Page last updated: 2024-12-05

piretanide

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

Description

piretanide: potent inhibitor of chloride transport; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4849
CHEMBL ID349803
CHEBI ID32015
SCHEMBL ID49473
MeSH IDM0064705

Synonyms (88)

Synonym
4-phenoxy-3-(pyrrolidin-1-yl)-5-sulfamoylbenzoic acid
smr001233430
MLS002154123
BRD-K87990216-001-03-7
tauliz
piretanide
hoe-118
eurelix
3-(aminosulfonyl)-4-(phenyloxy)-5-pyrrolidin-1-ylbenzoic acid
einecs 259-852-9
s 734118
acide phenoxy-4-(1-pyrrolidinyl)-3-sulfamoyl-5 benzoique [french]
arlix
brn 5633965
3-(aminosulfonyl)-4-phenoxy-5-(1-pyrrolidinyl)-benzoic acid
piretanidum [inn-latin]
4-phenoxy-3-(1-pyrrolidinyl)-5-sulfamoylbenzoic acid
piretanido [inn-spanish]
4-phenoxy-3-pyrrolidin-1-yl-5-sulfamoylbenzoic acid
benzoic acid, 3-(aminosulfonyl)-4-phenoxy-5-(1-pyrrolidinyl)-
s 73 4118
piretanido [spanish]
hoe 118
NCGC00016878-01
cas-55837-27-9
BPBIO1_001072
BSPBIO_000974
AB00514020
DB02925
piretanide (jan/usan/inn)
arelix (tn)
D01634
55837-27-9
SPBIO_002907
PRESTWICK0_001047
PRESTWICK1_001047
PRESTWICK2_001047
PRESTWICK3_001047
NCGC00016878-02
s-734118
CHEMBL349803
s-73-4118
tauliz-d4
HMS1571A16
HMS2098A16
tox21_110661
dtxcid703488
dtxsid2023488 ,
HMS2230G15
FT-0673944
piretanido
acide phenoxy-4-(1-pyrrolidinyl)-3-sulfamoyl-5 benzoique
piretanide [usan:inn:ban:jan]
dq6kk6gv93 ,
unii-dq6kk6gv93
piretanidum
AKOS015895445
piretanide [mart.]
piretanide [ep monograph]
4-phenoxy-3-(pyrrolidinyl)-5-sulfamoylbenzoic acid
piretanide [inn]
piretanide [usan]
piretanide [who-dd]
piretanide [mi]
piretanide [jan]
HMS3372O22
gtpl4742
CCG-221047
SCHEMBL49473
NCGC00016878-04
tox21_110661_1
UJEWTUDSLQGTOA-UHFFFAOYSA-N
3-(1-pyrrolidinyl)-4-phenoxy-5-sulphamylbenzoic acid
4-phenoxy-3-(1-pyrrolidinyl)-5-sulphamoylbenzoic acid
W-105543
SR-01000838837-2
sr-01000838837
CHEBI:32015
HMS3715A16
F2173-0688
Q3905617
2-methyl-2-propylpropane-1,3-diyl dicarbamate
A924106
MS-25753
HY-119816
piretanide for system suitability
EN300-18568088
CS-0078068

Research Excerpts

Overview

Piretanide is a high-ceiling, loop-active diuretic that has been developed for treatment of congestive heart failure, hypertension and edematous states caused by renal and hepatic diseases. It is structurally related to bumetanide and furosemide.

ExcerptReferenceRelevance
"Piretanide is a high-ceiling, loop-active diuretic that has been developed for treatment of congestive heart failure, hypertension and edematous states caused by renal and hepatic diseases. "( Piretanide: a loop-active diuretic. Pharmacology, therapeutic efficacy and adverse effects.
Marsh, JD; Smith, TW,
)
3.02
"Piretanide is a new diuretic agent that is structurally related to bumetanide and furosemide. "( [Clinical comparative trial of piretanide and furosemide in patients with advanced renal insufficiency. Drug levels and diuretic potency of single oral doses].
Fink, R; Heuer, LJ; Machnik, H; Studt, J, 1983
)
1.99
"Piretanide is a new loop diuretic similar to furosemide in pharmacologic properties and approximately six times as potent. "( Effects of piretanide in normal subjects.
Anderson, S; Baird, B; Brater, DC; Kaojarern, S, 1983
)
2.1
"Piretanide is a potent diuretic and treated patients should be monitored for hypokalemia."( Piretanide (HOE 118) in dogs.
Lumb, WV; Scott, RJ; Seegmiller, J, 1982
)
2.43
"1. Piretanide is a new loop diuretic resembling furosemide. "( Piretanide and urinary excretion of ions in rat. Effect of indomethacin.
Gauthier, C; Nguyen-Simonnet, H; Pellet, M, 1981
)
2.33
"Piretanide is a potent 'loop' diuretic whose principal site of action is in the thick ascending limb of the loop of Henle. "( Piretanide. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Brogden, RN; Clissold, SP, 1985
)
3.15

Effects

Piretanide has no effect on photophosphorylation catalyzed by phenazine methosulfate or on Ca2+-dependent ATPase activity of isolated chloroplast coupling factor (CF1)

ExcerptReferenceRelevance
"Thus piretanide SR 6 mg has a mild effect on the number of mictions; it should not alter patients' well-being."( [Comparative study, using a placebo, of the frequency of micturition after repeated administration of piretanide SR 6 mg/day (Eurelix) to healthy volunteers].
Chassard, D; Derobert, E; Genthon, R; Kabir, M; Lendresse, P,
)
0.8
"Piretanide has no effect on photophosphorylation catalyzed by phenazine methosulfate or on Ca2+-dependent ATPase activity of isolated chloroplast coupling factor (CF1)."( Chloride ion transport and its inhibition in thylakoid membranes.
Schechter, S; Vambutas, V, 1983
)
0.99
"Thus piretanide SR 6 mg has a mild effect on the number of mictions; it should not alter patients' well-being."( [Comparative study, using a placebo, of the frequency of micturition after repeated administration of piretanide SR 6 mg/day (Eurelix) to healthy volunteers].
Chassard, D; Derobert, E; Genthon, R; Kabir, M; Lendresse, P,
)
0.8

Actions

ExcerptReferenceRelevance
"Piretanide does not cause lysis of fibrin in vitro in any concentration."( Piretanide: a new synthetic fibrinolytic and anti-platelet agent.
Chohan, IS, 1986
)
2.44

Toxicity

ExcerptReferenceRelevance
" The method is based on the determination of the toxic dose (TD50) which causes a defined hearing loss in 50% of the animals tested."( Quantitative evaluation of ototoxic side effects of furosemide, piretanide, bumetanide, azosemide and ozolinone in the cat--a new approach to the problem of ototoxicity.
Göttl, KH; Klinke, R; Roesch, A, 1985
)
0.51
" Adverse effects reported to date are limited to those attributable to excess loss of fluid and electrolytes."( Piretanide: a loop-active diuretic. Pharmacology, therapeutic efficacy and adverse effects.
Marsh, JD; Smith, TW,
)
1.57

Pharmacokinetics

Three doses (3 mg, 6 mg and 12 mg) of piretanide, a new high ceiling diuretic, and placebo were given to 8 volunteers to investigate the relationship between the pharmacodynamic parameters, the dose and urinary excretion.

ExcerptReferenceRelevance
" Mean peak concentration of triamterene was increased in the elderly patients compared with the data of young healthy volunteers."( Pharmacokinetics of triamterene in geriatric patients--influence of piretanide and hydrochlorothiazide.
Jung, R; Mühlberg, W; Mutschler, E; Platt, D; Spahn, H, 1989
)
0.51
"Hydroxy propyl cellulose (HPC)-ethyl cellulose (EC) microcapsules containing piretanide were newly by a solvent evaporation technique and their slow-release properties were evaluated on dissolution properties in vitro and pharmacokinetic and pharmacodynamic parameters in beagle dogs."( Preparation and pharmacokinetic and pharmacodynamic evaluation of hydroxy propyl cellulose-ethyl cellulose microcapsules containing piretanide.
Goto, S; Kawata, M; Suzuki, N; Tsujiyama, T; Uchida, T, 1989
)
0.71
" A pharmacokinetic and pharmacodynamic link model which was developed in the previous paper was applied to the present experimental results."( Pharmacokinetic and pharmacodynamic studies of piretanide in rabbits. IV. Effect of piretanide on the proximal tubules and the loop of Henle under a hydrated condition.
Kakemi, M; Koizumi, T; Lu, W, 1988
)
0.53
" Pharmacokinetic data showed rapid and almost complete absorption (bioavailability 92%) and a rapid elimination with renal clearance of 50% of the total 200 ml/min in the normals and renal clearance of about 50% of actual GFR in the patients."( Pharmacokinetic-pharmacodynamic relationship of piretanide in healthy and uremic subjects. Determinants of the diuretic effect of a loop diuretic.
Beermann, B; Odlind, B; Sjöström, P, 1987
)
0.53
" In spite of the similarities in the pharmacokinetic properties, the pharmacologic effects of piretanide were influenced considerably by the hydrated conditions of the body."( Pharmacokinetic and pharmacodynamic studies of piretanide in rabbits. I. Effect of different hydrated conditions.
Endoh, M; Kakemi, M; Katayama, K; Koizumi, T; Lu, W, 1987
)
0.75
"A sustained-release property of gelatin microcapsules of piretanide was evaluated by pharmacodynamic parameters."( Pharmacokinetic and pharmacodynamic evaluation of gelatin microcapsule containing piretanide in beagle dogs.
Goto, S; Kawata, M; Suzuki, N; Tsujiyama, T, 1986
)
0.74
" Tmax after relief of ascites was similar to that seen for normal volunteers."( The influence of ascites on the pharmacokinetics of piretanide in cirrhotic patients.
Bouchier, IA; Shepherd, AN, 1985
)
0.52
"Three doses (3 mg, 6 mg and 12 mg) of piretanide, a new high ceiling diuretic, and placebo were given to 8 volunteers to investigate the relationship between the pharmacodynamic parameters, the dose and its urinary excretion."( Pharmacodynamics and urine pharmacokinetics of three doses of piretanide.
Dagrosa, EE; Grigoleit, HG; Meyer, BH; Müller, FO, 1983
)
0.78
" No other pharmacokinetic parameter was affected."( Pharmacokinetics and pharmacodynamics of ramipril and piretanide administered alone and in combination.
de la Rey, N; Gera, S; Jähnchen, E; Löffler, K; Luus, HG; Ruf, G; Schulz, W; Trenk, D, 1994
)
0.54
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" The purpose of the present study was to examine whether long-term therapy with ramipril (RA, and ACE inhibitor) would lower blood pressure more effectively and without adverse reactions in combination with the loop diuretics piretanide (PI) or furosemide (FU)."( Loop diuretics combined with an ACE inhibitor for treatment of hypertension: a study with furosemide, piretanide, and ramipril in spontaneously hypertensive rats.
Baldes, L; Becker, RH; Treudler, M, 1989
)
0.68

Bioavailability

Pretreatment with probenecid produced significant increases in absolute peak and plasma diuretic concentrations, t1/2 and mean residence time. The bioavailability of piretanide was unaffected by combination with penbutolol.

ExcerptReferenceRelevance
" Pretreatment with probenecid produced significant increases in absolute peak and plasma diuretic concentrations, t1/2 and mean residence time while decreasing steady-state volume of distribution, total clearance, renal clearance and fraction of unchanged drug excreted without affecting the bioavailability of piretanide."( Renal responses and pharmacokinetics of piretanide in humans: effect of route of administration, state of hydration and probenecid pretreatment.
Dixey, JJ; Lant, AF; McNabb, WR; Noormohamed, FH, 1990
)
0.72
" Thus the bioavailability of piretanide was unaffected by combination with penbutolol."( Kinetics of piretanide tablets, penbutolol tablets and the fixed combination of both drugs in healthy male subjects after a single oral dose.
Grigoleit, HG; Meyer, B; Müller, F, 1987
)
0.94
"In a recent report, it was shown that the loop diuretic piretanide is rapidly absorbed after placement of a piretanide solution in the duodenum, while the rate of absorption is definitely slower when the drug is instilled into the ascending colon (5)."( Kinetics of piretanide absorption from the gastrointestinal tract.
Brockmeier, D; Grigoleit, HG; Heptner, H; Meyer, BH, 1986
)
0.9
"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

Piretanide is of comparable antihypertensive efficacy as hydrochlorothiazide 50 to 100 mg/day, but has significantly less effect on serum potassium levels. No differences between the dose-response curves of furosemide, bumetanide, or pireTanide could be demonstrated.

ExcerptRelevanceReference
" In a dosage of 2 to 3 mg, it induced an increase in sodium excretion of almost 13% of filtered load, and there was an associated 2- to 3-fold increase in potassium excretion."( Acute effects of piretanide in normal subjects.
Puschett, JB; Teredesai, P, 1979
)
0.6
" dosage of 6 mg piretanide."( Rapid assay for the quantification of piretanide in biological fluids.
Hahn, G; Mutschler, E; Spahn-Langguth, H, 1991
)
0.9
"01); these differences caused by fluid replacement did not however occur after oral dosing of piretanide (181 +/- 12 vs 167 +/- 14 mmol 6 h-1)."( Analysis of the natriuretic action of a loop diuretic, piretanide, in man.
Lant, AF; Noormohamed, FH, 1991
)
0.75
" HPC-EC10 (5:3) microcapsules containing piretanide were satisfactory as a sustained-release preparation in the light of the anti hypertensive effect even at a half frequency of daily dosing of the solution."( Pharmacological evaluation of hydroxypropylcellulose-ethylcellulose microcapsules containing piretanide.
Goto, S; Kawata, M; Kuriki, T; Suzuki, N; Tsujiyama, T, 1990
)
0.76
" dosing in the nonhydrated state where changes in drug excretion after probenecid (2."( Renal responses and pharmacokinetics of piretanide in humans: effect of route of administration, state of hydration and probenecid pretreatment.
Dixey, JJ; Lant, AF; McNabb, WR; Noormohamed, FH, 1990
)
0.55
" Thus, combined treatment with low doses of loop diuretics and ACE inhibitors that permit partial recovery of serum ACE activity during the 24 h after dosing synergistically lowers blood pressure without adverse reactions associated with larger doses of either therapy alone."( Loop diuretics combined with an ACE inhibitor for treatment of hypertension: a study with furosemide, piretanide, and ramipril in spontaneously hypertensive rats.
Baldes, L; Becker, RH; Treudler, M, 1989
)
0.49
" A dosage of 2 x 6 mg day-1 to 2 x 12 mg day-1 of intravenous piretanide for 7 days was sufficient to abrogate most symptoms of cardiac insufficiency."( Efficacy and pharmacokinetics of piretanide in patients with congestive heart failure.
Frey, F; Lahn, W; Marone, C; Rivera, B; Zwahlen, H, 1989
)
0.8
" Overall, five patients were withdrawn due to increased diuresis: two patients on each dosage of piretanide and one receiving bendroflumethiazide."( Comparison of slow-release piretanide and bendroflumethiazide in the treatment of mild to moderate hypertension.
Hegbrant, J; Månsby, J; Skogström, K,
)
0.65
"Eight patients with chronic heart failure classified as NYHA class II to III (group 1) and nine patients with acute decompensated heart failure classified as NYHA class IV (group 2) were treated with piretanide at a dosage of 12 mg administered intravenously."( [Piretanide in chronic and acute decompensated heart failure. Effect on hemodynamics and vasoactive hormones].
Hopf, R; Kaltenbach, M; Kirsten, R; Nelson, K; Pooth, R; Sievert, H; Vens-Cappell, F, 1989
)
1.38
" In patients not responding to this dosage regimen at the end of a 4-week treatment period, the dose was doubled."( A multi-centre comparative study between ramipril and enalapril in patients with mild to moderate essential hypertension.
Akbary, MA; Rangoonwala, B; Rosenfeld, J; Schinzel, S; Zabludowski, J, 1988
)
0.27
" In comparative studies, the piretanide dose-response curve was found to be parallel to that of frusemide over the dose range studied."( Acute and long-term renal and metabolic effects of piretanide in congestive cardiac failure.
Lant, AF; McNabb, WR; Noormohamed, FH, 1988
)
0.82
" Eumagnesaemia and eupotassaemia were preserved at all dosage of the piretanide monosubstance."( Lack of effect of piretanide (a potassium-stable diuretic) on serum magnesium.
de Looze, S; Irmisch, R; Rangoonwala, B; Verho, M, 1987
)
0.84
" Piretanide (n = 20) administered orally in a daily dosage of up to 24 mg was compared with placebo (n = 18) for 28 days, using a double-blind, randomized, parallel design."( Piretanide, a potent diuretic with potassium-sparing properties, for the treatment of congestive heart failure.
Baumgardner, S; Chardo, F; Charuzi, Y; Kim, CS; Liang, CS; Sherman, LG, 1986
)
2.62
" The rapid extrarenal elimination reduces the risk of accumulation in renal patients but also reduces the active fraction of the dosage being cleared by the kidneys."( Pharmacokinetic-pharmacodynamic relationship of piretanide in healthy and uremic subjects. Determinants of the diuretic effect of a loop diuretic.
Beermann, B; Odlind, B; Sjöström, P, 1987
)
0.53
" Comparative trials of up to 3 months duration indicate that at this dosage piretanide is of comparable antihypertensive efficacy as hydrochlorothiazide 50 to 100 mg/day, but has significantly less effect on serum potassium levels."( Piretanide. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.
Brogden, RN; Clissold, SP, 1985
)
1.94
" Piretanide and furosemide both induced a short-term increase in plasma renin activity with a maximum about 4 hours after dosing which returned to initial levels after approximately 12 hours regardless of whether a single or twice daily dose had been given."( The effects of piretanide on catecholamine metabolism, plasma renin activity and plasma aldosterone: a double-blind study versus furosemide in healthy volunteers.
Heintz, B; Kirsten, R; Nelson, K; Verho, M, 1985
)
1.53
" Because the diuretic effect of piretanide depends on the concentration of the drug in the tubule, the observed correlation might be of use in evaluating the appropriate dosage of piretanide in patients with renal failure."( Pharmacokinetics of the loop diuretic piretanide in renal failure.
Heidland, A; Heptner, W; Lahn, W; Röckel, A; Walter, U, 1985
)
0.82
" If diastolic pressure was normalized (less than 95 mmHg), this dosage was continued for a further 6 weeks; patients whose blood pressure remained high after the initial 6 weeks received 1 capsule twice daily for a further 6 weeks."( The effects of piretanide capsules on blood pressure during ergometric and isometric work loads in patients with mild to moderate essential hypertension.
Maass, L; Meywald, W; Rangoonwala, B; Verho, M, 1985
)
0.62
" The results showed that although all three groups had significant reductions in systolic and diastolic blood pressures, both at rest and standing, compared with initial levels, the decrease was significantly greater in the two higher dosage groups."( A double-blind study of piretanide in the treatment of hypertension.
Dols, W; Freude, J; Rangoonwala, B; Verho, M, 1983
)
0.57
" A clear dose-response relationship was found for cumulative urinary output, cumulative excretion of Na+ and K+, clearance of Na+ and K+ and the urinary sodium/potassium ratio."( Pharmacodynamics and urine pharmacokinetics of three doses of piretanide.
Dagrosa, EE; Grigoleit, HG; Meyer, BH; Müller, FO, 1983
)
0.51
" No differences between the dose-response curves of furosemide, bumetanide, or piretanide could be demonstrated."( Effect of diuretics on the tubuloglomerular feedback response.
Brunkhorst, R; Franke, H; Gutsche, HU; Müller-Ott, K; Niedermayer, W, 1984
)
0.5
" In a randomized, single-blind dose-response study, each subject performed an UNW test immediately after nebulization of different doses of piretanide between 12 and 48 mg or placebo."( Protective effect of inhaled piretanide on the bronchial obstructive response to ultrasonically nebulized H2O. A dose-response study.
Bianco, S; Pieroni, MG; Robuschi, M; Sestini, P; Vaghi, A, 1993
)
0.78
" The three proposed methods were successfully applied for the determination of piretanide in bulk powder, laboratory-prepared mixtures and pharmaceutical dosage form with good accuracy and precision."( Stability-indicating methods for the determination of piretanide in presence of the alkaline induced degradates.
Youssef, NF, 2005
)
0.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[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 (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency12.58930.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency4.46685.623417.292931.6228AID485281
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.47310.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency15.84890.031637.5844354.8130AID504865
GLI family zinc finger 3Homo sapiens (human)Potency17.23250.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency10.05510.000221.22318,912.5098AID743040; AID743042; AID743054
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency8.91250.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency1.00000.00137.762544.6684AID914; AID915
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency8.92800.000214.376460.0339AID720691; AID720719
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency37.57510.001024.504861.6448AID743215
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency17.78280.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency10.12350.001723.839378.1014AID743083
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency14.12540.001815.663839.8107AID894
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency7.94330.65619.452025.1189AID927
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency12.58930.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency0.00400.891312.067628.1838AID1487
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency7.94331.584913.004325.1189AID927
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)790.60000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (61)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

Assay IDTitleYearJournalArticle
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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]
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.
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.
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]
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
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]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID59305Natriuretic potency was evaluated as oral dose required to produce an excretion of 2 mequiv of Na+/Kg of dog body weight, ED5 value based on N=2 dogs/dose1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
[(Aminomethyl)aryloxy]acetic acid esters. A new class of high-ceiling diuretics. 4. Substituted 6,7-dichloro-2,3-dihydrobenzofurans derived by ring annelation.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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]
AID173783Natriuretic potency was evaluated as oral dose required to produce an excretion of 2 mequiv of Na+/Kg of rat body weight, ED2 value based on N=4 rats/dose1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
[(Aminomethyl)aryloxy]acetic acid esters. A new class of high-ceiling diuretics. 4. Substituted 6,7-dichloro-2,3-dihydrobenzofurans derived by ring annelation.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
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]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1346941Human Basolateral Na-K-Cl symporter (SLC12 family of cation-coupled chloride transporters)2002Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 365, Issue:3
Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
AID1346968Human Kidney-specific Na-K-Cl symporter (SLC12 family of cation-coupled chloride transporters)2002Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 365, Issue:3
Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (240)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990162 (67.50)18.7374
1990's50 (20.83)18.2507
2000's9 (3.75)29.6817
2010's13 (5.42)24.3611
2020's6 (2.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.33

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

MetricThis Compound (vs All)
Research Demand Index32.33 (24.57)
Research Supply Index5.73 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index47.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials56 (22.22%)5.53%
Reviews10 (3.97%)6.00%
Case Studies1 (0.40%)4.05%
Observational0 (0.00%)0.25%
Other185 (73.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]