is allowed to approach alpha, a typical two-compartment oral absorption curve is obtained, which is described by a triexponential equation."( Interpretation of plasma concentration-time curves after oral dosing.
Benet, LZ; Ronfeld, RA, 1977
)
0.26
" Irradiation apparently does not affect the absorption of drugs that are normally well absorbed or poorly absorbed due to slow transport across the GI mucosa."( GI drug absorption in rats exposed to cobalt-60 gamma-radiation I: Extent of absorption.
Brady, ME; Hayton, WL, 1977
)
0.26
"The rate of absorption of sulfanilamide, bretylium tosylate, sulfisoxazole acetyl, and riboflavin was studied in rats exposed to 850 rad of cobalt-60 gamma-radiation either 1 or 5 days before oral drug administration."( GI drug absorption in rats exposed to cobalt-60 gamma-radiation II: in vivo rate of absorption.
Brady, ME; Hayton, WL, 1977
)
0.5
" This method can be used for an efficient monitoring of sulfisoxazole in plasma during the chemotherapy of bacterial infections, and also for the bioavailability study of the drug from dosage forms."( High pressure liquid chromatographic determination of sulfisoxazole in plasma.
Chiou, WL; Gadalla, MA; Peng, GW, 1977
)
0.75
" The systemic bioavailability was 19."( Kinetic disposition, systemic bioavailability, tissue levels and acetylation of some sulphonamides in goats.
Atef, M; Issa, M; Ramadan, A; Youssef, SA,
)
0.13
"Nonlinear regression analysis of plasma drug concentration data with irregular or stepwise absorption profiles was studied using multi-fraction absorption models in which drugs in the gastrointestinal tract were assumed to be divided into several fractions each with its respective lag time and absorption rate constant."( Pharmacokinetic analysis of concentration data of drugs with irregular absorption profiles using multi-fraction absorption models.
Kohno, K; Murata, K; Noda, K; Samejima, M, 1987
)
0.27
" The bioavailability was 69."( Pharmacokinetics of sulfisoxazole compared in humans and two monogastric animal species.
Edds, GT; Lee, C; Suber, RL; Torosian, G, 1981
)
0.59
" There was no significant variation between the two groups of volunteers in the absorption rate constant, Cmax, bioavailability, the fraction of the dose of sulfisoxazole excreted unchanged, the area under the plasma curve of the N4-acetyl conjugate formed, and in the apparent volume of distribution of the drug."( Pharmacokinetics of sulfisoxazole in young and elderly subjects.
Barbeau, G; Bélanger, PM; Boisvert, A, 1984
)
0.79
" The products had been the subject of earlier in vivo bioavailability studies with human subjects."( In vivo-in vitro correlations with a commercial dissolution simulator II: papaverine, phenytoin, and sulfisoxazole.
Meyer, MC; Yau, MK, 1983
)
0.48
" Bioavailability decreases both when osmotic pressure decreases and when it increases."( The effect of osmotic pressure on the intestinal absorption of sulfafurazol and ethanol in the rat.
Lehmussaari, L; Marvola, M; Niinimäki, L, 1980
)
0.26
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Pharmacokinetic parameters including absorption rate constant (k(a)), slope factor (beta), absorption half-life (t1/2a), half-life of elimination in aqueous humor (t1/2beta), maximal concentration in aqueous humor (C(max)), time to reach C(max) (t(max)), mean residence time in aqueous humor (MRT) and area under the concentration time curve from zero up to infinity (AUC(0-infinity)) were calculated."( Pharmacokinetic of sulfisoxazole in aqueous humor after topical and subconjunctival application in dogs.
Eraslan, G; Essiz, D; Kibar, M; Liman, BC; Sahindokuyucu, F, 2007
)
0.67
"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 relative bioavailability of N1AS to sulfisoxazole was about two, indicating that a half-dose of N1AS would be equivalent to a dose of sulfisoxazole to achieve the same systemic exposure to sulfisoxazole."( Simultaneous determination of N(1)-acetyl sulfisoxazole and its metabolites, and relative bioavailability compare to sulfisoxazole in rats.
Kang, W; Kim, E, 2016
)
0.96
"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 reverse phase high pressure liquid chromatographic method for the determination of sulfisoxazole in tablets, solution, and ointment dosage forms was collaboratively studied by 7 laboratories. The dissolution profiles of 11 commercially available papaverine, phenytoin, and sulfis Oxazole dosage forms were determined using a dissolution simulator.

ExcerptRelevanceReference
" The osmotic pressure of hypertonic solutions, especially, might affect absorption of drug from its dosage form."( The effects of some sweetening agents and osmotic pressure on the intestinal absorption of sulfafurazole in the rat.
Heliövaara, ML; Huikari, A; Marvola, M; Reinikainen, A, 1979
)
0.26
" Furosemide and ethacrynic acid, when used at the recommended dosage (1 mg/kg), would probably not produce a significant increase in free bilirubin in most infants."( Displacement of bilirubin from human albumin by three diuretics.
Ahlfors, CE; Rasmussen, F; Wennberg, RP, 1977
)
0.26
" This method can be used for an efficient monitoring of sulfisoxazole in plasma during the chemotherapy of bacterial infections, and also for the bioavailability study of the drug from dosage forms."( High pressure liquid chromatographic determination of sulfisoxazole in plasma.
Chiou, WL; Gadalla, MA; Peng, GW, 1977
)
0.75
" No useful correlation was observed between the in vivo and in vitro studies for the dosage forms tested."( Bioavailability of 11 sulfisoxazole products in humans.
Melikian, AP; Meyer, MC; Slywka, GW; Straughn, AB; Whyatt, PL, 1976
)
0.57
" However, from differences in dosage and the pharmacokinetics of the two substances it may be concluded, that the risk of possibly causing a kernicterus by Cardiogreen is limited to only extrem cases."( [The influence of cardiogreen on the albumin binding of bilirubin in the neonatal period].
Kretzschmar, GW, 1975
)
0.25
" In this study, mean daily dosage was 40-50 mg/kg for cefaclor and 50 mg/kg ES + 150 mg/kg sulfamide for Pediazole."( [An open randomized trial, Pediazole versus cefaclor in the treatment of acute otitis media in children].
Bedbeder, P; Boucherat, M; Bouhanna, CA; Cohen, R; de La Rocque, F; Geslin, P; Peynegre, R; Reinert, P, 1991
)
0.28
" They also consider questionable the elimination tendency of the small dosage of microtablets of nitrofurantoin (10 mcg) and sulfamide (30 mcg), since their apparent insufficiency might be due less to the inadequate contraction of substances and more to the inadequate testing media."( [Changes in the antibacterial activity of nitrofurantoin preparations induced by peptone and hydrolysates].
Chissacof, I; Corlăţean, M; Dancea, Z; Marica, D; Miclea, I; Oprea, C,
)
0.13
" We conclude that trimethoprim is as effective as sulphisoxazole in the treatment of simple acute urinary tract infections of children and recommend it, in the dosage used, as an alternative first-choice drug, especially for patients who have had side effects from sulphonamides or nitrofurantoin."( Trimethoprim in the treatment of acute urinary tract infections in children.
Hoppu, K; Koskimies, O; Vilska, J, 1988
)
0.27
" They suffered from acute urinary tract infection and were treated with conventional dosage regimen of either of the sulfonamides."( Sulfadiazine versus sulfafurazole excretion in urine and risk of crystallization in children with conventional dosage regimen.
Anttila, R; Janas, M; Wilén, G; Ylitalo, P, 1985
)
0.27
"A reverse phase high pressure liquid chromatographic method for the determination of sulfisoxazole in tablets, solution, and ointment dosage forms was collaboratively studied by 7 laboratories."( High pressure liquid chromatographic determination of sulfisoxazole in dosage forms: collaborative study.
Roos, RW, 1983
)
0.74
"The dissolution profiles of 11 commercially available papaverine, phenytoin, and sulfisoxazole dosage forms were determined using a dissolution simulator."( In vivo-in vitro correlations with a commercial dissolution simulator II: papaverine, phenytoin, and sulfisoxazole.
Meyer, MC; Yau, MK, 1983
)
0.71
"Plasma concentrations of total and unbound sulfisoxazole were followed after single intravenous and oral doses of 1 g sulfisoxazole and during a 500-mg, four-time-a-day dosing regimen in six healthy males, using a specific high pressure liquid chromatographic assay method."( Comparison of the disposition of total and unbound sulfisoxazole after single and multiple dosing.
Fleckenstein, L; Gambertoglio, JG; Oie, S, 1982
)
0.78
"A high pressure liquid chromatographic method has been developed for the identification and determination of sulfisoxazole in tablet, liquid, and ointment dosage forms."( High pressure liquid chromatographic determination of sulfisoxazole in pharmaceuticals and separation patterns of other sulfonamides.
Roos, RW, 1981
)
0.72
" Dosing of this drug on a mg kg-1 basis is contraindicated."( Surgically affected sulfisoxazole pharmacokinetics in the morbidly obese.
Eberst, K; Garrett, ER; O'Leary, JP; Süverkrup, RS; Yost, RL,
)
0.45
" SD in lower than the usual dosage would appear to be a practical alternative in the treatment of acute urinary tract infections caused by sulfonamide-sensitive micro-organisms in children."( Reduced sulfadiazine dose in the treatment of acute urinary tract infection in children.
Anttila, R; Julkunen, R; Seppänen, J, 1980
)
0.26
" 4 It is concluded that alternations in the dosage schedule may not be necessary in the treatment of undernourished adults with sulphafurazole."( Kinetics of sulphafurazole in undernutrition.
Shastri, RA, 1980
)
0.26
" In this study, the three spectrophotometric methods can be satisfactorily used for the quantitative analysis and for dissolution tests of multicomponent dosage forms."( Chemometric and derivative methods as flexible spectrophotometric approaches for dissolution and assaying tests in multicomponent tablets.
Koundourellis, JE; Malliou, ET; Markopoulou, CK, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
drug allergenAny drug which causes the onset of an allergic reaction.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
isoxazolesOxazoles in which the N and O atoms are adjacent.
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
sulfonamide antibioticA class of sulfonamides whose members generally have bacteriostatic antibiotic properties.
[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 (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
TDP1 proteinHomo sapiens (human)Potency18.83750.000811.382244.6684AID686978
GLI family zinc finger 3Homo sapiens (human)Potency3.91390.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency28.57380.000221.22318,912.5098AID588515; AID743036; AID743053
thyroid stimulating hormone receptorHomo sapiens (human)Potency4.59390.001318.074339.8107AID926; AID938
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.22020.000214.376460.0339AID588532
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency46.11020.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency13.88030.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.01730.001530.607315,848.9004AID1224841; AID1224848
farnesoid X nuclear receptorHomo sapiens (human)Potency50.11870.375827.485161.6524AID588527
pregnane X nuclear receptorHomo sapiens (human)Potency27.25050.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.67210.000229.305416,493.5996AID743069; AID743079
67.9K proteinVaccinia virusPotency22.38720.00018.4406100.0000AID720580
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.00630.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency8.91250.010039.53711,122.0200AID588547
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency30.57560.000323.4451159.6830AID743066
gemininHomo sapiens (human)Potency29.09290.004611.374133.4983AID624296
Cellular tumor antigen p53Homo sapiens (human)Potency14.96010.002319.595674.0614AID651631
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
[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)422.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
Endothelin-1 receptorHomo sapiens (human)IC50 (µMol)7.81330.00000.76479.9000AID625257; AID66341; AID68661
Endothelin-1 receptorHomo sapiens (human)Ki13.46500.00000.430010.0000AID625257
Endothelin-1 receptorRattus norvegicus (Norway rat)IC50 (µMol)4.89000.00001.774610.0000AID66057; AID66184
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]

Biological Processes (238)

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)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic cell cycleEndothelin-1 receptorHomo sapiens (human)
branching involved in blood vessel morphogenesisEndothelin-1 receptorHomo sapiens (human)
response to hypoxiaEndothelin-1 receptorHomo sapiens (human)
in utero embryonic developmentEndothelin-1 receptorHomo sapiens (human)
blood vessel remodelingEndothelin-1 receptorHomo sapiens (human)
response to amphetamineEndothelin-1 receptorHomo sapiens (human)
regulation of heart rateEndothelin-1 receptorHomo sapiens (human)
glomerular filtrationEndothelin-1 receptorHomo sapiens (human)
cardiac chamber formationEndothelin-1 receptorHomo sapiens (human)
left ventricular cardiac muscle tissue morphogenesisEndothelin-1 receptorHomo sapiens (human)
atrial cardiac muscle tissue developmentEndothelin-1 receptorHomo sapiens (human)
cardiac neural crest cell migration involved in outflow tract morphogenesisEndothelin-1 receptorHomo sapiens (human)
noradrenergic neuron differentiationEndothelin-1 receptorHomo sapiens (human)
intracellular calcium ion homeostasisEndothelin-1 receptorHomo sapiens (human)
smooth muscle contractionEndothelin-1 receptorHomo sapiens (human)
mitochondrion organizationEndothelin-1 receptorHomo sapiens (human)
signal transductionEndothelin-1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
activation of adenylate cyclase activityEndothelin-1 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEndothelin-1 receptorHomo sapiens (human)
respiratory gaseous exchange by respiratory systemEndothelin-1 receptorHomo sapiens (human)
regulation of blood pressureEndothelin-1 receptorHomo sapiens (human)
cell population proliferationEndothelin-1 receptorHomo sapiens (human)
response to woundingEndothelin-1 receptorHomo sapiens (human)
gene expressionEndothelin-1 receptorHomo sapiens (human)
protein kinase A signalingEndothelin-1 receptorHomo sapiens (human)
regulation of glucose transmembrane transportEndothelin-1 receptorHomo sapiens (human)
neural crest cell fate commitmentEndothelin-1 receptorHomo sapiens (human)
artery smooth muscle contractionEndothelin-1 receptorHomo sapiens (human)
neuron remodelingEndothelin-1 receptorHomo sapiens (human)
heparin metabolic processEndothelin-1 receptorHomo sapiens (human)
thyroid gland developmentEndothelin-1 receptorHomo sapiens (human)
cellular response to oxidative stressEndothelin-1 receptorHomo sapiens (human)
embryonic heart tube developmentEndothelin-1 receptorHomo sapiens (human)
aorta developmentEndothelin-1 receptorHomo sapiens (human)
vasoconstrictionEndothelin-1 receptorHomo sapiens (human)
norepinephrine metabolic processEndothelin-1 receptorHomo sapiens (human)
middle ear morphogenesisEndothelin-1 receptorHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionEndothelin-1 receptorHomo sapiens (human)
cellular response to human chorionic gonadotropin stimulusEndothelin-1 receptorHomo sapiens (human)
enteric nervous system developmentEndothelin-1 receptorHomo sapiens (human)
sympathetic nervous system developmentEndothelin-1 receptorHomo sapiens (human)
axon extensionEndothelin-1 receptorHomo sapiens (human)
embryonic skeletal system developmentEndothelin-1 receptorHomo sapiens (human)
neuromuscular processEndothelin-1 receptorHomo sapiens (human)
sodium ion homeostasisEndothelin-1 receptorHomo sapiens (human)
canonical Wnt signaling pathwayEndothelin-1 receptorHomo sapiens (human)
face developmentEndothelin-1 receptorHomo sapiens (human)
axonogenesis involved in innervationEndothelin-1 receptorHomo sapiens (human)
establishment of endothelial barrierEndothelin-1 receptorHomo sapiens (human)
pharyngeal arch artery morphogenesisEndothelin-1 receptorHomo sapiens (human)
renal sodium ion absorptionEndothelin-1 receptorHomo sapiens (human)
calcium ion transmembrane transportEndothelin-1 receptorHomo sapiens (human)
cellular response to follicle-stimulating hormone stimulusEndothelin-1 receptorHomo sapiens (human)
cellular response to luteinizing hormone stimulusEndothelin-1 receptorHomo sapiens (human)
protein transmembrane transportEndothelin-1 receptorHomo sapiens (human)
glomerular endothelium developmentEndothelin-1 receptorHomo sapiens (human)
podocyte differentiationEndothelin-1 receptorHomo sapiens (human)
endothelin receptor signaling pathway involved in heart processEndothelin-1 receptorHomo sapiens (human)
renal albumin absorptionEndothelin-1 receptorHomo sapiens (human)
vascular associated smooth muscle cell developmentEndothelin-1 receptorHomo sapiens (human)
mesenchymal cell apoptotic processEndothelin-1 receptorHomo sapiens (human)
sympathetic neuron axon guidanceEndothelin-1 receptorHomo sapiens (human)
semaphorin-plexin signaling pathway involved in axon guidanceEndothelin-1 receptorHomo sapiens (human)
podocyte apoptotic processEndothelin-1 receptorHomo sapiens (human)
meiotic cell cycle process involved in oocyte maturationEndothelin-1 receptorHomo sapiens (human)
cranial skeletal system developmentEndothelin-1 receptorHomo sapiens (human)
response to acetylcholineEndothelin-1 receptorHomo sapiens (human)
regulation of protein localization to cell leading edgeEndothelin-1 receptorHomo sapiens (human)
positive regulation of cation channel activityEndothelin-1 receptorHomo sapiens (human)
endothelin receptor signaling pathwayEndothelin-1 receptorHomo sapiens (human)
developmental pigmentationEndothelin-1 receptorHomo 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 (59)

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)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
phosphatidylinositol phospholipase C activityEndothelin-1 receptorHomo sapiens (human)
endothelin receptor activityEndothelin-1 receptorHomo sapiens (human)
protein bindingEndothelin-1 receptorHomo 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 (35)

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)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneEndothelin-1 receptorHomo sapiens (human)
plasma membraneEndothelin-1 receptorHomo 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 (177)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
AID66201Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.
AID1185241Antimicrobial activity against Escherichia coli RCMB 010052 assessed as absence of turbidity after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
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.
AID1890854Antibacterial activity against methicillin-resistant Staphylococcus aureus N315 assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1890859Antibacterial activity against Pseudomonas aeruginosa assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
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.
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.
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.
AID24211Compound is evaluated for ionization constant log k1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
A simplified high-pressure liquid chromatography method for determining lipophilicity for structure-activity relationships.
AID167576In vitro functional antagonistic testing by obtaining ET-1 concentration response curves in rabbit carotid artery rings in the presence or absence of antagonist.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.
AID1890857Antibacterial activity against Escherichia coli assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1890855Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
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]
AID1668063Inhibition of DHPS in Klebsiella pneumoniae assessed as antibacterial activity by measuring inhibition of bacterial growth incubated for 24 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1185238Antimicrobial activity against Staphylococcus epidermidis RCMB 010024 assessed as inhibition zone at 5 mg/ml after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
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).
AID1668052Inhibition of DHPS in Streptococcus pneumoniae assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1668068Inhibition of DHPS in Syncephalastrum racemosum assessed as antifungal activity by measuring inhibition of fungal growth incubated for 48 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
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.
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]
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).
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).
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).
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).
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]
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]
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.
AID1185239Antimicrobial activity against Staphylococcus epidermidis RCMB 010024 assessed as absence of turbidity after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1668064Inhibition of DHPS in Aspergillus fumigatus assessed as antifungal activity by measuring inhibition zone at 5 mg/mL incubated for 48 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID13311Negative log of Langmuir's alpha constant (-log alpha), which is inversely proportional to the effective binding constant (protein binding)1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
A simplified high-pressure liquid chromatography method for determining lipophilicity for structure-activity relationships.
AID1185246Antifungal activity against Aspergillus fumigatus RCMB 02568 assessed as inhibition zone at 5 mg/ml after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1668065Inhibition of DHPS in Syncephalastrum racemosum assessed as antifungal activity by measuring inhibition zone at 5 mg/mL incubated for 48 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1185249Antifungal activity against Syncephalastrum racemosum RCMB 05922 assessed as absence of turbidity after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1185236Antimicrobial activity against Bacillis subtilis RCMB 010067 assessed as inhibition zone at 5 mg/ml after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID599144Intrinsic solubility, log 1/S0 of the compound2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Computational aqueous solubility prediction for drug-like compounds in congeneric series.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1668053Inhibition of DHPS in Bacillus subtilis assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase 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.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1668054Inhibition of DHPS in Staphylococcus epidermidis assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1890853Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
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).
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.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID409943Inhibition of human recombinant MAOB by fluorimetric method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1668066Inhibition of DHPS in Geotrichum candidum assessed as antifungal activity by measuring inhibition zone at 5 mg/mL incubated for 48 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1668061Inhibition of DHPS in Escherichia coli assessed as antibacterial activity by measuring inhibition of bacterial growth incubated for 24 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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).
AID1185244Antimicrobial activity against Klebsiella pneumoniae RCMB 010093 assessed as inhibition zone at 5 mg/ml after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID66040Antagonism of ET-1 induced increase in intracellular Ca+2 in rabbit carotid artery rings1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
AID64417Minimum inhibitory concentration (bacteriostatic) against Escherichia coli at pH 7.2 (Sauterne''s medium)1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
A simplified high-pressure liquid chromatography method for determining lipophilicity for structure-activity relationships.
AID68661Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells1994Journal of medicinal chemistry, Feb-04, Volume: 37, Issue:3
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
AID1668067Inhibition of DHPS in Aspergillus fumigatus assessed as antifungal activity by measuring inhibition of fungal growth incubated for 48 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1890852Antibacterial activity against Klebsiella pneumoniae assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1890858Antibacterial activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1668060Inhibition of DHPS in Staphylococcus epidermidis assessed as antibacterial activity by measuring inhibition of bacterial growth incubated for 24 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
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.
AID346025Binding affinity to beta cyclodextrin2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Convenient QSAR model for predicting the complexation of structurally diverse compounds with beta-cyclodextrins.
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).
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).
AID1185240Antimicrobial activity against Escherichia coli RCMB 010052 assessed as inhibition zone at 5 mg/ml after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1185237Antimicrobial activity against Bacillis subtilis RCMB 010067 assessed as absence of turbidity after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID624647Inhibition of AZT glucuronidation by human UGT enzymes from liver microsomes2005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID26320pKa value is evaluated1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
A simplified high-pressure liquid chromatography method for determining lipophilicity for structure-activity relationships.
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).
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.
AID1918193Dissociation constant, pKa of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID66699Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor.2000Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
AID1185248Antifungal activity against Syncephalastrum racemosum RCMB 05922 assessed as inhibition zone at 5 mg/ml after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1890856Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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).
AID1185247Antifungal activity against Aspergillus fumigatus RCMB 02568 assessed as absence of turbidity after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID64418Minimum inhibitory concentration (bacteriostatic) against Escherichia coli at pH 7.41983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
A simplified high-pressure liquid chromatography method for determining lipophilicity for structure-activity relationships.
AID1185251Antifungal activity against Geotrichum candidum RCMB 05097 assessed as absence of turbidity after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID433903Hepatotoxicity in mouse assessed as carcinogenic potency2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Development of QSAR models for predicting hepatocarcinogenic toxicity of chemicals.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1668069Inhibition of DHPS in Geotrichum candidum assessed as antifungal activity by measuring inhibition of fungal growth incubated for 48 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
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
AID1668057Inhibition of DHPS in Klebsiella pneumoniae assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1668058Inhibition of DHPS in Streptococcus pneumoniae assessed as antibacterial activity by measuring inhibition of bacterial growth incubated for 24 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
AID66184Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor2000Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
AID1185234Antimicrobial activity against Streptococcus pneumoniae RCMB 010010 assessed as inhibition zone at 5 mg/ml after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID1668056Inhibition of DHPS in Proteus vulgaris assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID409942Inhibition of human recombinant MAOA by fluorimetric method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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).
AID1185235Antimicrobial activity against Streptococcus pneumoniae RCMB 010010 assessed as absence of turbidity after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
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]
AID1890860Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
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.
AID1890861Antibacterial activity against Acinetobacter baumannii assessed as inhibition of bacterial growth measured after 24 hrs by CLSI based broth microdilution method2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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.
AID1918194Lipophilicity, log D of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1668055Inhibition of DHPS in Escherichia coli assessed as antibacterial activity by measuring inhibition zone at 5 mg/mL incubated for 24 hrs by disk diffusion method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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).
AID1185245Antimicrobial activity against Klebsiella pneumoniae RCMB 010093 assessed as absence of turbidity after 24 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID599143Lipophilicity, log P of the compound2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Computational aqueous solubility prediction for drug-like compounds in congeneric series.
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.
AID66341Inhibitory concentration against Endothelin A receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
Selective optimization of side activities: another way for drug discovery.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1668059Inhibition of DHPS in Bacillus subtilis assessed as antibacterial activity by measuring inhibition of bacterial growth incubated for 24 hrs by microbroth dilution method2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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).
AID66057Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.
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.
AID1185250Antifungal activity against Geotrichum candidum RCMB 05097 assessed as inhibition zone at 5 mg/ml after 48 hrs2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis, antimicrobial evaluation and molecular docking studies of some new thiophene, pyrazole and pyridone derivatives bearing sulfisoxazole moiety.
AID180489Tested for antagonistic activity against ET-1 induced increase in intracellular [Ca2+] in VSM-A10 cells.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.
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.
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.
AID493017Wombat Data for BeliefDocking2000Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (947)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990792 (83.63)18.7374
1990's54 (5.70)18.2507
2000's31 (3.27)29.6817
2010's46 (4.86)24.3611
2020's24 (2.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 47.05

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

MetricThis Compound (vs All)
Research Demand Index47.05 (24.57)
Research Supply Index6.99 (2.92)
Research Growth Index4.47 (4.65)
Search Engine Demand Index76.22 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (47.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials81 (8.10%)5.53%
Reviews23 (2.30%)6.00%
Case Studies53 (5.30%)4.05%
Observational0 (0.00%)0.25%
Other843 (84.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Prospective Randomized Controlled Study to Compare Efficacy of Caspofungin Combined With Trimethoprim-sulfamethoxazole Versus Trimethoprim/Sulfamethoxazole as First-line Therapy in Non-HIV Patients With Severe Pneumocystis Pneumonia [NCT03978559]Phase 4122 participants (Anticipated)Interventional2019-08-14Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]