Page last updated: 2024-11-04

linsidomine

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

Description

Linsidomine is a nitric oxide (NO) donor that has been investigated for its potential therapeutic effects in various conditions. Its synthesis involves the reaction of a nitro compound with a suitable reducing agent. Linsidomine releases NO, a signaling molecule involved in vasodilation, neurotransmission, and other physiological processes. The release of NO contributes to the vasodilatory effects of linsidomine, potentially improving blood flow and reducing blood pressure. It has been studied for its potential benefits in conditions such as erectile dysfunction, peripheral artery disease, and Raynaud's phenomenon. Linsidomine is also being investigated for its neuroprotective and anti-inflammatory properties. Research on linsidomine continues to explore its potential as a therapeutic agent in various medical conditions.'

linsidomine: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5219
CHEMBL ID1189150
CHEBI ID136004
SCHEMBL ID160502
MeSH IDM0042933

Synonyms (51)

Synonym
linsidomine
cv 664
linsidomina [spanish]
3-morpholinosydnone imine
3-morpholinosydnonimine-1
linsidominum [latin]
3-morpholinosydnoneimine
linsidomine [inn]
lopac-m-184
NCGC00015636-01
33876-97-0
linsidomine (inn)
D07161
3-morpholinosydnonimine
NCGC00018289-01
NCGC00162279-01
CHEBI:136004
NCGC00015636-03
3-morpholin-4-yl-1-oxa-3-azonia-2-azanidacyclopent-3-en-5-imine
NCGC00018289-02
NCGC00018289-03
AKOS006280506
AKOS005252588
CCG-204937
NCGC00015636-02
5o5u71p6vq ,
linsidomina
unii-5o5u71p6vq
FT-0630574
CHEMBL1189150
linsidomine [who-dd]
SCHEMBL160502
bdbm83470
cid_9859122
(3-morpholino-1-oxa-3-azonia-2-azanidacyclopent-3-en-5-ylidene)amine;hydrochloride
3-(4-morpholinyl)-1-oxa-3-azonia-2-azanidacyclopent-3-en-5-imine;hydrochloride
FKDHHVKWGRFRTG-UHFFFAOYSA-N
MLS-0003225
5-azanidyl-3-(morpholin-4-yl)-1,2,3|e?-oxadiazol-3-ylium
5-imino-3-morpholino-5h-1,2,3-oxadiazol-3-ium-2-ide
cv 664;3-morpholinosydnonmine
BCP26037
3-morpholin-4-yl-1,2,3-oxadiazol-3-ium-5-amine chloride
DB13400
Q1130256
NCGC00015636-05
NCGC00015636-06
(3-morpholino-1,2,3-oxadiazol-3-ium-5-yl)amide
HY-126849
CS-0107790
DTXSID501026026

Research Excerpts

Overview

Linsidomine is a direct donor of EDRF/NO which has an action on blood vessels. It reduces preload and dilatation of the large epicardial coronary vessels.

ExcerptReferenceRelevance
"Linsidomine is a direct donor of EDRF/NO which has an action on blood vessels (reduction of preload and dilatation of the large epicardial coronary vessels) and on platelets (inhibition of aggregation) without risk of tolerance."( [Linsidomine, direct donor of EDRF/NO: a new treatment for unstable angina].
Charansonney, O; Delonca, J; Giraud, T; Lennuyeux, E, 1996
)
1.93

Treatment

ExcerptReferenceRelevance
"Treatment with linsidomine and molsidomine was associated with a modest improvement in the long-term angiographic result after angioplasty but had no effect on clinical outcome. "( Effect of the direct nitric oxide donors linsidomine and molsidomine on angiographic restenosis after coronary balloon angioplasty. The ACCORD Study. Angioplastic Coronaire Corvasal Diltiazem.
Bassand, JP; Battaglia, S; Béard, T; Bertrand, B; Bertrand, ME; Boschat, J; Coste, P; Crochet, PD; Desveaux, B; Drobinski, G; Dubois-Randé, JL; Finet, G; Giraud, T; Grollier, G; Juillière, Y; Juliard, JM; Lablanche, JM; Le Breton, H; Leclercq, F; Letac, B; Livarek, B; Lusson, JR; Metzger, JP; Quiret, JC; Virot, P, 1997
)
0.92

Toxicity

ExcerptReferenceRelevance
" SIN-1 (< 1 mM) was only slightly toxic to HepG2 cells."( Increased cytotoxicity of 3-morpholinosydnonimine to HepG2 cells in the presence of superoxide dismutase. Role of hydrogen peroxide and iron.
Cederbaum, AI; Gergel, D; Misík, V; Ondrias, K, 1995
)
0.29
"We sought to investigate whether linsidomine chlorhydrate (SIN1, the active metabolite of molsidomine and a nitric oxide donor) has a toxic effect when used chronically for the treatment of impotence."( Intracavernous injection of linsidomine chlorhydrate in monkeys: lack of toxic effect with long-term use.
Brock, GB; Lue, TF; Martinez-Piñeiro, L; von Heyden, B, 1996
)
0.87
"SIN1 appears to be a safe option for the pharmacotherapy of erectile dysfunction."( Intracavernous injection of linsidomine chlorhydrate in monkeys: lack of toxic effect with long-term use.
Brock, GB; Lue, TF; Martinez-Piñeiro, L; von Heyden, B, 1996
)
0.59
" We conclude that exposures to toxic levels of NO cause prolonged disruption of [Ca2+]i homeostatic mechanisms, and that the resulting persistent [Ca2+]i elevations contribute to the delayed neurotoxicity of NO."( Disrupted [Ca2+]i homeostasis contributes to the toxicity of nitric oxide in cultured hippocampal neurons.
Brorson, JR; Zhang, H, 1997
)
0.3
" These results demonstrate that the immediate toxic agent formed from SIN-1 decisively depends on the presence of Hepes."( The critical role of Hepes in SIN-1 cytotoxicity, peroxynitrite versus hydrogen peroxide.
de Groot, H; Kirsch, M; Lomonosova, EE; Rauen, U, 1998
)
0.3
"Microglia have been shown to be immunostimulated by inflammatory cytokines and produce a number of toxic mediators."( Potentiation of N-methyl-D-aspartate-mediated neurotoxicity by immunostimulated murine microglia.
Kim, WK; Ko, KH, 1998
)
0.3
"1 mM SIN-1 were not toxic to MAC-T cells."( Cytotoxic effects of peroxynitrite, polymorphonuclear neutrophils, free-radical scavengers, inhibitors of myeloperoxidase, and inhibitors of nitric oxide synthase on bovine mammary secretory epithelial cells.
Douglass, LW; Ledbetter, TK; Paape, MJ, 2001
)
0.31
"Peroxynitrite, MPO, and histidine are toxic to mammary secretory epithelial cells."( Cytotoxic effects of peroxynitrite, polymorphonuclear neutrophils, free-radical scavengers, inhibitors of myeloperoxidase, and inhibitors of nitric oxide synthase on bovine mammary secretory epithelial cells.
Douglass, LW; Ledbetter, TK; Paape, MJ, 2001
)
0.31
" Furthermore, when cells reached confluence they were highly resistant to the toxic effects of peroxynitrite, hydrogen peroxide, and superoxide."( Role of intracellular calcium mobilization and cell-density-dependent signaling in oxidative-stress-induced cytotoxicity in HaCaT keratinocytes.
Bai, P; Bakondi, E; Csernoch, L; Gergely, P; Gönczi, M; Hunyadi, J; Kovács, L; Pacher, P; Szabó, C; Szabó, E; Virág, L, 2003
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
" After a 2 mg oral dose, molsidomine elimination half-life was prolonged in cirrhotic patients (13."( Pharmacokinetics of molsidomine and its active metabolite, linsidomine, in patients with liver cirrhosis.
Advenier, C; Andrieu, J; Cordonnier, P; Doll, J; Dutot, C; Grandjean, N; Pays, M; Spreux-Varoquaux, O, 1991
)
0.52
" After a 2 mg oral administration, molsidomine elimination half-life was prolonged in elderly subjects (1."( Pharmacokinetics of molsidomine and of its active metabolite, SIN-1 (or linsidomine), in the elderly.
Advenier, C; Cordonnier, P; Ducreuzet, C; Forestier, A; Pays, M; Spreux-Varoquaux, O; Ulmer, B, 1991
)
0.51
" The pharmacokinetic parameters of molsidomine were similar to already published data in healthy volunteers and patients."( Liver function and pharmacokinetics of molsidomine and its metabolite 3-morpholinosydnonimine in healthy volunteers.
Chamberlain, J; Gärtner, W; Ostrowski, J; Stockhausen, H; Wildgrube, HJ, 1986
)
0.27
"The pharmacokinetic properties and hemodynamic effect of molsidomine and its pharmacologically active metabolite SIN-1 were investigated in 13 healthy volunteers following single oral doses."( Relationship between pharmacokinetics and pharmacodynamics of molsidomine and its metabolites in humans.
Brandstätter, A; Gärtner, W; Jähnchen, E; Meinertz, T; Ostrowski, J; Trenk, D, 1985
)
0.27

Compound-Compound Interactions

ExcerptReferenceRelevance
"Molsidomine and its vasoactive metabolite SIN-1 elicit anti-ischemic properties by a therapeutically useful pattern of different vasoactive actions combined with a cyclic GMP-mediated inhibition of platelet adhesion and aggregation."( Anti-ischemic actions of molsidomine by venous and large coronary dilatation in combination with antiplatelet effects.
Bassenge, E; Mülsch, A, 1989
)
0.28
" Moreover, CSM dramatically enhances the production of IL-8 in combination with TNF-alpha."( IL-8 production by macrophages is synergistically enhanced when cigarette smoke is combined with TNF-alpha.
Folkerts, G; Givi, ME; Janse, WT; Mortaz, E; Nijkamp, FP; Sarir, H, 2010
)
0.36

Bioavailability

ExcerptReferenceRelevance
" Its absolute bioavailability (44 +/- 15%) and a 14C-labeled triale give evidence of quick biotransformation of molsidomine to active metabolites."( Pharmacokinetics of molsidomine in humans.
Ostrowski, J; Resag, K, 1985
)
0.27
"Ischemia-reperfusion injury causes tissue damage that leads to a decrease in bioavailability of nitric oxide."( The effects of the nitric oxide donor SIN-1 on ischemia-reperfused cutaneous and myocutaneous flaps.
Kerrigan, CL; Khiabani, KT, 2002
)
0.31
" cell-mediated) types of action in protecting LDL against oxidation, strengthening the need for improving the knowledge of its bioavailability in humans."( Grape and grape seed extract capacities at protecting LDL against oxidation generated by Cu2+, AAPH or SIN-1 and at decreasing superoxide THP-1 cell production. A comparison to other extracts or compounds.
Carbonneau, MA; Descomps, B; Leger, CL; Shafiee, M; Urban, N, 2003
)
0.32
"Nitric oxide (NO) derived from eNOS is mostly responsible for the maintenance of vascular homeostasis and its decreased bioavailability is characteristic of reactive oxygen species (ROS)-induced endothelial dysfunction (ED)."( Reversal of SIN-1-induced eNOS dysfunction by the spin trap, DMPO, in bovine aortic endothelial cells via eNOS phosphorylation.
Cardounel, AJ; Das, A; De Pascali, F; Druhan, LJ; Gopalakrishnan, B; Racoma, I; Rockenbauer, A; Varadharaj, S; Villamena, FA; Wang, TY; Zweier, JL, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" Preincubation of contracted artery rings with GTP (100 microM) or guanosine (100 microM) before eliciting relaxations with nitrovasodilators significantly shifted the dose-response curves of nitrocompounds to the left and augmented the increases in cyclic GMP."( Modification of nitrovasodilator effects on vascular smooth muscle by exogenous GTP and guanosine.
Laustiola, KE; Manninen, V; Metsä-Ketelä, T; Pörsti, I; Vapaatalo, H; Vuorinen, P, 1991
)
0.28
" This is a short-term action and the dosage is limited by systemic hypotension."( [Endothelial factors and thrombocyte function].
Schrör, K, 1991
)
0.28
" Major (coronary substrate, study design) and minor (measuring devices, methods of evaluation) methodological problems make it difficult to precisely evaluate pharmacological effects such as dose-response relationship, duration of action, and selective responses, and to compare the effects of different drugs."( Response of coronary arteries to nitrates, the EDRF-donor SIN-1, and calcium antagonists.
Kober, G; Schulz, W, 1991
)
0.28
" After elevation of tone with KCl (15 mM), dose-response curves were constructed for nitroglycerin or SIN1 (3-morpholino-syndnonimin) on control and tolerant rings."( Persistence of the response to SIN1 on isolated coronary arteries rendered tolerant to nitroglycerin in vitro or in vivo.
Berkenboom, G; Degre, S; Fontaine, J, 1988
)
0.27
" Furthermore, the inhibition of 45Ca2+ uptake and of fluorescence increase observed in the presence of extracellular Ca2+ displayed remarkably parallel dose-response curves, suggesting that elevation of cyclic GMP brought about by SIN-1 inhibits the opening of "receptor-operated channels" whose precise nature remains to be determined."( Inhibition of calcium influx in thrombin-stimulated platelets by SIN-1, an activator of soluble guanylate cyclase.
Chap, H; Simon, MF, 1989
)
0.28
" As a result, the dose-response curve of SIN-1 was shifted to the left."( Interaction between SIN-1 and prostacyclin in inhibiting platelet aggregation.
Bult, H; Fret, HR; Herman, AG, 1989
)
0.28
" When the strips were treated with submaximal effective concentrations of NO, some tolerance was observed, as shown by moderate attenuation of the rises in cyclic GMP, and a rightward shift of the dose-response curve of the relaxing effects by a dose factor of 10 (DF = 10)."( Tolerance and cross-tolerance between SIN-1 and nitric oxide in bovine coronary arteries.
Holzmann, S; Kukovetz, WR, 1989
)
0.28
"Plasma levels of N-carboxy-3-morpholinosydnonimine ethyl ester (molsidomine, Corvaton) and its pharmacologically active metabolite 3-morpholinosydnonimine (SIN-1) were measured in six healthy male and female volunteers after single intravenous and oral dosing of 4 mg molsidomine."( Liver function and pharmacokinetics of molsidomine and its metabolite 3-morpholinosydnonimine in healthy volunteers.
Chamberlain, J; Gärtner, W; Ostrowski, J; Stockhausen, H; Wildgrube, HJ, 1986
)
0.27
"The pharmacokinetics of molsidomine were investigated in the plasma and urine of healthy male volunteers and patients with coronary heart disease after intravenous and/or oral administration of different galenic dosage forms of molsidomine."( Pharmacokinetics of molsidomine in humans.
Ostrowski, J; Resag, K, 1985
)
0.27
" Moreover, oxyhemoglobin, a scavenger of free NO, suppressed the chemotactic effect of SNAP, whereas LY-83583, a soluble guanylate cyclase inhibitor, inhibited the SNAP-mediated chemotaxis in a dose-response manner."( Exogenous nitric oxide elicits chemotaxis of neutrophils in vitro.
Beauvais, F; Dubertret, L; Michel, L, 1995
)
0.29
"The combination of hydralazine and nitrates has been shown to provide long-term benefit in congestive heart failure, despite a nitrate dosage that should induce tolerance."( Interaction between hydralazine and nitrovasodilators in vascular smooth muscle.
Berkenboom, G; Fontaine, J; Unger, P, 1993
)
0.29
" PGE1 always achieved the best response, SIN-1 performed statistically significantly poorer irrespective of the dosage used."( Prostaglandin E1 versus linsidomine chlorhydrate in erectile dysfunction.
Klän, R; Knispel, HH; Meier, T; Miller, K; Wegner, HE, 1994
)
0.6
" Nitroglycerin pre-exposure (10 microM for 30 min) provoked a significant shift to the right of the dose-response curve to nitroglycerin in aortae isolated from rats of 8 weeks, 12 and 18 months."( Nitrate tolerance and aging in isolated rat aorta.
Berkenboom, G; Brékine, D; Fontaine, J; Unger, P, 1993
)
0.29
" The differences between aorto-caval fistula rats and sham operated rats were probably the result of increased basal EDRF-NO release in the former, since NO synthase blockade abolished the differences in both aortic cGMP and the dose-response curve to Sin-1."( Vascular relaxation and cyclic guanosine monophosphate in a rat model of high output heart failure.
Arnal, JF; Michel, JB; Schott, C; Stoclet, JC, 1993
)
0.29
"Pharmacokinetic measurements were performed in two groups of patients with coronary heart disease (CHD) after single and multiple dosing of 2 mg linsidomine (SIN 1)."( Pharmacokinetics of linsidomine (SIN 1) after single and multiple intravenous short infusions in patients with renal insufficiency.
Degré, S; Gaertner, W; Ostrowski, J; Sennesael, J; Stolear, JC; Unger, P; Verbeelen, D; von Hattingberg, HM, 1993
)
0.81
" However, the inhibition of the combined CPA and CCh response was reduced and the dose-response curve of SIN-1 shifted to the right."( Involvement of intracellular Ca2+ stores in inhibitory effects of NO donor SIN-1 and cGMP.
Allescher, HD; Franck, H; Puschmann, A; Schusdziarra, V; Storr, M, 1998
)
0.3
" Acetaminophen is a phenolic compound which produces a clear inhibitory dose-response curve with peroxynitrite in its range of clinical effectiveness."( A new screening method to detect water-soluble antioxidants: acetaminophen (Tylenol) and other phenols react as antioxidants and destroy peroxynitrite-based luminol-dependent chemiluminescence.
Qazi, N; Sacks, M; Van Dyke, K,
)
0.13
"05) in all prostanoids evaluated in a dose-response fashion."( Nitric oxide inhibits prostanoid synthesis in the rat oviduct.
Farina, M; Franchi, AM; Gimeno, M; Ogando, D; Perez Martinez, S; Ribeiro, ML, 2000
)
0.31
"01); (3) in the presence of L-arginine (a substrate of NO synthase), a left shift of the ACh dose-response curves was found in control subjects, but not in ADPKD patients; (4) in the presence of the N(G)-nitro-L-arginine methyl ester (an inhibitor of NO synthase), a right shift of the ACh dose-response curve was found in control subjects, but not in ADPKD patients; and (5) endothelium-independent relaxation rate induced with SIN-1 was similar in patients and control subjects."( Endothelium-dependent relaxation of small resistance vessels is impaired in patients with autosomal dominant polycystic kidney disease.
Iversen, J; Strandgaard, S; Wang, D, 2000
)
0.31
" ODQ (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one), a potent and selective inhibitor of soluble guanylyl cyclase (sGC), did not significantly affect relaxant actions of ONOO-, but ODQ markedly attenuated SIN-1-elicited relaxation with a rightward shift in the dose-response curve and an unaltered maximal response."( Comparative vasodilation of peroxynitrite and 3-morpholinosydnonimine.
Trakranrungsie, N; Will, JA, 2001
)
0.31
" unstimulated conditions), the nitric oxide synthase (NOS) inhibitor L-NIO (L-N(5)-(1-iminoethyl) ornithine, 10(-5) and 10(-4) M), caused a marked vasoconstriction (20%), indicating a basal nitrergic vasodilator tone, while the dose-response curve of the NO donor SIN-1 (3-morpholinosydnonimine) showed a dose-dependent vasodilator effect."( Control of cardiovascular function in the icefish Chionodraco hamatus: involvement of serotonin and nitric oxide.
Acierno, R; Pellegrino, D; Tota, B, 2003
)
0.32
" In both dogfish and eel, AD dose-response curves showed a biphasic effect: vasoconstriction (pico to nanomolar range) and vasodilation (micromolar range)."( Adenosine/nitric oxide crosstalk in the branchial circulation of Squalus acanthias and Anguilla anguilla.
Pellegrino, D; Randall, DJ; Tota, B, 2005
)
0.33
"Each of the single topical drugs produced significant dose-dependent antiallodynic effects compared with vehicle in CPIP rats (N = 30), and the antiallodynic dose-response curves of either PA or PDE inhibitors were shifted 5- to 10-fold to the left when combined with nonanalgesic doses of α2A receptor agonists or NO donors (N = 28)."( Topical combinations to treat microvascular dysfunction of chronic postischemia pain.
Abaji, R; Coderre, TJ; Laferrière, A; Ragavendran, JV; Tsai, CY, 2014
)
0.4
" Myocytes superfused with 3-morpholinosydnonimine N-ethylcarbamide (SIN-1), an ONOO- donor, decreased the amplitude of Ca2+ transients and contraction in a dose-response (1-200 μM) manner."( Peroxynitrite-Induced Intracellular Ca2+ Depression in Cardiac Myocytes: Role of Sarco/Endoplasmic Reticulum Ca2+ Pump.
Escalante, B; Flores-Tamez, V; Rios, A, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
morpholinesAny compound containing morpholine as part of its structure.
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency7.87580.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency7.87580.025120.237639.8107AID886; AID893
thioredoxin reductaseRattus norvegicus (Norway rat)Potency42.28410.100020.879379.4328AID488773; AID588453
ATAD5 protein, partialHomo sapiens (human)Potency29.08100.004110.890331.5287AID493107
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624146
regulator of G-protein signaling 4Homo sapiens (human)Potency18.88760.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.91250.035520.977089.1251AID504332
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.07940.00106.000935.4813AID943
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID1278458Upregulation of SOD in H2O2-induced mouse 661W cells at 50 to 100 uM by Cayman's superoxide dismutase assay2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID1278454Half life of compound in 0.5 M phosphate buffer at pH 6.5 at 25 degC by LC/MS analysis2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID1278459Induction of nitric oxide release in 50 mM phosphate buffer at pH 7.4 after 10 mins by Greiss assay2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID1278457Increase in number of mouse 661W cells at 10 to 50 uM after 24 hrs by MTT assay relative to vehicle control2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID1278453Half life of compound in 0.5 M phosphate buffer at pH 7.4 at 25 degC by LC/MS analysis2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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 (1,398)

TimeframeStudies, This Drug (%)All Drugs %
pre-199074 (5.29)18.7374
1990's651 (46.57)18.2507
2000's557 (39.84)29.6817
2010's107 (7.65)24.3611
2020's9 (0.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.36

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 Index21.36 (24.57)
Research Supply Index7.30 (2.92)
Research Growth Index5.33 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials35 (2.43%)5.53%
Reviews16 (1.11%)6.00%
Case Studies3 (0.21%)4.05%
Observational0 (0.00%)0.25%
Other1,387 (96.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]