Page last updated: 2024-12-05

moxisylyte

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

Description

Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4260
CHEMBL ID159226
CHEBI ID94754
SCHEMBL ID456546
MeSH IDM0021466

Synonyms (81)

Synonym
BRD-K81144366-003-03-1
thymoxamine
sympal
54-32-0
moxisylyte
4-{[2-(dimethylamino)ethyl]oxy}-2-methyl-5-(1-methylethyl)phenyl acetate
carlytene
moxilite
opilon
BPBIO1_000181
moxisilita [inn-spanish]
moxisylytum [inn-latin]
(2-(4-acetoxy-2-isopropyl-5-methylphenoxy)ethyl)dimethylamine
4-(2-(dimethylamino)ethoxy)-2-methyl-5-(1-methylethyl)phenol acetate (ester)
carvacrol, 5-(2-(dimethylamino)ethoxy)-, acetate (ester)
timoxamina
acetoxythymoxamine
moxisylyt
phenol, 4-(2-(dimethylamino)ethoxy)-2-methyl-5-(1-methylethyl)-, acetate (ester)
arlytene
einecs 200-204-1
NCGC00015678-01
lopac-m-5154
LOPAC0_000767
PRESTWICK3_000042
BSPBIO_000163
PRESTWICK2_000042
PRESTWICK0_000042
PRESTWICK1_000042
SPBIO_002084
NCGC00024362-03
NCGC00015678-03
NCGC00015678-07
moxisylyte (inn)
carlytene (tn)
D08239
CHEMBL159226
thymoxamine hcl
nsc759308
nsc-759308
pharmakon1600-01506079
CCG-204852
NCGC00015678-05
NCGC00015678-04
NCGC00015678-06
NCGC00015678-08
pw8qya7ki0 ,
moxisilita
unii-pw8qya7ki0
moxisylytum
moxisylyte [inn:ban:dcf]
moxisylyte [inn]
6-acetoxythymol 2-(dimethylamino)ethyl ether
moxisylyte [mi]
moxisylyte [who-dd]
SCHEMBL456546
4-(2-dimethylaminoethoxy)-2-methyl-5-isopropylphenyl acetate
5-(2-(dimethylamino)ethoxy)carvacrol acetate
((6-acetoxythymoxy)ethyl)dimethylamine
[2-(4-acetoxy-2-isopropyl-5-methylprhenoxy)ethyl]dimethylamine
carvacrol, 5-(2-(dimethylamino)ethoxy)-, acetate
phenol, 4-[2-(dimethylamino)ethoxy]-2-methyl-5-(1-methylethyl)-, acetate
4-dimethylaminoethoxycarvacrol
4-(2-dimethylaminoethoxy)-5-isopropyl-2-methylphenyl acetate
4-[2-(dimethylamino)ethoxy]-2-methyl-5-(methylethyl)phenyl acetate
bdbm50452139
4-(2-(dimethylamino)ethoxy)-5-isopropyl-2-methylphenyl acetate
DTXSID4023339
DB09205
CHEBI:94754
acetic acid [4-[2-(dimethylamino)ethoxy]-2-methyl-5-propan-2-ylphenyl] ester
SR-01000000205-7
SBI-0050745.P002
Q646045
SDCCGSBI-0050745.P003
NCGC00015678-13
arlytene; moxilite; moxisylite; moxisylyt; moxisylyte
[4-[2-(dimethylamino)ethoxy]-2-methyl-5-propan-2-ylphenyl] acetate
EN300-18567368
4-[2-(dimethylamino)ethoxy]-2-methyl-5-(propan-2-yl)phenyl acetate
gtpl12306

Research Excerpts

Overview

Moxisylyte is a competitive noradrenaline antagonist, acting preferentially on post-synaptic alpha-1 adrenoceptors. It is capable of producing erection when injected intra-cavernously.

ExcerptReferenceRelevance
"Moxisylyte chlorhydrate is a selective alpha-blocker of the post-synaptic alpha 1-adrenoreceptors. "( [Prolonged use of moxisylyte chlorhydrate (Icavex) by intracavernous self-injections in the treatment of impotence. Evaluation of long-term tolerance].
Arvis, G; Rivet, G; Schwent, B, 1996
)
2.07
"Moxisylyte is a competitive noradrenaline antagonist, acting preferentially on post-synaptic alpha-1 adrenoceptors. "( Moxisylyte: a review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in impotence.
Bressolle, F; Marquer, C, 1998
)
3.19
"Moxisylyte hydrochloride is an agent with potential clinical and research uses capable of producing erection when injected intra-cavernously."( Effect of moxisylyte hydrochloride on isolated human penile corpus cavernosum tissue.
Imagawa, A; Kawanishi, Y; Kimura, K; Tamura, M, 1989
)
1.4

Effects

ExcerptReferenceRelevance
"Moxisylyte has a relaxant action on the urethra that is probably ascribable to its alpha 1-adrenoceptor antagonist and Ca++ antagonist actions."( [Effect of moxisylyte on the lower urinary tracts (1). Effect on the isolated rabbit urethra and bladder].
Hayashi, Y; Ikeda, K; Ohnishi, H; Watanabe, K, 1991
)
1.39
"Moxisylyte has a relaxant action on the urethra that is probably ascribable to its alpha 1-adrenoceptor antagonist and Ca++ antagonist actions."( [Effect of moxisylyte on the lower urinary tracts (1). Effect on the isolated rabbit urethra and bladder].
Hayashi, Y; Ikeda, K; Ohnishi, H; Watanabe, K, 1991
)
1.39

Toxicity

ExcerptReferenceRelevance
" Observations were made of toxic reactions of ocular tissues using slit-lamp biomicroscopy."( Toxicity of intracameral thymoxamine.
Cheeks, L; Crosby, VA; Green, K, 1990
)
0.28

Pharmacokinetics

ExcerptReferenceRelevance
" In the present study, we have investigated the pharmacokinetic and pharmacodynamic characteristics of ibopamine after ocular application."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" The other pharmacokinetic parameters show no change between the two routes of administration."( Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and intracavernous administration.
Bressolle, F; Costa, P; Galtier, M; Mosser, J; Sarrazin, B, 1993
)
0.61
" The pharmacokinetic parameters determined after the first oral administration were not modified on multiple dosing."( Multiple-dose pharmacokinetics of moxisylyte after oral administration to healthy volunteers.
Bressolle, F; Costa, P; Galtier, M; Jarroux, E; Mosser, J; Navratil, H; Sarrazin, B, 1993
)
0.57
" Cmax and AUC increased in direct proportion to dose, except for the inactive DAM glucuronide."( Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses.
Bressolle, F; Costa, P; Marquer, C; Rouzier-Panis, R, 1996
)
0.62
"The percutaneous pharmacokinetic parameters of 14C-thymoxamine (4-(2-dimethylaminoethoxy)-5-isopropyl-2-methyl phenyl acetate, moxisylyte, Carlytène) were studied on female hairless rats."( Pharmacokinetics study of 14C-moxisylyte after percutaneous application to hairless rat.
Courtiol, C; Lambrey, B; Marty, JP; Neau, B; Roux, J, 1995
)
0.79

Bioavailability

ExcerptReferenceRelevance
" Ibopamine is well absorbed through the cornea, it is rapidly hydrolysed by esterases to epinine and the mydriatic effect is correlated with the concentration of epinine in the aqueous humor."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" Membrane permeability to urea, glucose, and protein, actual net ultrafiltration rate (UFR), transcapillary ultrafiltration rate (TCUFR), and peritoneal net fluid absorption rate (PNFAR) were measured."( Effects of vasodilators on peritoneal solute and fluid transport in rat peritoneal dialysis.
Go, M; Kumano, K; Ning, H; Sakai, T, 1996
)
0.29

Dosage Studied

ExcerptRelevanceReference
"In six patients with extrinsic bronchial asthma the inhalation of prostaglandin (PG) F2 alpha in a small dosage produced significant bronchoconstriction, whereas PGE2 produced bronchodilatation."( Atropine, sodium cromoglycate, and thymoxamine in PGF2 alpha-induced bronchoconstriction in extrinsic asthma.
Patel, KR, 1975
)
0.25
" Dose-response lines for all the compounds except clonidine were parallel."( Comparison of pre-junctional alpha-adrenoceptors at the neuromuscular junction with vascular post-junctional alpha-receptors in cat skeletal muscle.
Malta, E; McPherson, GA; Raper, C, 1979
)
0.26
" Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effect of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens."( [Comparative study of the pre and post-synaptic alpha blocking activity of thymoxamine and its metabolites in the rat vas deferens (author's transl)].
Canellas, J; Demichel, P; Malek, A; Roquebert, J,
)
0.13
" The dose-response curves were parallel and no statistically significant difference could be shown between the IC50 values."( Adrenergic receptors on smooth muscle cells isolated from human penile corpus cavernosum.
Bali, JP; Costa, P; Navratil, H; Rebillard, X; Sarrazin, B; Soulie-Vassal, ML, 1993
)
0.29
" Whatever etiology of impotence and dosage tested, the erectile response induced by moxisylyte was significantly higher than the placebo-induced response."( Efficiency and side effects of intracavernous injections of moxisylyte in impotent patients: a dose-finding study versus placebo.
Bondil, P; Bressolle, F; Colson, MH; Costa, P; Sarrazin, B; Saudubray, F, 1993
)
0.75
" The injections were then repeated with increasing dosage to archive a rigid erection."( [Intracavernous injections in the treatment of erectile dysfunction in spinal cord injured patients: experience with 36 patients].
Boiteau, F; Boyer, F; Dizien, O; Laffont, I; Lebib Ben Achour, S, 2001
)
0.31
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
monoterpenoidAny terpenoid derived from a monoterpene. The term includes compounds in which the C10 skeleton of the parent monoterpene has been rearranged or modified by the removal of one or more skeletal atoms (generally methyl groups).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency0.56230.35487.935539.8107AID624146
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency25.11890.00137.762544.6684AID914; AID915
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency10.00000.00207.533739.8107AID891
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency10.26630.00106.000935.4813AID943; AID944
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.01262.511912.262825.1189AID954; AID958
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (59)

Assay IDTitleYearJournalArticle
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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]
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.
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID35982In vitro relative blocking action (pA2) of the post-synaptic Alpha-1 adrenergic receptor from rat and rabbit aorta1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
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]
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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
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]
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS 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]
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]
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
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]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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.
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]
AID36042In vitro for relative blocking action (pA2) of Presynaptic Alpha-2 adrenergic receptor from guinea pig ileum.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID625293Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (275)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990182 (66.18)18.7374
1990's61 (22.18)18.2507
2000's13 (4.73)29.6817
2010's13 (4.73)24.3611
2020's6 (2.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.07

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 Index28.07 (24.57)
Research Supply Index5.86 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index35.70 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.07)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials55 (18.64%)5.53%
Reviews18 (6.10%)6.00%
Case Studies11 (3.73%)4.05%
Observational0 (0.00%)0.25%
Other211 (71.53%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]