Page last updated: 2024-11-04

bendroflumethiazide

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Description

Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2315
CHEMBL ID1684
CHEBI ID3013
SCHEMBL ID26016
MeSH IDM0002310

Synonyms (210)

Synonym
3-benzyl-6-(trifluoromethyl)-3,4-dihydro-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
bendroflumetiazida
bendroflumethiazidum
chebi:3013 ,
MLS001076062
BRD-A80017228-001-05-9
smr000058802
KBIO1_000274
DIVK1C_000274
3-(phenylmethyl)-6-(trifluoromethyl)-3,4-dihydro-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
flumesil
relan beta
bhft
benzylhydroflumethiazide
hsdb 3293
livesan
6-trifluoromethyl-3-benzyl-7-sulfamyl-3,4-dihydro-1,2,4-benzothiadiazine, 1,1-dioxide
2h-1,2,4-benzothiadiazine-7-sulfonamide, 3,4-dihydro-3-(phenylmethyl)-6-(trifluoromethyl)-, 1,1-dioxide
2h-1,2,4-benzothiadiazine-7-sulfonamide, 3-benzyl-3,4-dihydro-6-(trifluoromethyl)-, 1,1-dioxide
bentride
centyl
salural
be 724-a
aprinox
3-benzyl-3,4-dihydro-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
benzylrodiuran
rauzide
plusuril
naturetin-10
brn 0373316
pluryle
bl h368
neo-rontyl
berkozide
benuron
intolex
neo-naclex
2h-1,2,4-benzothiadiazine-7-sulfonamide, 3-benzyl-3,4-dihydro-6-(trifluoromethyl)-,1,1-dioxide
naturetin-5
sinesalin
bendroflumethiazidum [inn-latin]
salures
2h-1,2,4-benzothiadiazine-7-sulfonamide, 3,4-dihydro-3-(phenylmethyl)-6-(trifluoromethyl)-, 1,1-dioxide, (+-)-
rautrax n
bendroflumetiazida [inn-spanish]
(+-)-3-benzyl-3,4-dihydro-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
niagaril
poliuron
3-benzyl-6-trifluoromethyl-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine, 1,1-dioxide
pluryl
naturetin-2.5
nikion
urlea
thiazidico
orsile
einecs 200-800-1
sodiuretic
repicin
bristuric
bristuron
ft 81
naturetin
bendroflumetiazide [dcit]
SPECTRUM_001386
PRESTWICK_992
bendrofumethiazide
cas-73-48-3
NCGC00016312-01
BSPBIO_000888
PRESTWICK2_000784
BSPBIO_003036
BPBIO1_000978
EU-0009291
AB00052315
bendroflumethiazide
C07758
73-48-3
UNM000000601501
DB00436
benzhydroflumethiazide
6-trifluoromethyl-3-benzyl-7-sulfamyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide
+/--3-benzyl-3,4-dihydro-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
3,4-dihydro-3-(phenylmethyl)-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
bendroflumethiazide (jan/usp/inn)
naturetin (tn)
D00650
NCGC00089729-03
NCGC00089729-02
bendrofluazide
MLS000028558 ,
KBIO2_007002
KBIO2_001866
KBIO2_004434
KBIOGR_001188
KBIOSS_001866
KBIO3_002536
NINDS_000274
PRESTWICK0_000784
SPBIO_001308
PRESTWICK1_000784
SPBIO_002827
SPECTRUM3_001558
SPECTRUM4_000774
SPECTRUM2_001524
SPECTRUM1503104
IDI1_000274
SPECTRUM5_001016
PRESTWICK3_000784
HMS2092J16
HMS500N16
FT-0662520
FT-0662519
HMS1922E15
HMS1570M10
benzydroflumethiazide
CHEMBL1684
nsc-758229
NCGC00018194-03
NCGC00018194-04
NCGC00018194-02
HMS2097M10
HMS3259D17
naturine
nsc 758229
4-27-00-08041 (beilstein handbook reference)
5q52x6icji ,
bendroflumetiazide
unii-5q52x6icji
bendroflumethiazide [usp:inn:ban:jan]
pharmakon1600-01503104
MLS002548857
nsc758229
dtxsid5022647 ,
tox21_110365
dtxcid402647
nateretin
bendroflumethazide
naigaril
benzy-rodiuran
flumersil
HMS2230G10
CCG-39302
gtpl7122
3-benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2h-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
HMS3370I20
(+/-)-3-benzyl-3,4-dihydro-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
bendroflumethiazide [mart.]
bendroflumethiazide [who-dd]
bendroflumethiazide [orange book]
2h-1,2,4-benzothiadiazine-7-sulfonamide, 3,4-dihydro-3-(phenylmethyl)-6-(trifluoromethyl)-, 1,1-dioxide, (+/-)-
bendroflumethiazide [vandf]
bendroflumethiazide [usp-rs]
bendroflumethiazide [jan]
bendroflumethiazide [mi]
corzide component bendroflumethiazide
bendroflumethiazide [hsdb]
bendroflumethiazide [ep impurity]
bendroflumethiazide component of corzide
bendroflumethiazide [inn]
bendroflumethiazide [ep monograph]
bendroflumethiazide [usp monograph]
NC00664
SCHEMBL26016
tox21_110365_1
NCGC00018194-08
HS-0095
AKOS024255718
bendroflumethiazide, british pharmacopoeia (bp) reference standard
3-benzyl-6-(trifluoromethyl)-3,4-dihydro-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide #
relan .beta.
3-benzyl-6-trifluoromethyl-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide
(.+/-.)-bendroflumethiazide
neonaclex
AB00052315_15
OPERA_ID_1043
AB00052315_16
3-benzyl-6-trifluoromethyl-7-sulfamoyl-3,4-dihydro-2h-1,2,4-benzothiadiazine 1,1-dioxide
bendroflumethiazide, analytical standard
bendroflumethiazide, european pharmacopoeia (ep) reference standard
sr-01000000103
SR-01000000103-2
bendroflumethiazide, united states pharmacopeia (usp) reference standard
SR-01000000103-4
SBI-0051772.P002
HMS3714M10
3-benzyl-6-(trifluoromethyl)-3,4-dihydro-2h-benzo[e][1,2,4]thiadiazine-7-sulfonamide 1,1-dioxide
SW028069-4
3-benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2h-1lambda6,2,4-benzothiadiazine-7-sulfonamide
BCP24525
FT-0662518
Q1169164
BRD-A80017228-001-15-8
3-benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2h-1,2,4- benzothiadiazine-7-sulfonamide
mfcd00078963
3,4-dihydro-3-(phenylmethyl)-6-(trifluoromethyl)-2h-1,2,4-benzothiadiazine-7-sulfonamide-1,1-dioxide
A851258
HY-B1363
CS-0013104
bendroflumethiazide (usp:inn:ban:jan)
bendroflumethiazid
bendroflumethiazidum (inn-latin)
relan
bendroflumethiazide (mart.)
bendroflumethiazide (usp monograph)
c03aa01
bendroflumetiazida (inn-spanish)
bendroflumethiazide (ep monograph)
bendroflumethiazide (ep impurity)
bendroflumethiazide (usp-rs)
Z1575277625

Research Excerpts

Treatment

Treatment with bendroflumethiazide (2.5 mg, twice daily with potassium supplements) in 63 patients with calcium-containing renal stones for a minimum period of 1 year increased the serum urate values in all patients with an average of 90 mumol./l.

ExcerptReferenceRelevance
"Treatment with bendroflumethiazide (2.5 mg, twice daily with potassium supplements) in 63 patients with calcium-containing renal stones for a minimum period of 1 year (average duration of treatment 2.6 years) increased the serum urate values in all patients with an average of 90 mumol./l. "( Effects of bendroflumethiazide on urate metabolism during treatment of patients with renal stones.
Backman, U; Danielson, BG; Fellström, B; Johansson, G; Ljunghall, S; Odlind, B; Wikström, B, 1982
)
1.01
"Treatment with bendroflumethiazide was associated with a 10% reduction in the stimulated whole saliva secretion rate and a 15% reduction in the salivary sodium concentration, as compared with placebo."( Oral mucosal friction and subjective perception of dry mouth in relation to salivary secretion.
Axéll, T; Dahlöf, C; Henricsson, V; Nederfors, T, 1993
)
0.63

Toxicity

ExcerptReferenceRelevance
" Effects on systolic blood pressure, heart rate, biochemical variables, adverse events and quality of life were studied as secondary efficacy parameters."( Efficacy and safety of 24 weeks of therapy with bendroflumethiazide 1.25 mg/day or 2.5 mg/day and potassium chloride compared with enalapril 10 mg/day and amlodipine 5 mg/day in patients with mild to moderate primary hypertension : a multicentre, randomis
Borrild, N; Rasmussen, S; Vang Andersen, J, 2006
)
0.59
" The incidences of adverse events were similar in the low-dose bendroflumethiazide groups, with significantly higher incidences in the enalapril and amlodipine groups."( Efficacy and safety of 24 weeks of therapy with bendroflumethiazide 1.25 mg/day or 2.5 mg/day and potassium chloride compared with enalapril 10 mg/day and amlodipine 5 mg/day in patients with mild to moderate primary hypertension : a multicentre, randomis
Borrild, N; Rasmussen, S; Vang Andersen, J, 2006
)
0.83
" This report describes profound bradycardia as a late consequence of chronic lithium poisoning, and reminds us to consider the possibility of delayed toxic effects, even in situations where serum lithium concentrations appear to be declining."( Delayed cardiotoxicity in chronic lithium poisoning: discrepancy between serum lithium concentrations and clinical status.
Waring, WS, 2007
)
0.34

Pharmacokinetics

ExcerptReferenceRelevance
" Chronic treatment did not consistently change the kinetics except for a slight prolongation of terminal half-life of non-protein-bound captopril."( Pharmacokinetics of captopril and its effects on blood pressure during acute and chronic administration and in relation to food intake.
Kågedal, B; Karlberg, BE; Larsson, R; Ohman, KP, 1985
)
0.27
" A 2-compartment model was taken as the basis for the calculation of the steady-state plasma concentration curves and the pharmacokinetic parameters of Bft, canrenone and the sum of the fluorogenic spironolactone metabolites."( [Pharmacokinetic studies and bioavailability of bendroflumethiazide in combination with spironolactone].
Nuss, U; Strobel, K; Vergin, H, 1986
)
0.53
" 6 There was no significant difference in plasma propranolol levels, Cmax propranolol or AUCo-x following the three preparations."( Comparative pharmacological and pharmacokinetic observations on propranolol (long acting formulation) and bendrofluazide administered separately and concurrently to volunteers.
Barker, NP; Castle, WM; Harron, DW; McAinsh, J; Nicholls, DP; Shanks, RG, 1982
)
0.26

Bioavailability

ExcerptReferenceRelevance
" As judged by AUC and urinary recovery of BFT, the bioavailability of the diuretic was not influenced by concomitant intake of a meal."( Effect of food on the bioavailability of bendroflumethiazide.
Beermann, B; Groschinsky-Grind, M; Lindström, B, 1978
)
0.52
"An intraindividual comparative multiple-dose study (6 days) was carried out under controlled conditions on 10 healthy volunteers in order to establish the bioavailability of bendroflumethiazide (Bft; 3-benzyl-6-trifluoromethyl-7-sulfamyl-3,4-dihydro-1,2,4-benzoth iad iazine-1, 1-oxide), the sum of the fluorogenic metabolites of spironolactone (3-[3-oxo-7-alpha-acetylthio-17 beta-hydroxy-4-androstene-17-alpha-yl]-propionic acid-gamma-lactone) and canrenone, the main spironolactone metabolite from a fixed combination of Bft with spironolactone vs."( [Pharmacokinetic studies and bioavailability of bendroflumethiazide in combination with spironolactone].
Nuss, U; Strobel, K; Vergin, H, 1986
)
0.72
" Bioavailability of Bft was not altered following administration of the fixed combination."( Pharmacokinetics of bendroflumethiazide alone and in combination with propranolol and hydralazine.
Mutschler, E; Schäfer-Korting, M, 1982
)
0.59
"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

We performed a meta-analysis to characterize the dose-response relationships for 3 commonly prescribed thiazide diuretics. Overall, five patients were withdrawn due to increased diuresis: two patients on each dosage of piretanide and one receiving bendroflumethiazide.

ExcerptRelevanceReference
" Both timolol and acebutolol had a significant hypotensive effect at 24 hours and a low incidence of side effects, suggesting that further increases in dosage might be effective and well tolerated."( Randomised study of six beta-blockers and a thiazide diuretic in essential hypertension.
Wilcox, RG, 1978
)
0.26
" In the dosage used, hydrallazine affected only the diastolic blood pressure, and when added to either bendrofluazide or bendrofluazide plus atenolol it produced a further mean reduction in pressure of 6 mm Hg."( Contribution of atenolol, bendrofluazide, and hydrallazine to management of severe hypertension.
Mitchell, JR; Wilcox, RG, 1977
)
0.26
" However, variability of plasma potassium within the dose interval was not increased markedly, and 12 hourly dosing is probably satisfactory for both potassium chloride and spironolactone at the doses studied."( Adequacy of twice daily dosing with potassium chloride and spironolactone in thiazide treated hypertensive patients.
Brawn, LA; Ramsay, LE; Toner, JM; Yeo, WW, 1991
)
0.28
" After at least 6 months of treatment, the mean daily dosage of indoramin was higher among patients who received indoramin alone (122 mg/day) than among those who received indoramin plus a diuretic (92 mg/day)."( Antihypertensive therapy with indoramin in the elderly.
Allen, IE; Deitch, MW; Pascucci, VL, 1986
)
0.27
" 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,
)
0.6
"Pharmacokinetics of bendroflumethiazide (bft) were investigated in blood and skin suction blister fluid (SBF) in rats dosed 10 mg/kg intravenously."( Skin blister fluid--an access to the peripheral compartment. Implications of a study on the behaviour of bendroflumethiazide in rats.
Schäfer-Korting, M, 1985
)
0.81
" All patients were then given a combination of half the initial dosage of both drugs for an additional period of 6 weeks."( Controlled trial of nifedipine and bendroflumethiazide in hypertension.
Andrén, L; Hallin, L; Hansson, L,
)
0.41
" If patients failed to respond adequately at this dosage level, prazosin (0."( Timolol/bendrofluazide combination ('Prestim') in the treatment of poorly controlled hypertensive patients in general practice.
Douglas-Jones, AP, 1984
)
0.27
" 4 The results suggest that the duration of antihypertensive effect of methyldopa is long enough to permit twice daily dosing, but that single daily dosing cannot be recommended for most patients."( Duration of effect of single daily dose methyldopa therapy.
Dollery, CT; Orozco-Gonzalez, M; Polak, G; Wright, JM, 1982
)
0.26
"6%) patients who required a dosage reduction and 2 (0."( A multi-centre general practice study on the use of a timolol/bendrofluazide combination ('Prestim') in the management of hypertension: preliminary report.
Head, AC; Langrick, AF, 1981
)
0.26
" In a smaller study potassium chloride induced a significant log dose-response on plasma potassium, but the effect was small in absolute terms."( Amiloride, spironolactone, and potassium chloride in thiazide-treated hypertensive patients.
Fraser, R; Hettiarachchi, J; Morton, JJ; Ramsay, LE, 1980
)
0.26
"The effect of conventional propranolol and bendrofluazide tablets given twice daily has been compared with an equivalent dosage combined in a single capsule given twice daily in fourteen patients with essential hypertension."( Treatment of essential hypertension with a combination of propranolol and bendrofluazide.
Dawes, PM; Solomon, LR, 1980
)
0.26
" In a complementary investigation, 14 patients who completed the 16-weeks' treatment were changed onto a regimen in which the drug dosage remained unchanged but was taken on a once-daily basis for a further 16 weeks to assess the efficacy of once-daily dosing and to monitor any further long-term changes in biochemistry."( A hospital out-patient study of timolol/bendrofluazide combination ('Prestim') in essential hypertension.
Kubik, MM, 1980
)
0.26
" These complications may be mitigated with careful monitoring, dosage adjustment, and replacement of electrolyte losses."( Diuretic complications.
Greenberg, A, 2000
)
0.31
" Bendrofluazide appears to be an ineffective hypotensive agent at the standard dosage in the initial post-stroke period."( Bendrofluazide fails to reduce elevated blood pressure levels in the immediate post-stroke period.
Eames, PJ; Panerai, RB; Potter, JF; Robinson, TG, 2005
)
0.33
" Least square means (95% CI) of all observations during the first 6 h after dosing showed that diclofenac caused a reduction in GFR from 71 (64-78) to 59 (52-66) ml/min."( Cyclooxygenase inhibition causes marked impairment of renal function in elderly subjects treated with diuretics and ACE-inhibitors.
Björkman, S; Höglund, P; Juhlin, T, 2005
)
0.33
"5 mg; n=22), captopril (50 mg twice daily; n=22) or a capsule containing each of the 4 above at one-quarter dosage (n=22) in a parallel group design for 4 weeks."( Low-dose quadruple antihypertensive combination: more efficacious than individual agents--a preliminary report.
Feely, J; Mahmud, A, 2007
)
0.34
" We performed a meta-analysis to characterize the dose-response relationships for 3 commonly prescribed thiazide diuretics, hydrochlorothiazide, chlorthalidone, and bendroflumethiazide, on BP, serum potassium, and urate."( Meta-analysis of dose-response relationships for hydrochlorothiazide, chlorthalidone, and bendroflumethiazide on blood pressure, serum potassium, and urate.
Chaturvedi, N; Hardy, R; Hughes, AD; Peterzan, MA, 2012
)
0.8
" This could be due to limitations in the connectivity mapping, such as implausible dosage requirements, or the pharmacoepidemiology, such as residual confounding."( A combined connectivity mapping and pharmacoepidemiology approach to identify existing medications with breast cancer causing or preventing properties.
Busby, J; Cardwell, CR; Liberante, F; Mills, K; Murray, L; Zhang, SD, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
diureticAn agent that promotes the excretion of urine through its effects on kidney function.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
benzothiadiazineHeterocyclic compound of a ring with sulfur and two nitrogen atoms fused to a benzene ring. Members inhibit sodium-potassium-chloride symporters and are used as diuretics.
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
Bendroflumethiazide Action Pathway319

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.62280.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency25.60180.002541.796015,848.9004AID1347395; AID1347398
glp-1 receptor, partialHomo sapiens (human)Potency17.78280.01846.806014.1254AID624172
RAR-related orphan receptor gammaMus musculus (house mouse)Potency18.83360.006038.004119,952.5996AID1159521
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency44.66840.011212.4002100.0000AID1030
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency33.48890.001024.504861.6448AID743215
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.07950.01789.637444.6684AID588834
DNA polymerase kappa isoform 1Homo sapiens (human)Potency10.00000.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency39.81070.031610.279239.8107AID884; AID885
lamin isoform A-delta10Homo sapiens (human)Potency0.50120.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
GABA theta subunitRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency39.81071.000012.224831.6228AID885
[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)69.55000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (40)

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)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

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)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

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)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (96)

Assay IDTitleYearJournalArticle
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]
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]
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.
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).
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
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).
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).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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).
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).
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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]
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
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).
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).
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).
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' 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).
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).
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).
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).
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]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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).
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' 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
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).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (636)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990434 (68.24)18.7374
1990's86 (13.52)18.2507
2000's64 (10.06)29.6817
2010's44 (6.92)24.3611
2020's8 (1.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 73.55

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index73.55 (24.57)
Research Supply Index6.81 (2.92)
Research Growth Index4.22 (4.65)
Search Engine Demand Index131.01 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (73.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials239 (35.83%)5.53%
Reviews20 (3.00%)6.00%
Case Studies46 (6.90%)4.05%
Observational0 (0.00%)0.25%
Other362 (54.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Mechanisms of Diuretic Resistance in Heart Failure, Aim 2 [NCT05753059]Phase 150 participants (Anticipated)Interventional2023-08-10Recruiting
A Randomised, Parallel-group, Double-blind, Double-dummy Study to Compare the Effects of Lacidipine Versus Bendrofluazide on Markers of Platelet Activation and Haemorheological Factors in Hypertensive Patients [NCT02235402]Phase 426 participants (Actual)Interventional1997-12-31Completed
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931]22,213 participants (Actual)Observational2020-01-19Completed
Single-Dose Fed Bioequivalence Study of Nadolol/Bendroflumethiazide Tablets (80 mg/5 mg; Mylan) and Corzide® Tablets (80 mg/5 mg; King) in Healthy Volunteers [NCT00648297]Phase 142 participants (Actual)Interventional2006-08-31Completed
Single-Dose Fasting Bioequivalence Study of Nadolol/Bendroflumethiazide Tablets (80 mg/5 mg; Mylan) to Corzide® Tablets (80 mg/5 mg; King) in Healthy Volunteers [NCT00647660]Phase 166 participants (Actual)Interventional2006-07-31Completed
Double Blind Crossover Comparison od Diuretics in Young Patients With Low Renin Hypertension [NCT00429897]30 participants Interventional2006-08-31Recruiting
Pathophysiological Mechanisms of Hypertensive LVH:Optimising Regression [NCT00518479]42 participants (Actual)Interventional2003-09-30Completed
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial [NCT04330300]Phase 42,414 participants (Anticipated)Interventional2020-04-30Suspended(stopped due to Challenges with funding and very low incidence of COVID-19 at Irish study site)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]