Page last updated: 2024-12-04

bupranolol

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

Description

Bupranolol: An adrenergic-beta-2 antagonist that has been used for cardiac arrhythmia, angina pectoris, hypertension, glaucoma, and as an antithrombotic. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2475
CHEMBL ID305380
CHEBI ID135123
SCHEMBL ID34061
MeSH IDM0003051

Synonyms (62)

Synonym
gtpl550
14556-46-8
1-[(2-chloro-5-methylphenyl)oxy]-3-[(1,1-dimethylethyl)amino]propan-2-ol
2-propanol, 1-(tert-butylamino)-3-((6-chloro-m-tolyl)oxy)-
2-propanol, 1-(tert-butylamino)-3-(6-chloro-m-tolyloxy)-
kl 255
2-propanol, 1-(2-chloro-5-methylphenoxy)-3-((1,1-dimethylethyl)amino)-
bupranolol [inn:dcf]
1-t-butylamino-3-(2-chloro-5-methylphenoxy) -2-propanol
3-(tert-butylamino)-1-(6-chloro-m-tolyloxy)-2-propanol
brn 2272923
1-(tert-butylamino)-3-((6-chloro-m-tolyl)-oxy)-2-propanol
2-propanol, 1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)-
ophtorenin
sk&f 16805-a
bupranololum [inn-latin]
D07590
bupranolol (inn)
bdbm25765
tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine
bupranolol
CHEBI:135123
DB08808
CHEMBL305380
bupranol
kl-255 [as hydrochloride]
b 1312 [as hydrochloride]
L000149
1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)propan-2-ol
858ygi5pit ,
unii-858ygi5pit
bupranololum
AKOS016015423
b 1312 free base
b-1312 free base
bupranolol [mi]
kl-255 free base
bupranolol [who-dd]
bupranolol [inn]
SCHEMBL34061
NCGC00249915-01
tox21_113691
dtxsid7022704 ,
dtxcid202704
cas-14556-46-8
1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)-2-propanol #
1-(tert-butylamino)-3-[(6-chloro-m-tolyl)-oxy]-2-propanol
HMS3604F15
sr-01000945044
SR-01000945044-1
38104-34-6
Q425838
Z1497043450
(+/-)-bupranolol; bupranol; ophtorenin
(s)-bupranolol
F81732
EN300-134241
()-bupranolol; bupranol; ophtorenin
AS-82519
CS-0017596
HY-A0252
s-bupranolol

Research Excerpts

Overview

Bupranolol is an antagonist at the cardiostimulatory low-affinity state of b(1)-adrenoceptors. The extensive first-pass metabolism and rapid elimination half-life make it well suited to be developed as a transdermal delivery system (TDS)

ExcerptReferenceRelevance
"Bupranolol is an antagonist at the cardiostimulatory low-affinity state of b(1)-adrenoceptors and we were interested whether this effect is shared by its fluorine (GD-6), methyl (DZ-51) and isopropyl analogue (DZ-13) and by the analogue hydroxylated at the tertiary butyl moiety (DZ-52). "( Four close bupranolol analogues are antagonists at the low-affinity state of beta1-adrenoceptors.
Baranowska, M; Baranowska, U; Kiec-Kononowicz, K; Kozlowska, H; Malinowska, B; Reutelsterz, A; Schlicker, E; Zelaszczyk, D, 2009
)
2.19
"Bupranolol (BPL) is a potent beta-blocking agent, the extensive first-pass metabolism (>90%) and rapid elimination half-life (1.5-2.0 h) of this drug make it well suited to be developed as a transdermal delivery system (TDS). "( Effect of cyclodextrins on the complexation and transdermal delivery of bupranolol through rat skin.
Babu, RJ; Pandit, JK, 2004
)
2
"Bupranolol (BPL) is a suitable drug candidate for transdermal drug delivery system development based on its favorable physicochemical and pharmacokinetic properties. "( Effect of penetration enhancers on the transdermal delivery of bupranolol through rat skin.
Babu, RJ; Pandit, JK,
)
1.81
"Bupranolol is a promising candidate for transdermal drug delivery system (TDDS) development. "( Cardiovascular effects of transdermally delivered bupranolol in rabbits: effect of chemical penetration enhancers.
Babu, RJ; Dhanasekaran, M; Pandit, JK; Singh, PN; Vaithiyalingam, SR, 2008
)
2.04
"Bupranolol is a non-selective beta-adrenoceptor antagonist with a Ki-value of 6-15 nmol/l (equivalent to 1.5-4 ng/ml in plasma) at beta 1- (rat salivary gland) and beta 2-adrenoceptors (rat reticulocytes) in receptor binding studies with 3H-CGP 12177 in the presence of human plasma. "( Transdermal delivery of bupranolol: pharmacodynamics and beta-adrenoceptor occupancy.
Küppers, H; Palm, D; Pitschner, HF; Wellstein, A, 1986
)
2.02

Treatment

ExcerptReferenceRelevance
"Treatment with Bupranolol is given for six months and results in clear reduction of intraocular pressure in all patients, so that satisfactory control can be achieved with Bupranolol eye drops either alone or in combination with a miotic agent."( [Long-term treatment of angle-closure glaucoma with bupranolol eye drops (author's transl)].
Demmler, N, 1980
)
0.85

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacodynamic effect of the model drug bupranolol in vivo was investigated over a 10-hr time period."( Influence of supersaturation on the pharmacodynamic effect of bupranolol after dermal administration using microemulsions as vehicle.
Kemken, J; Müller, BW; Ziegler, A, 1992
)
0.78
"The pharmacodynamic effect of a homologous series of aminomethyldimethyl-(methoxyphenyl)-silane derivatives have been tested on isolated guinea-pig left atria."( Pharmacodynamic specification and membrane stabilising action of a homologous series of silasympathomimetics.
Greeff, K; Schlieper, P; Tawfik, H, 1986
)
0.27

Compound-Compound Interactions

ExcerptReferenceRelevance
"The optimal daily dose and dose regimen of a new drug combination (Pertenso), consisting of 10 mg bemetizide, 20 mg triamterene, 20 mg dihydralazine and 20 mg bupranolol were tested in 14 hypertensive outpatients (WHO I to III) in a single blind crossover trial."( [Treatment of hypertension with a drug combination, consisting of bemetizide, triamterene, dihydralazine and bupranolol (author's transl)].
Brandstetter, G; Gasser, RW; Skrabal, F, 1982
)
0.67

Bioavailability

ExcerptReferenceRelevance
" This leads to in situ formation of a super-saturated ME that possesses a particularly high absorption rate due to the enhanced diffusion pressure of the drug."( Pharmacodynamic effects of transdermal bupranolol and timolol in vivo: comparison of microemulsions and matrix patches as vehicle.
Kemken, J; Müller, BW; Ziegler, A, 1991
)
0.55
"An oral dose of 14C-bupranolol hydrochloride was well absorbed by humans (100 mg), dogs (1 mg/kg), and rhesus monkeys (1 mg/kg)."( Metabolic fate of the beta-blocker 14C-bupranolol in humans, dogs, and rhesus monkeys.
Bonn, R; Chasseaud, LF; Darragh, A; Down, WH; Doyle, E; Girkin, R; Taylor, T; Waller, AR,
)
0.72
" Nasal administration of selected batches of polymeric solutions were found to be nontoxic and were able to improve drug bioavailability when compared to oral, nasal, and intravenous solution administrations of BPH."( Polymer based solutions of bupranolol hydrochloride for intranasal systemic delivery.
Mishra, B; Mishra, M; Sankar, C, 2011
)
0.67

Dosage Studied

ExcerptRelevanceReference
" ST-depression at comparative work load at 2 h after dosing was reduced by 49% acutely after administration of IS-5-MN."( Evaluation of the antianginal and anti-ischemic efficacy of slow-release isosorbide-5-mononitrate capsules, bupranolol and their combination, in patients with chronic stable angina pectoris.
Krepp, HP, 1991
)
0.49
"Combinations of antianginal drugs may be used for an additive effect against angina, but also to off-set unwanted effects of one drug with another, either by direct effects or by a reduction of dosage of each drug."( Interactions of vasodilators with calcium entry- and beta-blockers in patients with coronary heart disease.
Adam, WE; Haerer, W; Henze, E; Hermann, T; Kohler, J; Kress, P; Stauch, M, 1986
)
0.27
" Initial dosage of two tablets could be reduced to one tablet daily following normalization (less than 90 mm Hg) of diastolic blood pressure in one third of patients."( [Treatment of medium-severe essential hypertension with beta-Aldopur under practice conditions].
Guberner, G; Hitzenberger, G; Nitsch-Fitz, R; Rheindorf, H; Tutsch, G; Ziegler, KT, 1985
)
0.27
" beta-Adrenoceptor blocking agents were found to interact with isoproterenol in a manner consistent with a simple competitive antagonism provided that (1) the antagonist had little intrinsic stimulant action on the preparation under study, (2) the concentrations of antagonist used had no direct depressant action on the preparation, (3) precautions were taken to assure that the pattern of antagonism was not distorted by loss of agonist into tissue sinks, and (4) dose-response curves were normalized for changes in the baseline frequency or force in successive curves."( Comparative assessment of beta-adrenoceptor blocking agents as simple competitive antagonists in isolated heart muscle: similarity of inotropic and chronotropic blocking potencies against isoproterenol.
Blinks, JR; Gilmour, DP; Kaumann, AJ; McInerny, TK, 1980
)
0.26
" The optimum daily dosage are 2 to 3 tablets; duration of treatment ranged from 2 to 12 weeks."( [Betamed in the treatment of psychogenic disorders with a somatic component].
Jellinger, K, 1983
)
0.27
[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]

Pathways (1)

PathwayProteinsCompounds
Bupranolol Action Pathway478

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLI family zinc finger 3Homo sapiens (human)Potency13.33320.000714.592883.7951AID1259392
pregnane X nuclear receptorHomo sapiens (human)Potency33.49150.005428.02631,258.9301AID1346982
cytochrome P450 2D6Homo sapiens (human)Potency1.73770.00108.379861.1304AID1645840
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency27.96440.057821.109761.2679AID1159526; AID1159528
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.62280.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-2 adrenergic receptorHomo sapiens (human)Kd0.03140.00000.62888.9130AID1798580
Beta-1 adrenergic receptorHomo sapiens (human)Kd0.03140.00010.803910.0000AID1798580
Beta-3 adrenergic receptorHomo sapiens (human)Kd0.03140.00010.76318.9130AID1798580
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID1346297Human beta3-adrenoceptor (Adrenoceptors)1995European journal of pharmacology, Nov-30, Volume: 291, Issue:3
Carazolol: a potent, selective beta 3-adrenoceptor agonist.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
AID1346297Human beta3-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3
LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
AID1346260Human beta1-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3
LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
AID1346297Human beta3-adrenoceptor (Adrenoceptors)1993Molecular pharmacology, Dec, Volume: 44, Issue:6
Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3
LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
AID1346297Human beta3-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
AID1346260Human beta1-adrenoceptor (Adrenoceptors)1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
Potent and selective human beta(3)-adrenergic receptor antagonists.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
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.
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.
AID40539Selectivity for beta-1 receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID41488Selectivity for beta-2 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
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.
AID41892Tested for intrinsic sympathomimetic activity (ISA); pure antagonist1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID17985803H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: \\The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.\\2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (208)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990108 (51.92)18.7374
1990's49 (23.56)18.2507
2000's36 (17.31)29.6817
2010's8 (3.85)24.3611
2020's7 (3.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.49

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 Index32.49 (24.57)
Research Supply Index5.49 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index47.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials28 (13.08%)5.53%
Reviews1 (0.47%)6.00%
Case Studies3 (1.40%)4.05%
Observational0 (0.00%)0.25%
Other182 (85.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]