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egtazic acid

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Description

Egtazic Acid: A chelating agent relatively more specific for calcium and less toxic than EDETIC ACID. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ethylene glycol bis(2-aminoethyl)tetraacetic acid : A diether that is ethylene glycol in which the hydrogens of the hydroxy groups have been replaced by 2-[bis(carboxymethyl)amino]ethyl group respectively. [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 CID6207
CHEMBL ID240390
CHEBI ID30740
SCHEMBL ID22901
MeSH IDM0007133

Synonyms (128)

Synonym
2-[2-[2-[2-(bis(carboxymethyl)amino)ethoxy]ethoxy]ethyl-(carboxymethyl)amino]acetic acid
nsc615010
nsc-615010
3,12-bis(carboxymethyl)-6,9-dioxa-3,12-diazatetradecane-1,14-dioic acid
2-[2-[2-[2-[bis(carboxymethyl)amino]ethoxy]ethoxy]ethyl-(carboxymethyl)amino]acetic acid
smr000059072
MLS000069445
ethyleneglycol-bis(beta-aminoethyl ether)-n,n1-tetra-acetic acid
glycoletherdiamine-n,n,n',n'-tetraacetic acid
ethylene glycol bis(aminoethyl ether)tetraacetate
acetic acid, (ethylenebis(oxyethylenenitrilo))tetra-
egtazic acid [usan:inn]
ethylene glycol tetraacetic acid
(ethylenebis(oxyethylenenitrilo))tetraacetic acid
ethylenebis(oxyethylenenitrilo)tetra(acetic acid)
1,2-bis(2-dicarboxymethylaminoethoxy)ethane
ethylene glycol bis(beta-aminoethyl ether)-n,n'-tetraacetic acid
acidum egtazicum [inn-latin]
acido egtazico [inn-spanish]
acide egtazique [inn-french]
ethylene glycol, di(2-(n,n-dicarboxylmethyl)amino)ethyl ether
c14h24n2o10
ethylene glycol bis(2-aminoethyl ether)tetraacetic acid
glycol-etherdiaminetetraacetic acid
brn 1717370
einecs 200-651-2
6,9-dioxa-3,12-diazatetradecanedioic acid, 3,12-bis(carboxymethyl)-
ethylenedioxybis(ethyleneamino)tetraacetic acid
nsc 615010
EU-0100512
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid, >=97.0%
h4egta
3,12-bis(carboxymethyl)-6,9-dioxa-3,12-diazatetradecanedioic acid
ethylene glycol bis(beta-aminoethyl ether)-n,n,n',n'-tetraacetic acid
ethylene glycol-o,o'-bis(2-aminoethyl)-n,n,n',n'-tetraacetic acid
2,2',2'',2'''-[ethane-1,2-diylbis(oxyethane-2,1-diylnitrilo)]tetraacetic acid
CHEBI:30740 ,
ethylene glycol bis(2-aminoethyl)tetraacetic acid
lopac-e-4378
NCGC00015416-01
LOPAC0_000512
D03967
egtazic acid (usan)
ethylene glycol bis(b-aminoethyl ether)-n,n,n',n'-tetraacetic acid
67-42-5
3,6-dioxaoctane-1,8-diamine-n,n,n',n'-tetraacetic acid
ethylene glycol bis(2-aminoethyl ether)-n,n,n',n'-tetraacetic acid
edga
6,9-dioxa-3,12-diazatetradecanedioic acid, 3,12-bis(carboxymethyl)- (9ci)
gedta
ebonta
[ethylenebis(oxyethylenenitrilo)]tetraacetic acid
1,2-bis(2-aminoethoxyethane)-n,n,n',n'-tetraacetic acid
acetic acid, [ethylenebis(oxyethylenenitrilo)]tetra- (6ci,8ci)
2,2'-ethylenedioxybis(ethylamine)-n,n,n',n'-tetraacetic acid
glycol ether diamine tetraacetic acid
EGTA ,
egtazic acid
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid, for molecular biology, >=97.0%
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid, bioxtra, >=97 .0%
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid
NCGC00093909-01
NCGC00093909-02
NCGC00015416-02
E 4378
egta; egtazic acid
1,2-bis[2-[bis(carboxymethyl)amino]ethoxy]ethane
glycoletherdiaminetetraacetic acid
E0805
NCGC00015416-04
CHEMBL240390
E0106
AKOS004910388
HMS3261H05
ethylenebis(oxyethylenenitrilo)tetraacetic acid
tox21_110141
cas-67-42-5
dtxsid2045151 ,
dtxcid0025151
BMSE001011
CCG-204603
NCGC00015416-03
acidum egtazicum
526u7a2651 ,
acido egtazico
unii-526u7a2651
acide egtazique
FT-0606293
LP00512
SCHEMBL22901
NCGC00015416-05
tox21_110141_1
egta [mi]
egtazic acid [inn]
egtazic acid [usan]
ethylene glycol bis(.beta.-aminoethyl ether)-n,n,n',n'-tetraacetic acid
ethyleneglycol bis-(2-aminoethyl)ether tetraacetic acid
ethylene glycol-bis(.beta.-aminoethyl ether)-n,n,n',n'-tetraacetic acid
glycoletherdiamine-tetraacetic acid
3,12-bis(carboxymethyl)-6,9-dioxa-3,12-diazatetradecane-1,14-dioic acid #
tox21_500512
NCGC00261197-01
ethylene glycol-bis(2-aminoethyl)-n,n,n',n'-tetraacetic acid
W-104715
ethylene glycol bis-(2-aminoethyl ether)tetraacetic acid
AC-31252
mfcd00004291
sr-01000075861
SR-01000075861-1
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid, >=98.0% (t)
ethylene glycol-bis(2-aminoethylether)-n,n,n',n'-tetraacetic acid, bioultra, for molecular biology, >=99.0% (t)
AS-72032
H10668
SY010980
ethylene glycol-bis(2-aminoethylether)-n,n,n inverted exclamation marka,n inverted exclamation marka-tetraacetic acid
1,2-bis[2-[bis(carboxymethyl)amino]ethoxy]ethane ; ethylene glycol-bis(2-aminoethylether)-n,n,n??,n??-tetraacetic acid
Q408437
egta, molecular biology grade - cas 67-42-5
2,11-bis(carboxymethyl)-5,8-dioxa-2,11-diazadodecane-1,12-dicarboxylic acid
ethylene glycol-o,o'-bis(2-aminoethyl)-n,n,n',n'-tetraacetic acid, egta
SDCCGSBI-0050496.P002
NCGC00015416-06
3,12-bis(carboxymethyl)-6,9-dioxa-3,12-diazatetra-decane-1,14-dioic acid (egta)
ethylenebis(oxyethylenenitrilo)tetraacet
ethylene glycol-bis(2-aminoethylether)-n,n,n,n-tetraacetic acid
HB4708
CS-0015171
HY-D0861

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Calcium chelating agents, such as ethylenediaminetetraacetate are toxic to urothelium."( Rationale for local toxicity of calcium chelators.
Cuvelier, C; Oosterlinck, W; Verbeeck, R; Vergauwe, D, 1992
)
0.28
" We propose that oxidative events contribute to the toxic mechanism of action of methyl mercury in isolated cerebellar granule neurons."( Oxidative mechanisms underlying methyl mercury neurotoxicity.
Sarafian, T; Verity, MA, 1991
)
0.28
"EGTA-treated rat serum was added to the culture medium and tested the toxic effect of EGTA on development of embryo using 11."( Embryotoxic effects of EGTA-induced hypocalcemic condition on cultured rat embryos.
Eto, K; Igarashi, T; Kitagawa, H; Ueno, K; Yokoyama, A, 1985
)
0.27
" None of the tested agents was able to reduce the toxic effects of triethyl lead."( On the toxic effects of tetraethyl lead and its derivatives on the chrysophyte Poterioochromonas malhamensis. IV. Influence of lead antidotes and related agents.
Röderer, G, 1983
)
0.27
" Contrary to their action in the toxic effect, both 100 microM amiloride and the intracellular loading of BAPTA failed to counteract the nontoxic effect of 1 microM ouabain."( Toxic and nontoxic effects of ouabain on the transmitter release from frog motor nerve terminals.
Enomoto, K; Hara, N; Ichinose, M; Maeno, T; Sawada, M, 1995
)
0.29
" Accordingly, intracellular hydrogen ion concentrations were measured in cultured hippocampal neurons with the fluorescent dye BCECF during and after toxic exposures."( Changes in intracellular pH associated with glutamate excitotoxicity.
Dubinsky, JM; Hartley, Z, 1993
)
0.29
" It is concluded that a) plasma membrane indicator dyes, not neutral red, might be better indicators of cytotoxicity occurring during cryopreservation; b) DMSO might be toxic to lysosomes during cryopreservation of cultured cells; and c) although [Ca+2]e can contribute to cytotoxicity, the presence of [Ca+2]e might not influence cryopreservation-induced cytotoxicity."( Extracellular calcium does not contribute to cryopreservation-induced cytotoxicity.
Baust, J; Danks, AM; Im, J; Isaacson, RL; Rhoads, LS; Van Buskirk, RG; Warner, A, 1993
)
0.29
"D-myo-Inositol hexakisphosphate (InsP6, phytate), a normal cellular constituent, was found to be toxic to neuronal perikarya when injected into the rat hippocampus."( Neuronal cytotoxicity of inositol hexakisphosphate (phytate) in the rat hippocampus.
Lees, GJ; Leong, W, 1996
)
0.29
" Reduced glutathione (GSH), adenosine-5'-triphosphate (ATP) and lipid peroxidation were investigated to evaluate the toxic effect of MDMA, in vitro, using freshly isolated rat hepatocytes."( 3,4-Methylenedioxymethamphetamine (ecstasy)-induced hepatotoxicity: effect on cytosolic calcium signals in isolated hepatocytes.
Beitia, G; Cenarruzabeitia, E; Cobreros, A; Sainz, L, 1999
)
0.3
" Relative to NO release, SNP is more toxic than SNAP, due to synergism of NO with cyanide released by SNP."( Role of calcium in nitric oxide-induced cytotoxicity: EGTA protects mouse oligodendrocytes.
Benjamins, JA; Boullerne, AI; Nedelkoska, L, 2001
)
0.31
" It is primarily considered as a neurotoxin but its other toxic manifestations are also well documented."( Pharmacological interventions of cyanide-induced cytotoxicity and DNA damage in isolated rat thymocytes and their protective efficacy in vivo.
Bhattacharya, R; Lakshmana Rao, PV, 2001
)
0.31
" Thus, the different toxicities may permit the selection of agents that enhance gene transfer with minimal adverse effects."( Safety and efficiency of modulating paracellular permeability to enhance airway epithelial gene transfer in vivo.
Coyne, CB; Gavett, SH; Haykal-Coates, N; Johnson, LG; Vanhook, MK, 2003
)
0.32
" 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
"In this study, the toxic effect of sanguinarine (SANG) on heart was studied with isolated cardiac muscle strip isolated from Wistar rat."( Induction of contracture and extracellular Ca2+ influx in cardiac muscle by sanguinarine: a study on cardiotoxicity of sanguinarine.
Cheng, HW; Cheng, YW; Hu, CM; Kang, JJ; Liao, JW, 2005
)
0.33
" While this process could occur at the expense of NO production, NO alone does play a toxic role, with its production leading to the formation of the toxicant peroxynitrite."( Nitric oxide-mediated toxicity in paraquat-exposed SH-SY5Y cells: a protective role of 7-nitroindazole.
Bravo-San Pedro, JM; Fuentes, JM; González-Polo, RA; Morán, JM; Niso-Santano, M; Ortiz-Ortiz, MA; Soler, G, 2009
)
0.35
" Diverse cell-specific toxic effects were observed, with C2C12 being relatively resistant to tungsten-alloy mediated toxic impact."( In vitro profiling of epigenetic modifications underlying heavy metal toxicity of tungsten-alloy and its components.
Caretti, G; Galdzicki, Z; Jaiswal, MK; Mears, D; Olsen, C; Verma, R; Xu, X, 2011
)
0.37
" It is also known that local anesthetics may exert analgesic effect and, rarely, some adverse effects on the central nervous system (CNS)."( Correlation between the increased release of catecholamines evoked by local anesthetics and their analgesic and adverse effects: Role of K(+) channel inhibition.
Azamfirei, L; Baranyi, M; Borbély, Z; Lazar, A; Sircuta, C; Vizi, ES, 2016
)
0.43
"Bacillus thuringiensis crystal (Cry) proteins, used for decades as insecticidal toxins, are well known to be toxic to certain insects, but not to mammals."( The role of membrane-bound metal ions in toxicity of a human cancer cell-active pore-forming toxin Cry41Aa from Bacillus thuringiensis.
Crickmore, N; Domanska, B; Fortea, E; Schwartz, JL; West, MJ, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" This study suggests that the endothelium plays a necessary role in PGF2 alpha potentiation of vasoconstrictor response, possibly through the release of an endothelial vasoconstrictor factor which probably increases the Ca2+ bioavailability for the contraction."( Endothelium and Ca2+ in the prostaglandin F2 alpha potentiation of vasoconstrictor responses.
Aristegui, PM; Enero, MA, 1990
)
0.28
"The bioavailability of endothelial nitric oxide (NO) is regulated by transition metals but their mechanisms of action on NO synthesis and degradation are not clearly understood."( [Transition metals and nitric oxide production in human endothelial cells].
Brunet, A; David-Dufilho, M; Devynck, J; Devynck, MA; Privat, C; Richard, MJ, 2001
)
0.31
" Presumed functions at the maternal-fetal interface are to proteolyze IGFBP-4 and thus increase IGF bioavailability locally in the placenta, to promote IGF-II-mediated trophoblast invasion into the maternal decidua, and to modulate IGF regulation of steroidogenesis and glucose and amino acid transport in the villous."( Pregnancy-associated plasma protein A proteolytic activity is associated with the human placental trophoblast cell membrane.
Giudice, LC; Overgaard, MT; Oxvig, C; Sun, IY, 2002
)
0.31
"The peptide hormone calcitonin is a potent inhibitor of osteoclastic resorption, but it is unstable and poorly absorbed following oral administration."( Regulation of osteoclasts by calcitonin and amphiphilic calcitonin conjugates: role of cytosolic calcium.
Dixon, SJ; Komarova, SV; Paige, LA; Shum, JB; Sims, SM, 2003
)
0.32
", regarding their bioavailability or potential pro-oxidant activity."( Reduction of paraquat-induced renal cytotoxicity by manganese and copper complexes of EGTA and EHPG.
Chatterjee, PK; Gard, PR; Hague, T; Naughton, DP; Samai, M, 2008
)
0.35
" However, extensive first-pass hepatic metabolism would limit the oral bioavailability of this compound."( In vitro intestinal absorption and first-pass intestinal and hepatic metabolism of cycloastragenol, a potent small molecule telomerase activator.
Chin, AC; Harley, CB; Ho, MK; Hu, Y; Ip, FC; Ip, NY; Lee, S; Pang, H; Wong, YH; Zhu, J, 2010
)
0.36
"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

ExcerptRelevanceReference
" Dose-response curves to acetylcholine, histamine, phenylephrine, and isoproterenol were similar for the muscle of either part of the colon."( Comparison of proximal and distal colonic muscle of the rabbit.
Cohen, S; Snape, WJ; Tucker, HJ, 1979
)
0.26
" The dose-response curve for this suppression was very similar to that for stimulation of inositol monophosphate (IP1) formation and for stimulation of the initial rise of [Ca2+]i elicited by carbachol."( Suppressive effect of carbachol on forskolin-stimulated neurite outgrowth in human neuroblastoma NB-OK1 cells.
Nakagawa-Yagi, Y; Nakamura, H; Saito, Y; Takada, Y, 1992
)
0.28
" 3) Decreasing K+ efflux using K+ channel blockers (4-aminopyridine, quinine, sparteine) inhibited histamine release in a dose-response manner."( Regulation of human basophil activation. II. Histamine release is potentiated by K+ efflux and inhibited by Na+ influx.
Beauvais, F; Benveniste, J; Burtin, C; Hieblot, C; Inoue, I; Shimahara, T, 1992
)
0.28
" In permeabilized acini, mepacrine shifted the dose-response curve for calcium to the right by a factor 2 and inhibited the release of amylase stimulated by GTPrS."( Inhibition by mepacrine and amylase secretion from intact and permeabilized rat pancreatic acini.
Dehaye, JP; Gomez, F; Grosfils, K, 1992
)
0.28
" Comparison of the dose-response curve for oxytocin in Ca(2+)-free solution and that in the medium with 1 microM Ca2+ showed that the inhibition by Ca2+ is non-competitive."( Ca(2+)-dependent inhibition of Ca(2+)-independent contraction in uterine smooth muscle.
Gokita, T; Ishine, T; Matsuo, K; Miyauchi, Y; Uchida, MK, 1992
)
0.28
" Dose-response curves demonstrated that H-7 is the most effective among the inhibitors, and the transepithelial resistance was 70% of control up to 1 h after calcium removal."( Protein kinase inhibitors prevent junction dissociation induced by low extracellular calcium in MDCK epithelial cells.
Citi, S, 1992
)
0.28
" Millimolar concentration of ATP, which is present physiologically, will shift the dose-response relation of IP3 toward the higher IP3 concentration and enhance the maximal effect of IP3."( Effects of adenine nucleotides on inositol 1,4,5-trisphosphate-induced calcium release in vascular smooth muscle cells.
Iino, M, 1991
)
0.28
" The lipopeptides N-palmitoyl-(S)-[2,3-bis(palmitoyloxy)-(2RS)- propyl]-(R)-cysteinylalanylglycine, N-palmitoyl-(S)-[2,3-bis(palmitoyloxy)- (2RS)-propyl]-(R)-cysteinylseryl-lysyl-lysyl-lysine and (S)-(1,2- dicarboxyhexadecyl)ethyl-N-palmitoylcysteinylseryl-lysyl-lys yl-lysine stimulated both parameters, but the maximal effects on nitrite formation and the shape of the dose-response curves did not parallel the effects on [Ca2+]i."( Induction and activity of NO synthase in bone-marrow-derived macrophages are independent of Ca2+.
Bessler, W; Busse, R; Hauschildt, S; Kohler, J; Lückhoff, A; Mülsch, A, 1990
)
0.28
"Prostaglandin F2 alpha (PGF2 alpha), at a concentration that did not induce vascular contraction (10(-9) and 10(-10) M), potentiated the dose-response curves to norepinephrine (NE) in rat mesenteric ring segments only when the endothelium was present."( Endothelium and Ca2+ in the prostaglandin F2 alpha potentiation of vasoconstrictor responses.
Aristegui, PM; Enero, MA, 1990
)
0.28
" The La dose-response curves for H influx and for Ca efflux were similar [50% inhibitory concentration (IC50) = approximately 5 microM] in intact red blood cells."( Proton fluxes associated with the Ca pump in human red blood cells.
Milanick, MA, 1990
)
0.28
" A dose-response experiment with phytohemagglutinin demonstrated that similar concentrations of mitogen could induce both mitogenesis and the phosphodiesterase."( Induction of a calcium/calmodulin-dependent phosphodiesterase during phytohemagglutinin-stimulated lymphocyte mitogenesis.
Clark, DJ; Hirsch, KM; Holcombe, VN; Hurwitz, MY; Hurwitz, RL, 1990
)
0.28
" The dose-response relationships of this effect were measured by equilibrating cell aliquots with various Ca2+-EGTA buffers, preparing membrane vesicles (in the absence of Ca2+ ions), and assaying them for amiloride-sensitive Na+ permeability."( Ca2+-induced down-regulation of Na+ channels in toad bladder epithelium.
Asher, C; Garty, H, 1986
)
0.27
" The dose-response relations gave a Hill coefficient of approximately 1 for Mg2+ block and approximately 2 for Na+ block."( Voltage-dependent magnesium block of adenosine-triphosphate-sensitive potassium channel in guinea-pig ventricular cells.
Horie, M; Irisawa, H; Noma, A, 1987
)
0.27
" Carbachol-induced PKC translocation was concentration-dependent, with a biphasic dose-response curve yielding approximate EC50 values of 10(-6) M and 10(-4) M for the high- and low-affinity components, respectively."( Nicotinic and muscarinic agonists stimulate rapid protein kinase C translocation in PC12 cells.
Kiyasu, E; Messing, RO; Sneade, AB; Stevens, AM, 1989
)
0.28
" Dose-response curves to calcium in SHR aortae treated with 10(-3) mol/l ouabain were shifted to the left of those in WKY."( Calcium and contractile responses to ouabain and potassium-free solution in aortae from spontaneously hypertensive rats.
Lamb, FS; Moreland, RS; Webb, RC, 1988
)
0.27
" The exposure of FRTL-5 cells to physiological thyrotropin concentrations enhances the effect on cytosolic Ca2+ level induced by norepinephrine in vitro; the shape of the dose-response curve indicates a cooperative effect of the thyrotropin and norepinephrine."( Association of the changes in cytosolic Ca2+ and iodide efflux induced by thyrotropin and by the stimulation of alpha 1-adrenergic receptors in cultured rat thyroid cells.
Axelrod, J; Corda, D; Kohn, LD; Luini, A; Marcocci, C, 1985
)
0.27
" Investigations of the dose-response relationship of the effect of dexamethasone on GH mRNA performed under the same conditions showed that at dexamethasone concentrations that yielded a significant stimulation of GH mRNA (10 nM or greater), Ca2+ (0."( Glucocorticoid stimulation of growth hormone messenger ribonucleic acid levels in GH3 cells is inhibited by calcium but not by somatostatin.
Bancroft, C; Gick, GG, 1987
)
0.27
" 258, 5103-5109) but did not affect the dose-response curves for norepinephrine-induced Ca2+ mobilization and phosphorylase activation in these cells."( Studies on the hepatic alpha 1-adrenergic receptor. Modulation of guanine nucleotide effects by calcium, temperature, and age.
Blackmore, PF; Charest, R; Exton, JH; Lynch, CJ, 1985
)
0.27
" The first response, most notably involving a decrease in phosphatidylinositol content, was (a) observed at lower carbachol concentrations in dose-response studies, (b) inhibited by incubation in Ca2+-free media containing 1 mM EGTA, (c) associated with increases in inositol monophosphate production, and (d) provoked by all tissue secretagogues (carbachol, cholecystokinin, secretin, insulin, dibutyryl cAMP and the ionophore A23187), regardless of whether their mechanism of action primarily involved Ca2+ mobilization or cAMP generation."( Phosphatidylinositol hydrolysis and phosphatidylinositol 4',5-diphosphate hydrolysis are separable responses during secretagogue action in the rat pancreas.
Davis, JS; Farese, RV; Larson, RE; Orchard, JL; Sabir, MA, 1985
)
0.27
" The GH responses to the combined addition of TRH with all doses of GRF or DBcAMP were fully additive, causing parallel elevations of the dose-response curves."( TRH and GRF stimulate release of growth hormone through different mechanisms.
Szabo, M, 1986
)
0.27
" Isoproterenol, a known relaxant of these cells, caused a small decrease in Cai2+ (approximately 40 nM) below rest, when applied in maximal dosage (10(-4) M)."( Calcium transients and resting levels in isolated smooth muscle cells as monitored with quin 2.
Fay, FS; Williams, DA, 1986
)
0.27
" The dose-response curves for 45Ca uptake and release were identical to those of the hormonally evoked [Ca2+]i increase."( Agonist-sensitive calcium pool in the pancreatic acinar cell. I. Permeability properties.
Fimmel, CJ; Muallem, S; Pandol, SJ; Schoeffield, MS, 1988
)
0.27
"8 microM) was repeatedly dosed with acetylcholine (ACh, 10 microM)."( The relaxant and spasmogenic effects of some xanthine derivatives acting on guinea-pig isolated trachealis muscle.
Boyle, JP; Cortijo, J; Curtis-Prior, PB; Davies, JM; Foster, RW; Hofer, P; Small, RC, 1988
)
0.27
" This effect was inhibited by EGTA and had a dose-response curve identical to that for IP3-induced Ca2+ release, which suggests that the IP3-induced secretion is mediated by the released Ca2+ and not directly by the IP3."( A role for inositol triphosphate in intracellular Ca2+ mobilization and granule secretion in platelets.
Brass, LF; Joseph, SK, 1985
)
0.27
" The dose-response relationships were similar for bethanechol stimulation of 45Ca2+ uptake and amylase release, whereas stimulation of 45Ca2+ washout reached a maximum at a higher concentration of bethanechol."( Calcium fluxes in isolated pancreatic acini: effects of secretagogues.
Dormer, RL; Licko, V; Poulsen, JH; Williams, JA, 1981
)
0.26
" This secretory response was normal as judged by cell ultrastructure and FMLP dose-response relationships."( FMLP-induced enzyme release from neutrophils: a role for intracellular calcium.
Chandler, D; Meusel, G; Schumaker, E; Stapleton, C, 1983
)
0.27
" The effect that the observed degree of hydration (2-4%) has on calculated values for [Ca2+] in Ca-EGTA solutions is described with reference to a theoretical dose-response relationship."( EGTA purity and the buffering of calcium ions in physiological solutions.
Miller, DJ; Smith, GL, 1984
)
0.27
" Protoveratrine A increased the uptake of 22Na+ into the slices with a similar dose-response curve to that found for gamma-aminobutyrate release."( The role of Ca2+ in the protoveratrine-induced release of gamma-aminobutyrate from rat brain slices.
Minchin, MC, 1980
)
0.26
" A dose-response curve was obtained; 5,5'-difluoro-BAPTA was the most potent analogue."( Introduction of calcium buffers into the cytosol of Dictyostelium discoideum amoebae alters cell morphology and inhibits chemotaxis.
Schlatterer, C; Unterweger, N, 1995
)
0.29
" In the presence of the inhibitory protein fraction, ethanol stimulated Na+, K(+)-ATPase activity in EGTA-treated membranes with a dose-response like that observed with the crude (no EGTA) synaptosomes."( Stimulation of synaptosomal Na+,K(+)-ATPase by ethanol: possible involvement of an isozyme-specific inhibitor of Na+,K(+)-ATPase.
Foley, TD; Rhoads, DE, 1994
)
0.29
" The dose-response for calcium release induced by sphingosine-1-phosphate correlated closely with the concentration required for stimulation of DNA synthesis."( Sphingosine-1-phosphate, a putative second messenger, mobilizes calcium from internal stores via an inositol trisphosphate-independent pathway.
Brooker, G; Mattie, M; Spiegel, S, 1994
)
0.29
" The dose-response relation between ATP and the UDP-induced KATP-channel activity was shifted to the right in the presence of Mg2+ (2 mM)."( Regulation of ATP-sensitive K+ channels by ATP and nucleotide diphosphate in rabbit portal vein.
Kamouchi, M; Kitamura, K, 1994
)
0.29
" While there was a clear effect of dBcAMP-induced differentiation on the maximal NE-induced PI-response, no effect on the dose-response relationship was detectable, resulting in similar EC50-values for astrocytes cultured either in the absence or presence of dBcAMP."( Dibutyryl cyclic AMP-induced morphological differentiation of rat brain astrocytes increases alpha 1-adrenoceptor induced phosphoinositide breakdown by a mechanism involving protein synthesis.
Fahrig, T; Sommermeyer, H, 1993
)
0.29
" Both responses were dependent on the concentration of thrombin, displaying a sigmoidal dose-response pattern."( Intracellular calcium mobilization and activation of the Na+/H+ exchanger in platelets.
Botey, A; Cases, A; Gaya, J; Poch, E; Revert, L; Rivera, F, 1993
)
0.29
" The priming effect of MCAF was maximal within 5 minutes of preincubation, and the dose-response curves for priming were identical to those for triggering of an increase in [Ca2+]i."( Activation and priming of human monocytes by monocyte chemotactic activating factor: cooperation with other inflammatory cytokines and close association between an increase in cytoplasmic free Ca2+ and intracellular acidification.
Azuma, EK; Kasahara, T; Kitagawa, S; Matsushima, T; Mizoguchi, H; Saito, M; Takaku, F; Yuo, A, 1996
)
0.29
" Dose-response studies were performed using previously reported inhibitors of cytosolic calcium oscillation mechanisms."( The mechanisms underlying Bay K 8644-stimulated phasic myometrial contractions.
Chien, EK; Phillippe, M; Saunders, T,
)
0.13
" Rats were dosed concomitantly with indomethacin (40 mg/kg, subcutaneously) and an amino or pyridinyl bisphosphonate (orally at."( Nonclinical model for assessing gastric effects of bisphosphonates.
Berman, SK; Blank, MA; Ems, BL; Gibson, GW; Myers, WR; Phipps, RJ; Smith, PN, 1997
)
0.3
" When expressed in Spodoptera frugiperda Sf9 cells the alpha2A subtype showed only inhibition of forskolin-stimulated cAMP production when activated by norepinephrine (NE), whereas the alpha2B subtype displayed a biphasic dose-response curve with inhibition at low concentrations of NE and a potentiation at higher concentrations."( The second intracellular loop of the alpha2-adrenergic receptors determines subtype-specific coupling to cAMP production.
Akerman, KE; Jansson, CC; Näsman, J, 1997
)
0.3
"Harringtonine (HT), an anticancer drug with high chemotherapeutic efficiency to human chronic granulocytic/myelomonocytic leukemia, has been reported to rapidly induce apoptosis in HL-60 cells in a wide scope/range of dosage by investigators from our lab and others."( Intracellular calcium distribution in apoptosis of HL-60 cells induced by harringtonine: intranuclear accumulation and regionalization.
Fang, M; Li, N; Wang, L; Xue, S; Zhang, H, 1998
)
0.3
" 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
") pretreatment with calcium and thapsigargin, which increase intracellular calcium, reduced [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin (DAMGO)-induced antinociception by shifting its dose-response curve to the right."( Role of intracellular calcium in modification of mu and delta opioid receptor-mediated antinociception by diabetes in mice.
Kamei, J; Nagase, H; Ohsawa, M, 1998
)
0.3
" In contrast, agonist-stimulated coupling was diminished (desensitization), resulting in a substantially flattened morphine dose-response curve."( Calmodulin regulation of basal and agonist-stimulated G protein coupling by the mu-opioid receptor (OP(3)) in morphine-pretreated cell.
Sadée, W; Surratt, CK; Wang, D, 2000
)
0.31
" Dose-response curves were constructed for the chorion cell cultures with CRH or 8-bromo-cAMP."( Regulation of 15-hydroxy prostaglandin dehydrogenase by corticotrophin-releasing hormone through a calcium-dependent pathway in human chorion trophoblast cells.
Challis, JR; McKeown, KJ, 2003
)
0.32
" At a sub-effective dose, pargyline could cause a leftward shift in the dose-response curve of 5-HTP-induced antinociception."( L-type calcium channel blockers enhance 5-HTP-induced antinociception in mice.
Chen, B; Han, R; Li, JX; Liang, JH; Lu, Y; Wang, XH; Ye, XF; Zhang, P, 2004
)
0.32
" The kinetics and colorimetric dose-response profile of DP-109 indicate that the compound inserts into the lipid bilayers rather than being localized at the bilayer surface."( Membrane interactions and metal ion effects on bilayer permeation of the lipophilic ion modulator DP-109.
Angel, I; Friedman, J; Jelinek, R; Kolusheva, S, 2005
)
0.33
" ACh and Ca2+ dose-response studies demonstrated that NO3- solution does not shift their dose-response curves, and ATP depletion studies by dinitrophenol or anoxia demonstrated that exposure of NO3- solution prior to ATP depletion induced an enhanced initial phase followed by a sustained phase, whereas exposure of NO3- solution after ATP depletion induced only a sustained phase."( [Cl-]i modulation of Ca2+-regulated exocytosis in ACh-stimulated antral mucous cells of guinea pig.
Fujiwara, S; Kato, M; Katsu, K; Kubota, T; Nakahari, T; Shimamoto, C; Umegaki, E, 2007
)
0.34
" A dose-response relationship study using validated viability assays revealed that two MAC drugs, DP-b99 and DP-460, were cytotoxic for these parasites in vitro."( Membrane active chelators as novel anti-African trypanosome and anti-malarial drugs.
Bakshi, RP; Friedman, JE; Grab, DJ; Nenortas, E; Nikolskaia, OV; Shapiro, TA, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
chelatorA ligand with two or more separate binding sites that can bind to a single metallic central atom, forming a chelate.
[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 (3)

ClassDescription
tetracarboxylic acidAn oxoacid containing four carboxy groups.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
dietherA polyether in which the number of ether linkages is 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]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency31.54790.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency1.99530.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency1.99530.025120.237639.8107AID886
endonuclease IVEscherichia coliPotency63.09570.707912.432431.6228AID1708
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.04220.006038.004119,952.5996AID1159521
arylsulfatase AHomo sapiens (human)Potency0.12001.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.30240.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency100.00000.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency95.283423.934123.934123.9341AID1967
D(1A) dopamine receptorHomo sapiens (human)Potency0.58040.02245.944922.3872AID488982
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency14.11470.005612.367736.1254AID624044
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (56)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID303066Inhibition of Plasmodium falciparum FCB2 merozoite invasion of human erythrocytes at 50 mM2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Identifying merozoite surface protein 4 and merozoite surface protein 7 Plasmodium falciparum protein family members specifically binding to human erythrocytes suggests a new malarial parasite-redundant survival mechanism.
AID409443Inhibition of aph8 phosphorylation in Streptomyces coelicolor cell lysate assessed as [32Pi] incorporation into aph8 at 500 nM by microplate scintillation counter relative to control2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles.
AID479152Antiplasmodial activity against Plasmodium falciparum FCB2 assessed as inhibition of merozoite invasion of human RBCs at 1.9 mg/mL after 18 hrs using hydroethidine staining by flow cytometry2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Conserved high activity binding peptides are involved in adhesion of two detergent-resistant membrane-associated merozoite proteins to red blood cells during invasion.
AID513852Antiplasmodial activity against Plasmodium falciparum FCB2 assessed as inhibition of merozoite invasion of human erythrocytes at 1.9 mg/mL after 18 hrs using hydroethidine staining by flow cytometry2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Well-defined regions of the Plasmodium falciparum reticulocyte binding protein homologue 4 mediate interaction with red blood cell membrane.
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 (9,782)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903253 (33.25)18.7374
1990's3458 (35.35)18.2507
2000's2233 (22.83)29.6817
2010's773 (7.90)24.3611
2020's65 (0.66)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.71

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 Index16.71 (24.57)
Research Supply Index9.21 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.71)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (0.11%)5.53%
Reviews80 (0.80%)6.00%
Case Studies5 (0.05%)4.05%
Observational0 (0.00%)0.25%
Other9,925 (99.04%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]