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calcimycin

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Description

Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11957499
CHEMBL ID1256686
CHEBI ID107643
SCHEMBL ID17390959
MeSH IDM0000001

Synonyms (62)

Synonym
HMS3267F15
BRD-K41431477-001-05-6
LOPAC0_000317
EU-0100317
calcium ionophore a23187, >=98% (tlc), powder
einecs 258-084-1
a 23187
4-benzoxazolecarboxylic acid, 5-(methylamino)-2-((3,9,11-trimethyl-8-(1-methyl-2-oxo-2-(1h-pyrrol-2-yl)ethyl)-1,7-dioxaspiro(5.5)undec-2-yl)methyl)-, (6s-(6alpha(2s*,3s*),8beta(r*),9beta,11alpha))-
calcimycin
calcimycin a23187
MLS001056783 ,
smr000326983
NCGC00025064-02
NCGC00025064-03
CHEBI:107643
C 7522
a23187; calcium ionophore a23187
NCGC00025064-04
calcium ionophore a23187
HMS3260P16
CHEMBL1256686
antibiotic a-23187
5-(methylamino)-2-(((2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-((s)-1-oxo-1-(1h-pyrrol-2-yl)propan-2-yl)-1,7-dioxaspiro[5.5]undecan-2-yl)methyl)benzo[d]oxazole-4-carboxylic acid
CCG-204412
HMS2231L17
37h9vm9wzl ,
unii-37h9vm9wzl
calcium ionophore iii
4-benzoxazolecarboxylicacid,5-(methylamino)-2-[[(2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-[(1s)-1-methyl-2-oxo-2-(1h-pyrrol-2-yl)ethyl]-1,7-dioxaspiro[5.5]undec-2-yl]methyl]-
LP00317
4-benzoxazolecarboxylic acid, 5-(methylamino)-2-(((2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-((1s)-1-methyl-2-oxo-2-(1h-pyrrol-2-yl)ethyl)-1,7-dioxaspiro(5.5)undec-2-yl)methyl)-
calcimycin [mi]
5-(methylamino)-2-(((2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-((1s)-1-methyl-2-oxo-2-(1h-pyrrol-2-yl)ethyl)-1,7-dioxaspiro(5.5)undec-2-yl)methyl)-4-benzoxazolecarboxylic acid
tox21_500317
NCGC00261002-01
HIYAVKIYRIFSCZ-CYEMHPAKSA-N
bdbm44170
5-(methylamino)-2-[[(2s,3r,5r,6s,8r,9r)-3,5,9-trimethyl-2-[(2s)-1-oxo-1-(1h-pyrrol-2-yl)propan-2-yl]-1,7-dioxaspiro[5.5]undecan-8-yl]methyl]-1,3-benzoxazole-4-carboxylic acid
2-[[(2s,3r,5r,6s,8r,9r)-2-[(1s)-2-keto-1-methyl-2-(1h-pyrrol-2-yl)ethyl]-3,5,9-trimethyl-1,7-dioxaspiro[5.5]undecan-8-yl]methyl]-5-(methylamino)-1,3-benzoxazole-4-carboxylic acid
5-(methylamino)-2-[[(2s,3r,5r,6s,8r,9r)-3,5,9-trimethyl-2-[(2s)-1-oxidanylidene-1-(1h-pyrrol-2-yl)propan-2-yl]-1,7-dioxaspiro[5.5]undecan-8-yl]methyl]-1,3-benzoxazole-4-carboxylic acid
cid_11957499
a23187, free acid
5-(methylamino)-2-[[2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-[(1s)-1-methyl-2-oxo-2-(1h-pyrrol-2-yl)-ethyl]-1,7-dioxaspiro[5.5]undec-2-yl]methyl]-4-benzoxazolecarboxylic acid
AKOS024456478
DTXSID1040405
SCHEMBL17390959
sr-01000597415
SR-01000597415-1
calcium ionophore iii, selectophore(tm), function tested
SR-01000075434-1
SR-01000075434-5
sr-01000075434
Q3650244
79646-37-0
rel-calcimycin
SDCCGSBI-0050305.P002
NCGC00025064-09
CS-0006888
HY-N6687
calimycin;antibiotic a-23187
antibiotic a-23187a-23187
4-benzoxazolecarboxylic acid, 5-(methylamino)-2-[[(2r,3r,6s,8s,9r,11r)-3,9,11-trimethyl-8-[(1s)-1-methyl-2-oxo-2-(1h-pyrrol-2-yl)ethyl]-1,7-dioxaspiro[5.5]undec-2-yl]methyl]-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Ionophore A23187 (2 X 10(-5)M) was moderately toxic to normal but not to leukemic lymphocytes and caused the transformation of both types of cells."( Inhibition by ionophore A23187 of the cytotoxicity of vincristine, colchicine and X-rays to leukemic lymphocytes.
Schrek, R; Stefani, SS, 1976
)
0.26
" Nonetheless, preinduction of heat shock proteins was associated with protection from toxic concentrations of glutamate."( The stress protein response in cultured neurons: characterization and evidence for a protective role in excitotoxicity.
Chan, PH; Lowenstein, DH; Miles, MF, 1991
)
0.28
"Rat and canine hepatocyte suspensions were exposed to toxic concentrations of ethyl methanesulfonate (EMS) and ionophore A-23187 in the presence and absence of extracellular calcium (Ca2+) and alpha-tocopheryl succinate (alpha-TS)."( Alpha-tocopheryl succinate protects hepatocytes from chemical-induced toxicity under physiological calcium conditions.
Fariss, MW; Merson, MH; O'Hara, TM, 1989
)
0.28
" We conclude that while DBE is highly toxic to rat hepatocytes, hypoxia does not appear to contribute to the toxicity of DBE, even under conditions of low oxygen concentrations."( Toxicity of 1,2-dibromoethane in primary hepatocyte monolayer cultures: lack of dependence on oxygen concentration.
Costa, AK; Trudell, JR, 1988
)
0.27
" In parallel experiments, the calcium ionophore A23187 was not toxic in the presence of calcium."( The neurotoxicity of excitatory amino acids is produced by passive chloride influx.
Rothman, SM, 1985
)
0.27
" This indicates that the effect of the ionophore was not due to nonspecific release of toxic products from the effector cells."( A role for calcium-activated calmodulin in murine nonspecific cell-mediated cytotoxicity.
Cain, CA; Fan, S; Tompkins, WA; Weltzin, R, 1983
)
0.27
" Only tyrphostin B46, an inhibitor of tyrosine kinase, attenuated the toxic LPS effect, suggesting that the LPS-induced cytotoxicity in bovine aortic endothelial cell cultures is mediated by a specific tyrosine kinase, and not by NO or oxygen radicals."( Investigations into the mechanism of toxicity of lipopolysaccharide (LPS) in bovine aortic endothelial cells.
Loose, R; Melzig, MF, 1995
)
0.29
" Thus, these results show that statin, which is expressed at low levels in embryonic rat cultured hippocampal neurons, is rapidly overexpressed following a toxic insult produced by the activation of the NMDA receptor."( Statin, a marker of cell cycle arrest, is overexpressed during the early phase of delayed NMDA toxicity in hippocampal cell cultures.
Alonso, R; Boksa, P; Buisson, N; Diorio, J; O'Donnell, D; Poirier, J; Quirion, R, 1994
)
0.29
" It has been shown that a vasoactive role may be partially responsible for the toxic effects of CN."( The effects of EDRF/NO releasers or calcium ionophore A23187 on cyanide toxicity in mice.
Baskin, SI; Lempka, JC; Nealley, EW, 1996
)
0.29
"Although an excess intake of fluoride has been reported to cause skeletal fluorosis, very little is known about the mechanism of adverse effects of fluoride on bone."( Fluoride mediates apoptosis in osteosarcoma UMR 106 and its cytotoxicity depends on the pH.
Ando, M; Hirano, S, 1997
)
0.3
"The sea nettle jellyfish toxin (SNTX), which contains several polypeptides, was highly toxic to human hepatocytes."( Toxicity of sea nettle toxin to human hepatocytes and the protective effects of phosphorylating and alkylating agents.
Burnett, JW; Cao, CJ; Eldefrawi, AT; Eldefrawi, ME; Menking, DE; Mioduszewski, RJ; Valdes, JJ, 1998
)
0.3

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic studies indicate that after oral dosing L-680,833 is bioavailable in rats and rhesus monkeys."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
"RBx 7796, a 5-lipoxygenase inhibitor, was evaluated in in vivo efficacy models, in vitro ADME and in vivo pharmacokinetic models."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" Pharmacokinetic profile of RBx 7796 was also determined in rat and dog."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" The molecule also demonstrated acceptable pharmacokinetic profile warranting further development."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" In the present study, we used a two-step method combined with calcium ionophore to induce DC from cord blood (CB) or normal human bone marrow (BM) CD34+ progenitor cells."( Generation of functional and mature dendritic cells from cord blood and bone marrow CD34+ cells by two-step culture combined with calcium ionophore treatment.
Abe, T; Aizawa, Y; Furukawa, T; Fuse, I; Kanazawa, N; Liu, A; Narita, M; Nikkuni, K; Takahashi, M; Toba, K; Zheng, Z, 2002
)
0.31
" To increase the efficiency of interspecies somatic cell nuclear transfer, in the present study we introduced a method of whole cell intracytoplasmic injection (WCICI) combined with chemical enucleation into panda-rabbit nuclear transfer and assessed the effects of this method on the enucleation rate of rabbit oocytes and the in vitro development and spindle structures of giant panda-rabbit reconstructed embryos."( The effects of chemical enucleation combined with whole cell intracytoplasmic injection on panda-rabbit interspecies nuclear transfer.
Chen, DY; Jiang, MX; Liu, SZ; Sun, QY; Yang, CX; Zhang, LS; Zheng, YL, 2004
)
0.32

Bioavailability

ExcerptReferenceRelevance
" By introduction of selective enzyme inhibitors, it was determined that the bioavailability of each mediator class occurred without regulatory effects on the others."( Pharmacologic regulation of mediator generation and release from the murine bone marrow derived mast cell.
Austen, KF; Lewis, RA; Robin, JL, 1985
)
0.27
" Oral nafazatrom is ineffective as a 5-lipoxygenase inhibitor in man, probably because of poor bioavailability after administration."( Oral nafazatrom in man: effect on inhaled antigen challenge.
Dollery, CT; Fuller, RW; Maltby, N; Philipp, E; Richmond, R; Ritter, W; Taylor, GW, 1987
)
0.27
" Such measurements, combined with bioavailability data from other species, may be useful for predicting biochemical activity in man."( Assessment of the in vivo biochemical efficacy of orally active leukotriene biosynthesis inhibitors.
Black, C; Brideau, C; Chan, C; Ford-Hutchinson, A; Frenette, R; Tagari, P, 1993
)
0.29
" Bioavailability studies show that conversion to piroxicam is about 100%, 90%, 70%, and 50% in these four species, respectively."( Ampiroxicam, an anti-inflammatory agent which is a prodrug of piroxicam.
Carty, TJ; Falkner, FC; Marfat, A; Moore, PF; Twomey, TM; Weissman, A, 1993
)
0.29
" This oral bioavailability is reflected by the inhibition (i) of tissue damage elicited in hamster lungs by intratracheal instillation of human PMNE and (ii) enzyme released from human PMN stimulated after their transfer into the pleural cavity of mice."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
" Absolute bioavailability of the parent compound was 50%."( A prodrug of a 2,6-disubstituted 4-(2-arylethenyl)phenol is a selective and orally active 5-lipoxygenase inhibitor.
Farina, PR; Graham, AG; Gundel, RH; Hattox, SE; Homon, CA; Lazer, ES; Riska, PS; Wegner, CD, 1993
)
0.29
" This may represent a therapeutic strategy for vascular diseases characterized by decreased bioavailability of NO."( Adventitial gene transfer of recombinant endothelial nitric oxide synthase to rabbit carotid arteries alters vascular reactivity.
Barber, DA; Crotty, TB; Gloviczki, P; Katusic, ZS; Kullo, IJ; Mozes, G; O'Brien, T; Schwartz, RS, 1997
)
0.3
" However, when purified cells were preincubated with SNP in the presence of 5 mM N-acetylcysteine (NAC), increasing the bioavailability of NO, the downregulation was recovered."( Exogenous nitric oxide regulates the degranulation of human basophils and rat peritoneal mast cells.
Hirai, K; Iida, M; Iikura, M; Koshino, T; Morita, Y; Takaishi, T; Yamada, H, 1998
)
0.3
" Vascular NO bioavailability as assessed with ESR spectroscopy using iron-thiocarbamate as a trap for NO was significantly reduced in tolerant vessels."( Effects of long-term nitroglycerin treatment on endothelial nitric oxide synthase (NOS III) gene expression, NOS III-mediated superoxide production, and vascular NO bioavailability.
Duncker, L; Förstermann, U; Hartmann, M; Hink, U; Li, H; Matheis, E; Meinertz, T; Mollnau, H; Münzel, T; Oelze, M; Skatchkov, M; Warnholtz, A, 2000
)
0.31
" These results suggest a time and biphasic dose effect of nicotine treatment on endothelium-dependent responses that may be related to bioavailability of NO."( Time and dose effect of transdermal nicotine on endothelial function.
Bonde, S; Boston, US; Clouse, WD; Hurt, RD; Miller, VM; Rud, KS; Severson, SR; Tonnessen, BH, 2000
)
0.31
" A hallmark of endothelial dysfunction is a deficiency in production or bioavailability of vascular nitric oxide (NO)."( Glucose scavenging of nitric oxide.
Brodsky, SV; Dharia, N; Goligorsky, MS; Gross, SS; Morrishow, AM, 2001
)
0.31
" Conclusion, fluvastatin, a HMG-CoA reductase inhibitor, retards the initiation of atherosclerosis formation through the improvement of NO bioavailability by both up-regulation of eNOS mRNA and decrease of O(2)(-) production in vascular endothelial cells, and this means that part of the anti-atherosclerotic effect of fluvastatin may be due to nonlipid factors."( A HMG-CoA reductase inhibitor possesses a potent anti-atherosclerotic effect other than serum lipid lowering effects--the relevance of endothelial nitric oxide synthase and superoxide anion scavenging action.
Asai, Y; Hayashi, T; Iguchi, A; Jayachandran, M; Kano, H; Matsui, H; Sumi, D; Thakur, NK, 2001
)
0.31
"N-acetyl-L-cysteine exerts direct anti-aggregating effects through an increased bioavailability of platelet nitric oxide."( N-acetyl-L-cysteine exerts direct anti-aggregating effect on human platelets.
Anfossi, G; Cavalot, F; Massucco, P; Mattiello, L; Russo, I; Trovati, M, 2001
)
0.31
" The present study tests the hypothesis that HOCl decreases nitric oxide (NO) bioavailability in the vasculature of Sprague-Dawley rats."( Endothelial dysfunction is induced by proinflammatory oxidant hypochlorous acid.
Darley-Usmar, V; Eiserich, JP; Kelpke, S; Ma, W; Parks, DA; Patel, R; White, CR; Zhang, C; Zhou, F, 2001
)
0.31
" These results suggest that prolonged exposure of rabbits to oral arsenate may impair the bioavailability of BH(4) in endothelial cells and, as a consequence, disrupt the balance between NO and O2(."( A potential mechanism for the impairment of nitric oxide formation caused by prolonged oral exposure to arsenate in rabbits.
Hayashi, T; Horiguchi, S; Itoh, K; Kumagai, Y; Nikaido, M; Pi, J; Shimojo, N; Sun, G; Sun, Y; Waalkes, MP; Yamamoto, M; Yamauchi, H, 2003
)
0.32
" Hyperhomocysteinemia impairs endothelial function, in part due to a diminished bioavailability of BH4 with resultant uncoupling of nitric oxide synthase."( Tetrahydrobiopterin attenuates homocysteine induced endothelial dysfunction.
Badiwala, MV; Dhillon, B; Li, SH; Maitland, A; Rao, V; Verma, S, 2003
)
0.32
" The mechanisms by which NADPH oxidase-derived radicals mediate the cerebrovascular dysfunction involve reduced bioavailability of nitric oxide."( NADPH-oxidase-derived reactive oxygen species mediate the cerebrovascular dysfunction induced by the amyloid beta peptide.
Anrather, J; Carlson, GA; Frys, K; Iadecola, C; Park, L; Pitstick, R; Younkin, S; Zhou, P, 2005
)
0.33
" The effects of nebivolol on the bioavailability of NO and ONOO, indicators of endothelial function and dysfunction, respectively, were measured in vitro using nanosensors placed in mesenteric arteries."( Effect of nebivolol on endothelial nitric oxide and peroxynitrite release in hypertensive animals: Role of antioxidant activity.
Boychuk, B; Jacob, RF; Kubant, R; Malinski, T; Mason, RP; Walter, MF, 2006
)
0.33
" It is hypothesized that altered NO bioavailability may result from an increase in endogenous NO synthase (NOS) inhibitors, asymmetric dimethly araginine (ADMA), and N(G)-monomethyl arginine, which are normally metabolized by dimethyarginine dimethylamine hydrolase (DDAH)."( Role of DDAH-1 in lipid peroxidation product-mediated inhibition of endothelial NO generation.
Cardounel, AJ; Chicoine, LG; Druhan, L; Forbes, SP; Guzman, JE; Lu, D; Murugesan, V; Parinandi, NL; Pope, AJ; Xia, Y, 2007
)
0.34
" The oral bioavailability of RBx 7796 in rat and dog was 83 % and 47 %, respectively."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" These results indicate that in conjunction with microvascular dysfunction, nanoparticle exposure also decreases NO bioavailability through at least two functionally distinct mechanisms that may mutually increase local reactive species."( Pulmonary nanoparticle exposure disrupts systemic microvascular nitric oxide signaling.
Boegehold, MA; Castranova, V; Chen, BT; Frazer, DG; Hubbs, AF; Nurkiewicz, TR; Porter, DW; Stone, S, 2009
)
0.35
"In conclusion, uric acid decreased NO bioavailability and enhanced superoxide generation in A23187-stimulated bovine aortic endothelial cells."( The effect of uric acid on homocysteine-induced endothelial dysfunction in bovine aortic endothelial cells.
Kubala, L; Lojek, A; Papezikova, I; Pekarova, M, 2009
)
0.35
" These findings suggest that growth-related increases in arteriolar NO bioavailability may be due at least partially to changes in the regulation of eNOS phosphorylation and increased signaling activity, with no change in the abundance of eNOS signaling proteins."( Changes in eNOS phosphorylation contribute to increased arteriolar NO release during juvenile growth.
Boegehold, MA; Kang, LS; Nurkiewicz, TR; Wu, G, 2012
)
0.38
" We hypothesized that in addition to its MMP inhibitory effect, doxycycline attenuates oxidative stress and improves nitric oxide (NO) bioavailability in 2K-1C hypertension, thus improving hypertension-induced arterial endothelial dysfunction."( Doxycycline ameliorates 2K-1C hypertension-induced vascular dysfunction in rats by attenuating oxidative stress and improving nitric oxide bioavailability.
Bendhack, LM; Castro, MM; Ceron, CS; Gerlach, RF; Guimaraes, DA; Rizzi, E; Rodrigues, GJ; Tanus-Santos, JE, 2012
)
0.38
" We examined both in vivo and in vitro whether the compound might induce vasorelaxation in human blood vessels through the improvement of nitric oxide (NO) bioavailability and a reduction of oxidative stress mediated by endothelial NO synthase (eNOS) function."( Nitric oxide production and endothelium-dependent vasorelaxation ameliorated by N1-methylnicotinamide in human blood vessels.
Dobrucki, LW; Domagala, TB; Dropinski, J; Kalinowski, L; Kotula-Horowitz, K; Leszczynska-Wiloch, M; Polanski, S; Szczeklik, A; Szeffler, A; Wojciechowski, J; Wojnowski, L, 2012
)
0.38
"Endothelial dysfunction is associated with a reduced bioavailability of nitric oxide (NO)."( Long-term nitric oxide synthase inhibition prevents 17β-estradiol-induced suppression of cyclooxygenase-dependent contractions and enhancement of endothelium-dependent hyperpolarization-like relaxation in mesenteric arteries of ovariectomized rats.
Leung, SWS; Shi, Y, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" These results explain several previous, discordant reports on the presence or absence of an effect of A23187 on cellular secretory events, on differing dose-response relationships, and on cytotoxic versus noncytotoxic mechanisms of action."( Effect of solvent on the histamine-releasing, enzyme-releasing, and mitogenic properties of the calcium ionophore A23187.
Dorsey, NK; Findlay, SR; Lichtenstein, LM; Plaut, M; Thomas, LL, 1979
)
0.26
" For both CCK-OP and carbamylcholine there was close agreement between the dose-response curve for stimulation of calcium outflux and that for increase of cellular cyclic GMP."( Action of cholecystokinin, cholinergic agents, and A-23187 on accumulation of guanosine 3':5'-monophosphate in dispersed guinea pig pancreatic acinar cells.
Christophe, JP; Conlon, TP; Frandsen, EK; Gardner, JD; Krishna, G, 1976
)
0.26
" Stimulation of fluid secretion by 5-HT follows a definite dose-response curve, but there is no consistent relationship between the rate of enzyme secretion and the stimulating concentration of 5-HT."( The control of enzyme secretion from fly salivary glands.
Bay, CM, 1978
)
0.26
" The dose-response relationships and kinetics of histamine and BK-A release from antigen-challenged peripheral leukocytes are similar."( Anaphylactic relase of a basophil kallikrein-like activity. II. A mediator of immediate hypersensitivity reactions.
Lichtenstein, LM; Newball, HH; Talamo, RC, 1979
)
0.26
" The cell damaging and amylase releasing properties of A23187 were distinguished by their time course and dose-response relationship."( Intracellular uptake and alpha-amylase and lactate dehydrogenase releasing actions of the divalent cation ionophore A23187 in dissociated pancreatic acinar cells.
Chandler, DE; Williams, JA, 1977
)
0.26
" In the rat 4f inhibited LTB4 synthesis in blood ex vivo and in zymosan-inflamed air pouch exudate with an ED50 3 h after oral dosing of 10 mg/kg in each system."( Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.
Bird, TG; Bruneau, P; Crawley, GC; Dowell, RI; Edwards, PN; Foster, SJ; Giroaeau, JM; McMillan, RM; Walker, ER; Waterson, D, 1992
)
0.28
" Dose-response relationships to the EDRF dependent vasodilators thrombin, acetylcholine, and calcimycin, and to the EDRF independent vasodilator isoprenaline, were then established."( Effects of regional ischaemia, with or without reperfusion, on endothelium dependent coronary relaxation in the dog.
Ku, DD; Winn, MJ, 1992
)
0.28
" Dose-response experiments indicated that interleukin-4 is more potent than interleukin-1 alpha and interleukin-2 in inhibiting dexamethasone-induced apoptosis."( Interleukins modulate glucocorticoid-induced thymocyte apoptosis.
Crocicchio, F; Migliorati, G; Moraca, R; Nicoletti, I; Pagliacci, C; Riccardi, C, 1992
)
0.28
" Cumulative dose-response curves were obtained to methacholine, a receptor-mediated endothelium-dependent dilator; to A23187, a nonreceptor-mediated endothelium-dependent dilator; and to sodium nitroprusside, a direct-acting endothelium-independent dilator before, during, and after inhalational anesthetic exposure."( Halothane, enflurane, and isoflurane attenuate both receptor- and non-receptor-mediated EDRF production in rat thoracic aorta.
Johns, RA; Proctor, GJ; Uggeri, MJ, 1992
)
0.28
" Addition of the muscarinic antagonists atropine or pirenzepine shifted the carbachol dose-response curves to the right, without decreasing the carbachol maximal stimulatory effects."( Effects of muscarinic agonists and depolarizing agents on inositol monophosphate accumulation in the rabbit vagus nerve.
Dunant, Y; Sierro, CD; Vitus, J, 1992
)
0.28
" Oral dosing of nilvadipine suppressed carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen."( Inhibition by nilvadipine of ischemic and carrageenan paw edema as well as of superoxide radical production from neutrophils and xanthine oxidase.
Oyanagui, Y; Sato, S, 1991
)
0.28
" Time-course kinetics and dose-response curves of RNA and DNA synthesis induced by bryostatin 1 or PMA were comparable, albeit the phorbol ester was significantly more potent."( Synergistic action of calcium ionophore A23187 and protein kinase C activator bryostatin 1 on human B cell activation and proliferation.
Drexler, HG; Gignac, SM; Hoffbrand, AV; Pettit, GR, 1990
)
0.28
" Dose-response curve for DAG accumulation induced by A23187 was similar to that for amylase secretion."( Diacylglycerol accumulation is involved in the potentiating effect of A23187 on carbachol-stimulated amylase secretion from parotid gland.
Izawa, T; Komabayashi, T; Suda, K; Tsuboi, M; Yakata, A, 1990
)
0.28
"; n = 4) in antagonizing cumulative dose-response curve for Ca2+ in the depolarized aorta strips."( Ca2+ channel blocking effects of hirsutine, an indole alkaloid from Uncaria genus, in the isolated rat aorta.
Aimi, N; Horie, S; Horiuchi, H; Sakai, S; Watanabe, K; Yano, S, 1991
)
0.28
" Dose-response curves were also obtained to the direct smooth muscle dilator nitroprusside during normoxia and hypoxia."( Effects of oxygen tension on endothelium dependent responses in canine coronary microvessels.
Muller, JM; Myers, PR; Tanner, MA, 1991
)
0.28
" The dose-response curve for MLC phosphorylation by VP is similar to that for tight junctional permeabilization in perfused liver with maximal effect at about 10(-8) M VP."( Vasopressin and A23187 stimulate phosphorylation of myosin light chain-1 in isolated rat hepatocytes.
Dalle-Molle, E; Hardison, WG; Yamaguchi, Y, 1991
)
0.28
" The dose-response curve for EDRF-mediated relaxation to acetylcholine was shifted rightward in rats with heart failure, and the concentrations of acetylcholine required to achieve 50% maximal relaxation (EC50) were increased compared with those of control rats in both TA and PA segments."( Diminished endothelium-derived relaxing factor activity in an experimental model of chronic heart failure.
Gay, R; Greenberg, B; Ontkean, M, 1991
)
0.28
" The time course and dose-response curves for the effects of phorbol 12-myristate 13-acetate (PMA) on S6 kinase activity were similar to those for its effects on protein kinase C binding to the membrane fraction, indicating that S6 kinase activation was correlated with protein kinase C activation."( Regulation of S6 kinase activity in Madin-Darby canine kidney renal epithelial cells.
Bloom, TJ; Krebs, EG; Meier, KE; Weiel, JE, 1990
)
0.28
" H-7 produced a shift to the right of the dose-response curve for the PKC activator, 12-o-tetradecanoylphorbol-13-acetate (TPA) in the case of SHR aortas, while no such shift was noted in tissues from WKY."( Effects of H-7 (protein kinase inhibitor) and phorbol ester on aortic strips from spontaneously hypertensive rats.
Iwasaki, T; Miyata, S; Morita, S; Nagai, K; Shibata, R, 1990
)
0.28
" A23187 caused release of vasoactive intestinal polypeptide dose dependently and phorbol 12,13-dibutyrate (100 nM) markedly shifted the dose-response curve of A23187 to the left."( Enhancement of A23187-induced release of enteric vasoactive intestinal polypeptide by phorbol 12,13-dibutyrate.
Belai, A; Burnstock, G; Dale, MM, 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
"To evaluate the distribution of an amphiphile or its binding to membranes whose properties are affected by such binding, it is only necessary to establish to what extent the dose-response to the amphiphile depends on the membrane concentration."( How to evaluate the distribution of an "invisible" amphiphile between biological membranes and water.
Champeil, P; de Foresta, B; le Maire, M; Merah, Z, 1990
)
0.28
" The dose-response curves to Ca2+ ionophore for amylase release were similarly shaped in both groups."( Effect of obstructive jaundice on amylase secretion in rat pancreatic acini.
Fukumoto, T; Iwamoto, Y; Kanazawa, K; Kasahara, K; Kashii, A; Miyata, M; Tenmoku, S, 1985
)
0.27
" In dose-response studies, PMA stimulated amylase release independently of db-cAMP, but potentiated the effect of carbachol."( Phorbol ester stimulates amylase secretion from rat parotid cells.
Ichida, T; Takuma, T, 1986
)
0.27
" At peptide concentrations of 1 microM clear-cut plateaus of the dose-response curves are not yet reached."( Atrial natriuretic hormones raise the level of cyclic GMP in neural cell lines.
Friedl, A; Hamprecht, B; Harmening, C, 1986
)
0.27
" In the presence of TMB-8 the dose-response curve for carbachol-induced amylase release shifts to the right, suggesting competitive antagonism at the muscarinic receptor."( Stimulatory and inhibitory effects of TMB-8 on pancreatic enzyme secretion.
De Pont, JJ; Van Nooij, IG; Willems, PH, 1986
)
0.27
" Neither xanthine shifted the calcium dose-response when PMNs were activated with calcium ionophore."( Therapeutic concentrations of theophylline and enprofylline potentiate catecholamine effects and inhibit leukocyte activation.
Crowley, JJ; Cusack, BJ; Nielson, CP; Vestal, RE, 1986
)
0.27
" In dose-response curves, the isoproterenol-sensitive K+ efflux was half-maximally inhibited (IC50) with 2-5 X 10(-10) M of isoproterenol concentration."( Stimulation of beta-adrenoceptors inhibits calcium-dependent potassium-channels in mouse macrophages.
Braquet, P; Dausse, JP; Garay, R; Hannaert, P; Rosati, C, 1986
)
0.27
" Acini preexposed to concentrations of carbamylcholine of 10(-6) M or greater showed shifts to the right in the subsequent carbamylcholine dose-response curves of amylase release."( Short-term cholinergic desensitization of rat pancreatic secretory response.
Asselin, J; Larose, L; Morisset, J, 1987
)
0.27
"0 microM f-Met peptide), although anti-IgE-induced release was unaffected over a dose-response curve."( The effect of pertussis toxin on mediator release from human basophils.
MacGlashan, DW; Warner, JA; Yancey, KB, 1987
)
0.27
" Addition of 10(-8) M SP caused a shift to the left in the secretion dose-response curve caused by ISO, but did not enhance ISO-induced maximal response."( [3H]protein secretion in rat parotid gland: substance P-beta-adrenergic synergism.
Dreux, C; Imhoff, V; Rossignol, B, 1987
)
0.27
" With immunological activation of passively sensitized cells, histamine and PGD2 release had similar dose-response characteristics, but TXB2, LTC4, LTD4, and LTE4 release differed in reaching maximum at 50 micrograms/ml and declining at 125 micrograms/ml anti-human IgE."( The immunoglobulin E- and calcium-dependent release of histamine and eicosanoids from human dispersed mastocytosis spleen cells.
Agius, RM; Benyon, RC; Holgate, ST; Jones, DB; Robinson, C; Wright, DH, 1988
)
0.27
" Dose-response curves for CCK-8- or CCh-stimulated amylase release in TPA-pretreated acini revealed attenuation of both maximal efficacy and sensitivity."( Downregulation of protein kinase C in guinea pig pancreatic acini: effects on secretion.
Hootman, SR; Kuroiwa, C; Stuenkel, EL; Sung, CK; Williams, JA, 1988
)
0.27
" Evaluation of time courses and dose-response curves indicated that carbachol, CCK-OP, bombesin, and substance P cause extracellular Ca2+-independent transient increases in [Ca2+]i and transient bursts in amylase release (initial secretion)."( Free cytosolic calcium and secretagogue-stimulated initial pancreatic exocrine secretion.
Krims, PE; Pandol, SJ, 1988
)
0.27
" First, when the dose-response curve of PTH-induced ODC activity is compared with that of PTH-stimulated cAMP production, the ED50 for cAMP production is about five times as high as that for the induction of ODC activity."( Induction of ornithine decarboxylase activity in isolated chicken osteoblasts by parathyroid hormone: the role of cAMP and calcium.
Herrmann-Erlee, MP; Löwik, CW; Olthof, AA; van Leeuwen, JP; van Zeeland, JK, 1988
)
0.27
" The most effective inhibitory dosage with maximal carbachol (10(-5) M; 30."( Prostaglandin E analogue inhibition of pancreatic enzyme secretion.
Adrian, TE; Bilchik, AJ; Modlin, IM; Zucker, KA, 1989
)
0.28
" Chlordiazepoxide shifted the dose-response curves for TRH stimulation of PRL release and synthesis to the right, and did not change PRL release alone."( Pituitary thyrotropin-releasing hormone (TRH) receptors: effects of TRH, drugs mimicking TRH action, and chlordiazepoxide.
Hinkle, PM; Shanshala, ED, 1989
)
0.28
"8 mM Ca2+, the rate of glycogen breakdown was increased by theophylline in a dose-dependent manner and the dose-response curve was somewhat similar to that obtained with oxygen uptake."( Ca2+ requirement for metabolic effects of secretagogues in the amphibian gastric mucosa.
Chacín, J; Lobo, P; Subero, O, 1989
)
0.28
" In the same system, dose-response studies demonstrated that 4-O-methyl-phorbol myristate acetate (4-O-Me-PMA) and mezerein were approximately 50 times less active than PMA, while phorbol dibutyrate (PDB), phorbol diacetate (PDA), phorbol and the calcium ionophore A23187 did not cause an increase in the number of formazan-positive PECs at the doses used."( Tumor promoters differ in their ability to stimulate superoxide anion radical production by murine peritoneal exudate cells following in vivo administration.
Czerniecki, BJ; Witz, G, 1989
)
0.28
" We report that the GRP78 enhancer (i) exhibits strong cooperative interactions with its homologous promoter; (ii) can activate and confer a calcium ionophore (A23187) inducibility to heterologous promoters in an orientation-independent manner; (iii) prefers the 5' over the 3' location and; (iv) is dosage dependent in that two copies are twice as active as a single unit."( Cooperative interactions between the GRP78 enhancer and promoter elements in hamster fibroblasts.
Kim, YK; Lee, AS, 1989
)
0.28
" The time course and dose-response for the effect of PMA at 23 degrees C closely correlate with the phosphorylation of a set of relatively "slowly" phosphorylated proteins (P20, P35, P41, P60), but not the rapidly phosphorylated P47 protein."( Synergistic release of arachidonic acid from platelets by activators of protein kinase C and Ca2+ ionophores. Evidence for the role of protein phosphorylation in the activation of phospholipase A2 and independence from the Na+/H+ exchanger.
Banga, HS; Feinstein, MB; Halenda, SP; Lau, LF; Zavoico, GB, 1989
)
0.28
" At concentrations lacking agonist activity U-75302 was an effective antagonist, displacing the LTB4 dose-response curve."( Receptor antagonism of leukotriene B4 myotropic activity by the 2,6 disubstituted pyridine analog U-75302: characterization on lung parenchyma strips.
Fitzpatrick, FA; Lawson, CF; Morris, J; Wishka, DG,
)
0.13
" The slopes of the dose-response regression lines were similar for the three drugs."( Mechanism of action of colchicine. VI: Effect of colchicine on generation of leukotriene B4 by human polymorphonuclear leukocytes.
Bhuta, S; Chang, YH; Ouyang, Y; Wang, W,
)
0.13
" Dose-response curves for inositol phospholipid synthesis stimulated by carbachol and CCK-8 in mouse acini were biphasic and superimposable with those of amylase secretion."( The effects of gamma-hexachlorocyclohexane on amylase secretion and inositol phospholipid metabolism in mouse pancreatic acini.
Crouch, MF; Roberts, ML, 1985
)
0.27
"When the dose-response curve of adrenocorticotropin (ACTH)-induced aldosterone secretion is compared to that of ACTH-induced intracellular cAMP, the ED50 for intracellular cAMP is more than 10 times as high as that for aldosterone production."( Role of calcium and cAMP in the action of adrenocorticotropin on aldosterone secretion.
Kojima, I; Kojima, K; Rasmussen, H, 1985
)
0.27
" In addition, the Ca2+ dose-response curves of both activities in intact platelets, obtained by stimulation with A23187 in the presence of Ca2+/HEDTA-buffers, were compared."( Correlation between calpain-mediated cytoskeletal degradation and expression of platelet procoagulant activity. A role for the platelet membrane-skeleton in the regulation of membrane lipid asymmetry?
Bevers, EM; Comfurius, P; Verhallen, PF; Zwaal, RF, 1987
)
0.27
" Denervation caused a shift to the left of the 86Rb efflux dose-response curve to carbachol and phenylephrine (3."( Effect of parasympathetic denervation on K+ release by rat parotid slices.
Adham, N; Templeton, D, 1987
)
0.27
" Co-incubation of cells with 1 microM A23187 caused parallel upward shift of the TPA dose-response curve, and the further addition of 10 microM forskolin led to further upward shift."( Mechanisms of TSH release: studies with forskolin, phorbol ester and A23187.
Davis, JR; Sheppard, MC, 1987
)
0.27
" This decrease paralleled the time course and dose-response of the inhibition of cytocidal activity."( Tumor necrosis factor receptors and cytocidal activity are down-regulated by activators of protein kinase C.
Baglioni, C; Johnson, SE, 1988
)
0.27
" ANP stimulated production of cyclic GMP (cGMP), and inhibited aldosterone secretion with a similar dose-response relationship."( Regulation of aldosterone secretion by avian adrenocortical cells.
Hurwitz, S; Pines, M; Rosenberg, J, 1988
)
0.27
" In human red cells and mouse macrophages, the dose-response curves of K+ efflux as a function of Ca2+ ionophore, A23187, concentration were not modified by addition of ANF."( Atrial natriuretic factor inhibits Ca(2+)-dependent K+ fluxes in cultured vascular smooth muscle cells.
Bianchi, C; Braquet, P; Cantin, M; Dunham, B; Garay, R; Genest, J; Hannaert, P; Marche, P; Meyer, P; Rodrigue, F, 1985
)
0.27
" A dose-response relationship between inhibition of alpha-MSH secretion and the concentration of Leu-enkephalin, with ED50 approximately 10(-9) M, was observed."( Modulation by Leu-enkephalin of peptide release from perifused neurointermediate pituitary. II. Inhibition of calcium-mediated secretion of alpha-MSH and beta-endorphin.
Al Zein, M; Koch, B; Lutz-Bucher, B, 1986
)
0.27
" Incubation of the neutrophils with cholera toxin, unlike pertussis toxin, did not inhibit the fMet-Leu-Phe induced rise in the intracellular concentration of free calcium, and caused only a shift to the right of the dose-response curve of N-acetyl-beta-glucosaminidase release."( Pertussis but not cholera toxin inhibits the stimulated increase in actin association with the cytoskeleton in rabbit neutrophils: role of the "G proteins" in stimulus-response coupling.
Becker, EL; Feinstein, MB; Molski, TF; Munoz, JJ; Naccache, PH; Sha'afi, RI; Shefcyk, J; Volpi, M; Yassin, R, 1985
)
0.27
" Subsequent LH responses to GnRH in those cells pretreated with GnRH and KCl were markedly reduced and the dose-response characteristics altered such that the curves were non-sigmoidal."( Increased gonadotrophin releasing hormone receptors on pituitary gonadotrophs: effect on subsequent LH secretion.
Clayton, RN; Naik, SI; Young, LS, 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
" HA-1004 shifted the dose-response curve for CaCl2 to the right in a competitive manner in depolarized rabbit renal arterial strips."( Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase.
Hidaka, H; Inagaki, M; Ishikawa, T; Watanabe, M, 1985
)
0.27
" The leukotriene-generating response of monolayers of human monocytes pretreated with cytochalasin B to FMLP is receptor-mediated, as indicated by the inactivity of the structural analog N-acetyl-methionyl-leucyl-phenylalanine and by the capacity of the FMLP receptor antagonist carbobenzoxyphenylalanyl-methionine to inhibit the agonist action of FMLP in a dose-response fashion."( Generation of leukotrienes by human monocytes pretreated with cytochalasin B and stimulated with formyl-methionyl-leucyl-phenylalanine.
Austen, KF; Lee, TH; Lewis, RA; Robin, JL; Williams, JD, 1986
)
0.27
"12 to 80 microM) for 1 to 60 min at 37 degrees C to construct dose-response and time-dependence curves of lipoxygenase product generation."( Enhanced 5-lipoxygenase activity in lung macrophages compared to monocytes from normal subjects.
Bigby, TD; Holtzman, MJ, 1987
)
0.27
" A dose-response curve was achieved for all three cyclooxygenase products with the calcium ionophore A23187."( Human peritoneal eosinophils and formation of arachidonate cyclooxygenase products.
Foegh, ML; Maddox, YT; Ramwell, PW, 1986
)
0.27
" The dose-response and kinetics of inhibition by calmodulin antagonists of acidic phospholipid-activated phospholipase A2 activity in purified preparations were similar to those of Ca2+-induced arachidonic acid release from membrane fractions."( Calmodulin-independent inhibition of platelet phospholipase A2 by calmodulin antagonists.
Hashimoto, Y; Kume, S; Naito, C; Oka, H; Teramoto, T; Watanabe, T, 1986
)
0.27
" At all extracellular calcium concentrations Ca2+i reached significantly higher values in the presence of the ionophore and the dose-response relationship was shifted to the left."( Normalizing effect of Ca2+ ionophore on cytoplasmic Ca2+ and parathyroid hormone release of dispersed parathyroid cells from patients with hyperparathyroidism.
Akerström, G; Gylfe, E; Larsson, R; Ljunghall, S; Rastad, J; Wallfelt, C, 1986
)
0.27
" The C6 dose-response curve for release of C20:4 plus its metabolites was monotonic, which indicates dependence on channel formation, whereas the dose-response curve for lysis displayed multi-hit behavior."( Release of arachidonic acid and formation of oxygenated derivatives after complement attack on macrophages: role of channel formation.
Hammer, CH; Imagawa, DK; Koga, PG; Mayer, MM; Osifchin, NE; Ramm, LE; Shin, HS, 1986
)
0.27
"OH) radical was observed to affect cyclooxygenase metabolism in a dose-response manner."( Gender-related variations and interaction of human neutrophil cyclooxygenase and oxidative burst metabolites.
Bellanti, JA; Mallery, SR; Ramwell, PW; Zeligs, BJ, 1986
)
0.27
" Phorbol ester dose-response curves for growth arrest and enzymatic markers of differentiation were shifted to lower concentrations when the ionophore was present."( Ca2+ and phorbol ester synergistically induce HL-60 differentiation.
Harley, CB; Tyers, M, 1986
)
0.27
" Dose-response curves of thrombin stimulation and carbacyclin inhibition of apoB and beta-thromboglobulin (beta-TG) release were very similar."( Apolipoprotein B release from activated human platelets.
Fuki, IV; Mazurov, AV; Podrez, EA; Preobrazhensky, SN; Repin, VS; Smirnov, VN; Tsibulsky, VP, 1986
)
0.27
" Augmentation of each eosinophil function by GM-CSF was time- and dose-dependent, with a dose-response relationship at concentrations between 1 and 20 pM."( Enhancement of human eosinophil cytotoxicity and leukotriene synthesis by biosynthetic (recombinant) granulocyte-macrophage colony-stimulating factor.
Austen, KF; Bina, JC; David, JR; DiPersio, JF; Gasson, JC; Golde, DW; Owen, WF; Silberstein, DS; Soberman, R, 1986
)
0.27
" Furthermore, the magnitude of the translocation of protein kinase C from cytosol to plasma membrane corresponded to the physiologic IL 2 dose-response for IFN-gamma secretion."( Interleukin 2 induction of interferon-gamma mRNA synthesis.
Birchenall-Sparks, MC; Farrar, WL; Young, HB, 1986
)
0.27
" Furthermore, differing quin-2 AM dose-response profiles suggest the presence of dual Ca2+-dependent pathways in the adipocyte."( Chelation of intracellular calcium blocks insulin action in the adipocyte.
Delfert, DM; McDonald, JM; Pershadsingh, HA; Shade, DL, 1987
)
0.27
" The dose-response curve for nicotine was bell shaped, with a threshold at 10(-7) M, a maximum at 10(-5) M, and diminished release at higher concentrations, an observation indicative of desensitization."( Direct and continuous detection of ATP secretion from primary monolayer cultures of bovine adrenal chromaffin cells.
Bourke, JE; Livett, BG; White, TD, 1987
)
0.27
" Increasing Mg2+ concentrations only shifted the dose-response curve parallel to the right side."( Decreased magnesium effects of echinocytes formed by calcium plus A23187 in cryopreservation.
Shimizu, T, 1988
)
0.27
" The dose-response characteristics of zymosan-induced LTC4 generation were different from those of phagocytosis, suggesting that the two events were independent."( The generation and cellular distribution of leukotriene C4 in human eosinophils stimulated by unopsonized zymosan and glucan particles.
Clark, TJ; Howell, CJ; Lee, TH; Lessof, MH; Mahauthaman, R; Spur, BW; Youlten, LJ, 1988
)
0.27
" The NaF-PGI2 dose-response curve was moved to the left by the presence of adrenaline, phorbol 12,13-dibutyrate (PDBU) and the Ca2+ ionophore A23187 in the incubation media."( Fluoride stimulates in vitro vascular prostacyclin synthesis: interrelationship of G proteins and protein kinase C.
Dandona, P; Jeremy, JY, 1988
)
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
" Pretreatment of aortic rings with high concentrations of nifedipine (5 X 10(-7) M) or verapamil (10(-5) M) caused a comparable displacement to the right (2-3 times) in the relaxant dose-response curve for acetylcholine, A23187 and sodium nitroprusside with little or no changes in the maximal relaxation obtained with these vasodilators."( Blockade of endothelium-dependent relaxation by the amiloride analog dichlorobenzamil: possible role of Na+/Ca++ exchange in the release of endothelium-derived relaxant factor.
Bunting, PB; Schofield, TL; Winquist, RJ, 1985
)
0.27
" Dose-response studies revealed that 5 microM-carbachol significantly increased (16%) the accumulation of InsP3 whereas a significant increase in accumulation of InsP2 and InsP was observed only at agonist concentrations greater than 10 microM."( Carbachol causes rapid phosphodiesteratic cleavage of phosphatidylinositol 4,5-bisphosphate and accumulation of inositol phosphates in rabbit iris smooth muscle; prazosin inhibits noradrenaline- and ionophore A23187-stimulated accumulation of inositol pho
Abdel-Latif, AA; Akhtar, RA, 1984
)
0.27
" Analysis of the amiloride dose-response relations revealed a complex "non Michaelis-Menten" behavior."( Amiloride blockable sodium fluxes in toad bladder membrane vesicles.
Garty, H, 1984
)
0.27
" Inhibition of aggregation by the beta-adrenoceptor antagonists was manifested as a parallel shift to the right in the dose-response curve."( Beta-adrenoceptor antagonists and human platelets: relationship of effects to lipid solubility.
Kerry, R; Scrutton, MC; Wallis, RB, 1984
)
0.27
" Use of this technique enabled us to define the dose-response relationship of the aggregation produced by the cationophore A23187 and the inhibitory effect of tetracaine on divalent cation-dependent aggregation responses."( Digital integration of granulocyte aggregation responses. A simple and reproducible method for the quantitation of granulocyte adhesiveness.
Craddock, PR; Hammerschmidt, DE; Weisdorf, DJ; White, JG, 1980
)
0.26
" The anti-IgE dose-response pattern of this activation event further suggests that it is an integral part of the anti-IgE-induced release process itself."( Release of histamine from human leukocytes stimulated with the tumor-promoting phorbol diesters. II. Interaction with other stimuli.
Daiuta, R; Gillespie, E; Lichtenstein, LM; Schleimer, RP, 1982
)
0.26
" The S-shaped dose-response relationship with D2O was shifted to the left in the patients with BR to exercise compared to patients without (P less than 0 X 025)."( Release of histamine from leucocytes and its determinants in vitro in relation to bronchial responsiveness to inhaled histamine and exercise in vivo.
Degenhart, HJ; Kerrebijn, KF; Neijens, HJ; Raatgeep, HC, 1982
)
0.26
" The dose-response curves for CCK8 were similarly shaped in both CCK8-treated and control rats, but they were shifted 3- to 10-fold toward higher concentrations of CCK8 after 7 and 14 days of CCK8 treatment."( Amylase secretion by isolated pancreatic acini after chronic cholecystokinin treatment in vivo.
Otsuki, M; Williams, JA, 1983
)
0.27
" The dose-response curve for histamine release was similar to that obtained by specific antigen in type I allergy."( Basophil histamine release induced by leukocyte nuclei in patients with rheumatoid arthritis.
Norn, S; Permin, H; Stahl Skov, P, 1983
)
0.27
" The increase in the hydrolysis of PtdIns(4,5)P2 and the increase in [32P]Pi incorporation into PtdA commenced at the same concentration of carbachol in dose-response studies."( Effects of carbachol and pancreozymin (cholecystokinin-octapeptide) on polyphosphoinositide metabolism in the rat pancreas in vitro.
Davis, JS; Farese, RV; Larson, RE; Orchard, JL, 1984
)
0.27
" The dose-response inhibition curve is paralleled by a fenoterol-induced increase in the cAMP levels of human leukocyte preparations."( Inhibition of IgE-mediated histamine release from human basophils and mast cells by fenoterol.
Ambrosio, G; Bonaduce, D; Condorelli, M; Genovese, A; Marone, G; Triggiani, M, 1984
)
0.27
" Kinetic and dose-response studies showed that PGBX mimicked te action of ionophore A23187 in PMN."( PGBX, a prostagandin derivative, mimics the action of the calcium ionophore A23187 on human neutrophils.
Korchak, HM; Serhan, CN; Weissmann, G, 1980
)
0.26
" The dose-response to ionophore A23187 (1."( Role of calcium in antral gastrin release.
Harty, RF; Maico, DG; McGuigan, JE, 1981
)
0.26
" There was a dose-response relationship between both moieties of PTH and the rise in heart beats, but the effect of 1-84 PTH was significantly greater than that of 1-34 moiety."( Effect of parathyroid hormone on rat heart cells.
Bogin, E; Harary, I; Massry, SG, 1981
)
0.26
" The relevance of this reaction to secretory phenomena is indicated by its requirement for Ca, its rapid onset, and dose-response curves that paralleled those of the secretory response."( Calcium-phospholipid interactions in secretory cells: a new perspective on stimulus-secretion coupling.
Rubin, RP, 1982
)
0.26
" The dose-response curve of the fluorescence change and that of the superoxide release of th cells were very similar."( Release of the membrane-calcium and its relation to the superoxide formation by polymorphonuclear leukocytes.
Matsumoto, T; Minakami, S; Nabi, ZF; Takeshige, K, 1982
)
0.26
" These changes in phospholipid metabolism and Ca2+ flux were parallel to changes seen in K+ efflux as judged by dose-response studies."( Modulation of rat parotid cell alpha-adrenergic responsiveness at a step subsequent to receptor activation.
Baum, BJ; Bodner, L; Hoopes, MT; Ito, H; Roth, GS; Uchida, T, 1982
)
0.26
" Inhibition by proglumide was competitive and resulted in a parallel rightward shift of the cholecystokinin dose-response curve."( Cholecystokinin-induced contraction of dispersed smooth muscle cells.
Collins, SM; Gardner, JD, 1982
)
0.26
" The parallel dose-response relationship for the antigen-induced release of the performed mediator and the generation of both leukotrienes along with the superimposable time courses of their extracellular appearance indicate the origin of these mediators from a common cell type with IgE receptors."( Immunologic and ionophore-induced generation of leukotriene B4 from mouse bone marrow-derived mast cells.
Austen, KF; Corey, EJ; Hoover, D; Lewis, RA; Mencia-Huerta, JM; Razin, E; Ringel, EW, 1983
)
0.27
" Treatment of 20:4 with soybean lipoxygenase did not abolish its capacity to induce O2- production; native and lipoxygenase-treated 20:4 exhibited similar dose-response ratios."( Unsaturated fatty acids as second messengers of superoxide generation by macrophages.
Bromberg, Y; Pick, E, 1983
)
0.27
" But the dose-response curve for Ca2+ in the presence of A23187 (3 X 10(-5) M), a Ca ionophore, was not affected at all by verapamil (10(-6) M)."( Contractile response of the rabbit aorta to maitotoxin, the most potent marine toxin.
Ohizumi, Y; Yasumoto, T, 1983
)
0.27
" The parallel antigen-induced dose-response relationship, along with the superimposable time-course of the extracellular appearance, of beta-hexosaminidase, PAF-acether, and both leukotrienes indicated that the origin of these diverse mediators was from a common cell type with IgE-Fc receptors."( Antigen-initiated release of platelet-activating factor (PAF-acether) from mouse bone marrow-derived mast cells sensitized with monoclonal IgE.
Austen, KF; Lewis, RA; Mencia-Huerta, JM; Razin, E, 1983
)
0.27
" The dose-response curve for the initial rate of cytosolic free Ca2+ increase was very similar to those obtained for the initial rates of Ins-P3 production and PtdIns-4,5-P2 breakdown."( Relationship between inositol polyphosphate production and the increase of cytosolic free Ca2+ induced by vasopressin in isolated hepatocytes.
Alexander, J; Thomas, AP; Williamson, JR, 1984
)
0.27
" 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 dose-response curves for stimulation of 86Rb efflux and for endothelium-dependent relaxation were similar for each individual compound."( Endothelium-dependent relaxation of the pig aorta: relationship to stimulation of 86Rb efflux from isolated endothelial cells.
Gordon, JL; Martin, W, 1983
)
0.27
" The signal for priming could be clearly distinguished from the signal causing oxidase activation by the dose-response curves for each, as well as by the use of several pharmacologic agents."( The NADPH oxidase of human polymorphonuclear leukocytes. Evidence for regulation by multiple signals.
Clayton, CC; McPhail, LC; Snyderman, R, 1984
)
0.27
" A dose-response relationship resulted when explants were challenged with methacholine in nutrient medium containing varied calcium concentrations (0."( The calcium dependency of mucus glycoconjugate secretion by canine tracheal explants.
Barbieri, EJ; Bobyock, E; Chernick, WS; McMichael, RF, 1984
)
0.27
" In light of the relative ineffectiveness of the above calcium antagonists on the LTD4 dose-response curves, it is suggested that airways contraction is dependent on mobilization of intracellular calcium and that the action of nitrendipine and verapamil as inhibitors of antigen- and A23187-induced contractions is at the point of blocking mediator (i."( Effects of calcium channel blockers and a calmodulin antagonist on contractions of guinea pig airways.
Burka, JF, 1984
)
0.27
" On the basis of kinetic data, dose-response data, and failure of elevated cytosolic calcium levels to inhibit lipid secretion, it was concluded that disturbed intracellular calcium homeostasis probably is not important in CCl4-dependent inhibition of secretion of very low density lipoproteins."( Evidence against a role for disturbed hepatocellular calcium homeostasis in the fatty liver of carbon tetrachloride hepatotoxicity.
Brattin, WJ; Glende, EA; Pencil, SD; Recknagel, RO, 1984
)
0.27
" When verapamil was administered to the healthy volunteers at the dosage commonly used, inhibition of platelet aggregation was observed 2 hrs after the drug ingestion."( Inhibition of human platelet functions by verapamil.
Ando, Y; Ikeda, Y; Kikuchi, M; Toyama, K; Watanabe, K, 1981
)
0.26
"5mM-Ca2+ (food-deprived) for rats dosed with 1,25-dihydroxycholecalciferol."( Oxygen-dependent 1,25-dihydroxycholecalciferol-induced calcium ion transport in rat intestine.
DeLuca, HF; Kabakoff, B; Kendrick, NC, 1981
)
0.26
" Almost identical dose-response curves to OpZ were obtained with peritoneal and alveolar macrophages, while the dose-response curve of peritoneal macrophages to A23187 was much shallower."( Macrophages from different sources, their production of chemiluminescence under various stimuli and the effects of PGE2 and drugs.
Bittner, C; Parnham, MJ; Winkelmann, J, 1981
)
0.26
" This difference in Ca2+/Mg2+ affinities was exploited in dose-response studies designed to determine which cation exerts primary control over K+/H+ exchange activity."( On the relative roles of Ca2+ and Mg2+ in regulating the endogenous K+/H+ exchanger of rat liver mitochondria.
Dordick, RS; Garlid, KD; Nakashima, RA, 1982
)
0.26
" Guinea pigs, dosed orally once a day for 4 days with dexamethasone (3."( Effect of dexamethasone on A23187-induced airway responses in the guinea pig.
Bendele, AM; Cockerham, SL; Silbaugh, SA; Stengel, PW, 1994
)
0.29
" cAMP shifted the dose-response curve for calcium-induced secretion leftwards and elevated the peak value of secretion."( Inhibition by somatostatin of amylase secretion induced by calcium and cyclic AMP in rat pancreatic acini.
Kojima, I; Mine, T; Ohnishi, H, 1994
)
0.29
" The muscarinic antagonists, pirenzepine and AF-DX 116, shifted the dose-response curve for the muscarine INs to the right in a parallel manner."( Mechanism of activation of nonselective cation channels by putative M4 muscarinic receptor in guinea-pig chromaffin cells.
Imanaga, I; Inoue, M, 1995
)
0.29
" In contrast, the dose-response curve for amylase secretion induced by the phorbol ester phorbolmyristate-13-acetate was shifted to the right without a reduction of the maximal secretory response."( Cyclosporine A inhibits protein-kinase-C-mediated amylase release from isolated rat pancreatic acini.
Domagk, KA; Fölsch, UR; Höcker, M; Kern, HF; Schmidt, WE; Schwarzhoff, R; Waschulewski, IH, 1994
)
0.29
" In extracts from cells pretreated with glutamate, the activity-Ca2+ concentration dose-response relationship of the 13."( Glutamate stably enhances the activity of two cytosolic forms of phospholipase A2 in brain cortical cultures.
Bonventre, JV; Kim, DK; Koroshetz, WJ; Nemenoff, RA; Rordorf, G, 1995
)
0.29
" No differences in ELGV dose-response curves to LTD4 were seen in A23187- and vehicle-exposed animals."( Inhaled A23187 produces a preferential sensitization to substance P.
Bendele, AM; Cockerham, SL; Silbaugh, SA; Stengel, PW, 1993
)
0.29
" This inhibition reflects the ability of GnRH to shift the CNP dose-response curve rightward (increasing the EC50 for CNP action approximately 10-fold both with and without 3-isobutyl-1-methylxanthine)."( Cyclic guanosine monophosphate production in the pituitary: stimulation by C-type natriuretic peptide and inhibition by gonadotropin-releasing hormone in alpha T3-1 cells.
Käppler, K; McArdle, CA; Poch, A, 1993
)
0.29
") were found to enhance nicotine-induced antinociception by shifting its dose-response curve to the left."( Involvement of calcium and L-type channels in nicotine-induced antinociception.
Damaj, MI; Martin, BR; Welch, SP, 1993
)
0.29
" Dose-response analysis revealed that maximal reduction of IL-1 binding was reached at FMLP concentrations that were also optimal for chemotaxis (50% effective dose = 5 x 10(-9) M)."( Chemoattractants induce rapid release of the interleukin 1 type II decoy receptor in human polymorphonuclear cells.
Colotta, F; Fadlon, EJ; Mantovani, A; Matteucci, C; Orlando, S; Sozzani, S, 1995
)
0.29
" Significant protection was observed with NT-4/5 concentrations from 100-1000 ng/ml, with a dose-response curve similar to that of BDNF."( Neurotrophin-4/5 protects hippocampal and cortical neurons against energy deprivation- and excitatory amino acid-induced injury.
Begley, JG; Cheng, B; Goodman, Y; Mattson, MP, 1994
)
0.29
" Terfenadine, at concentrations achievable at standard dosing regimens, has anti-inflammatory properties in vitro."( Effect of terfenadine on human eosinophil and neutrophil chemotactic response and generation of superoxide.
Eda, R; Hopp, RJ; Townley, RG, 1994
)
0.29
" A single dose of aspirin was administered four hours after dosing and FEV1 was measured for six hours."( Effect of the 5-lipoxygenase inhibitor ZD2138 on aspirin-induced asthma.
Arm, JP; Bell, GS; Foster, S; Lee, TH; MacMillan, R; Nasser, SM; Spruce, KE; Williams, AJ, 1994
)
0.29
"In vitro prospective, repeated-measures, dose-response study."( Effect of calcium to reverse the electrocardiographic effects of hyperkalemia in the isolated rat heart: a prospective, dose-response study.
Bisogno, JL; Langley, A; Von Dreele, MM, 1994
)
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
" Ampiroxicam itself is not observed in plasma after oral dosing to man, nor in the rat, dog, and monkey as reported here."( Ampiroxicam, an anti-inflammatory agent which is a prodrug of piroxicam.
Carty, TJ; Falkner, FC; Marfat, A; Moore, PF; Twomey, TM; Weissman, A, 1993
)
0.29
" Likewise, dose-response relationships concerning heat production at 60 min depended on the composition of the media."( Dissipation of the calcium gradient in human erythrocytes results in increased heat production.
Engström, I; Nilsson-Ehle, P; Ronquist, G; Waldenström, A, 1993
)
0.29
" Pharmacokinetic studies indicate that after oral dosing L-680,833 is bioavailable in rats and rhesus monkeys."( Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Brause, K; Chandler, GO; Doherty, JB; Dorn, CP; Finke, PE; Hagmann, WK; Hale, JJ; Kissinger, AL; Shah, SK; Thompson, KR, 1993
)
0.29
" Such a complex dose-response effect may have significant impact in explaining the pathologic effects of NO2."( Dual effect of nitrogen dioxide on rat alveolar macrophage arachidonate metabolism.
Forman, HJ; Robison, TW,
)
0.13
" EC50s of the dose-response curves for adrenaline, AII and PDBU were also markedly increased in aortae from DM rats compared to controls."( Differential changes of adrenoceptor- and muscarinic receptor-linked prostacyclin synthesis by the aorta and urinary bladder of the diabetic rat.
Jeremy, JY; Mikhailidis, DP; Thompson, CS, 1993
)
0.29
" Dose-response curves showed a maximum at 10(-8) M morphine."( Direct influence of morphine on the release of arachidonic acid and its metabolites.
Mevkh, AT; Sergeeva, MG; Terentjeva, IV; Varfolomeev, SD, 1993
)
0.29
" In acini prepared from the camostate-treated rats, responsiveness to both CCK-8 and carbamylcholine was greatly decreased with no shift in the dose-response curves compared to control acini prepared from saline-treated rats."( Chronic oral administration of synthetic trypsin inhibitor camostate reduces amylase release from isolated rat pancreatic acini.
Fujii, M; Nakamura, T; Okabayashi, Y; Otsuki, M; Tani, S, 1995
)
0.29
" Dose-response curves to ACh, A23187, and SNP were generated in isolated pulmonary artery rings preconstricted with phenylepherine."( Antibody-mediated neutrophil depletion preserves pulmonary vasomotor function.
Agrafojo, J; Cleveland, JC; Eisenach, JH; Fullerton, DA; Harken, AH; McIntyre, RC; Meldrum, DR; Sheridan, BC, 1996
)
0.29
" Dose-response relationships were analyzed by probit dose-response methods and protective ratios for each compound were computed."( The effects of EDRF/NO releasers or calcium ionophore A23187 on cyanide toxicity in mice.
Baskin, SI; Lempka, JC; Nealley, EW, 1996
)
0.29
" The dose-response curve for stimulation by betagamma subunits of the m2 and rhodopsin phosphorylation was shifted to the higher concentration of betagamma subunits by addition of Ca2+-calmodulin."( Ca2+-dependent inhibition of G protein-coupled receptor kinase 2 by calmodulin.
Haga, K; Haga, T; Tsuga, H, 1997
)
0.3
" Although its ability to inhibit the cyclooxygenase pathway was readily observed in whole blood and in vivo, tenidap's 5-LO blockade could not be demonstrated by ionophore stimulated human blood, nor after oral dosing in rat models in which peritoneal leukotriene products were measured after challenge with three different stimuli."( Tenidap inhibits 5-lipoxygenase product formation in vitro, but this activity is not observed in three animal models.
Carty, TJ; Cheng, JD; Ernest, MJ; Eskra, JD; Griffiths, RJ; Joseph, PA; Kadin, SB; Loose, LD; Moore, PF; Murase, S; Nagahisa, A; Pazoles, PP; Pillar, JS; Sweeney, FJ, 1997
)
0.3
" Dose-response curves for A23187 and PMA were derived for the three functions."( Functional characterization of equine neutrophils in response to calcium ionophore A23187 and phorbol myristate acetate ex vivo.
Chilcoat, C; Crisman, M; Eyre, P; Moore, T; Wilcke, J, 1997
)
0.3
" Plasma concentration-time relationships and pharmacokinetic parameters for BAY Y 1015 administered intravenously and orally to six horses at a dosage of 10 mg/kg in a two period cross-over study were established."( Pharmacology of the 5-lipoxygenase inhibitors BAY Y 1015 and BAY X 1005 in the horse.
Andrews, M; Cunningham, FM; Landoni, MF; Lees, P, 1997
)
0.3
" Dose-response curves of gallbladder strips to cholecystokinin (CCK), bethanechol, and potassium (K+) were constructed in vitro."( The basis for progesterone impairment of gallbladder contractility in male guinea pigs in vitro.
Kiaii, B; Shaffer, EA; Xu, QW, 1998
)
0.3
" Dose-response curves were plotted, and calculations were performed to identify concentrations that caused 50% inhibition (IC50 [microM]) for each isozyme."( Evaluation of selective inhibition of canine cyclooxygenase 1 and 2 by carprofen and other nonsteroidal anti-inflammatory drugs.
Lundy, KM; Ricketts, AP; Seibel, SB, 1998
)
0.3
" The rings were suspended for isometric tension recording and contracted with phenylephrine, and cumulative dose-response curves for ACh or calcium ionophore (A-23187) were generated."( Superoxide anion scavengers restore NO-mediated pulmonary vasodilation after lung transplantation.
Flavahan, NA; Murray, PA; Seki, S; Smedira, NG, 1999
)
0.3
" In streptolysin-O permeabilized acini, 10 nM adrenomedullin shifted the calcium dose-response curve to the right, indicating that adrenomedullin inhibits calcium-induced amylase secretion by reducing calcium sensitivity of the pancreatic exocytotic machinery."( Inhibition of stimulated amylase secretion by adrenomedullin in rat pancreatic acini.
Fujita, T; Mine, T; Ohnishi, H; Tanaka, Y; Tsuchida, T, 1999
)
0.3
" Dose-response curves were obtained with acetylcholine, sodium nitroprusside, and calcium ionophore A23187 following contraction with phenylephrine (10(-6) M) in the presence of indomethacin (10(-5) M)."( A model of xenograft hyperacute rejection attenuates endothelial nitric oxide production: a mechanism for graft vasospasm?
Cable, DG; Hisamochi, K; Schaff, HV, 1999
)
0.3
" Atropine displaced the dose-response curve for carbamylcholine to the right so that in the presence of 7 microM atropine a concentration of 1 mM carbamylcholine now gave an optimal rate of enzyme secretion."( Morphological changes in rat pancreatic slices associated with inhibition of enzyme secretion by high concentrations of secretagogues.
Savion, N; Selinger, Z, 1978
)
0.26
" Western blotting confirmed that VT (50 to 1000 ng/ml) also significantly diminished GRP/BiP protein levels in a dose-response manner in PMA/ION-stimulated cells."( Down-regulation of the endoplasmic reticulum chaperone GRP78/BiP by vomitoxin (Deoxynivalenol).
Li, S; Pestka, JJ; Yang, GH, 2000
)
0.31
" The dose-response curve of the calculated AUC is consistent with the bell-shaped dose-response curve for antigen-induced mediator release, depolarization and 86Rb(+)-efflux."( The characterization and quantification of antigen-induced Ca2+ oscillations in a rat basophilic leukaemia cell line (RBL-2H3).
Assem, ES; Marsh, SJ; Narenjkar, J, 1999
)
0.3
" Clofibrate at lower concentrations (10-200 microM) produced increases in the mRNA levels of cPLA(2) in a dose-response manner."( Modulation of cytosolic phospholipase A(2) by PPAR activators in human preadipocytes.
Choy, PC; Dembinski, T; Hatch, GM; Jiang, YJ; Kroeger, EA; Mymin, D, 2001
)
0.31
" Inhibitory concentration (IC50) values for a number of compounds were calculated as means +/- SEM from dose-response determinations."( Second messengers in platelet aggregation evoked by serotonin and A23187, a calcium ionophore.
Cheema, M; Connor, JD; Gilani, AH; Rasheed, H; Rizvi, Z; Saeed, SA, 2001
)
0.31
" Our data suggested that PMA stimulated the production of superoxide anion in a dose-response manner, as compared with A23187, which did not induce a significant release of superoxide anion in PMNs-RA."( Phospholipase A2 modulates respiratory burst developed by neutrophils in patients with rheumatoid arthritis.
Bostan, M; Brasoveanu, LI; Constantin, MC; Galatiuc, C; Hirt, M; Iordachescu, D,
)
0.13
" In endothelium-intact rings precontracted with phenylephrine 10(-6) M, dose-response curves for acetylcholine (10(-9) to 10(-5) M) and calcium ionophore (10(-9) to 10(-6) M) were generated in the presence and absence of etomidate (5 x10(-6) 10(-5) M)."( Effect of etomidate on endothelium-dependent relaxation induced by acetylcholine in rat aorta.
Cho, HC; Chung, YK; Kim, HJ; Lee, HK; Shin, IW; Sohn, JT, 2004
)
0.32
" The differential responsiveness of JNK and p38 was dependent on the duration of treatment, as well as on the dosage of CKBM."( Immuno-regulatory effects of CKBM on the activities of mitogen-activated protein kinases and the release of cytokines in THP-1 monocytic cells.
Chan, AS; Luk, SC; Pang, H; Pang, SF; Wong, YH; Yip, EC; Yung, LY, 2005
)
0.33
" Dose-response curves to the Ca(2+) ionophore A-23187 and to the calmodulin/myosin light chain kinase inhibitor W-7 served to study Ca(2+)-dependent pathways."( Both Ca2+ -dependent and -independent pathways are involved in rat hepatic stellate cell contraction and intrahepatic hyperresponsiveness to methoxamine.
Bisschops, R; Cassiman, D; Fevery, J; Laleman, W; Nevens, F; Roskams, T; Severi, T; Van Landeghem, L; Van Pelt, J; Vander Elst, I; Zeegers, M, 2007
)
0.34
" In the rat air pouch model, oral dosing of CJ-13,610 and zileuton resulted in selective inhibition 5-LOX activity from pouch exudate and ex vivo rat whole blood with similar potency to in vitro assay."( A rat air pouch model for evaluating the efficacy and selectivity of 5-lipoxygenase inhibitors.
Anderson, GD; Dufield, DR; Hardy, MM; Masferrer, JL; Pufahl, RA; Zweifel, BS, 2008
)
0.35
" For OB assays, dose-response curves were performed for each activator."( Oxidative burst assessment and neutrophil-platelet complexes in unlysed whole blood.
Avendaño, A; Marin, L; Marin, P; Petriz, J; Sales-Pardo, I, 2008
)
0.35
" In addition, two narrow bell-shaped dose-response curves were identified with maxima in either the nanomolar or low micromolar NAADP concentration range, where TPC1 was found to be responsible for activating the low affinity pathway."( NAADP and the two-pore channel protein 1 participate in the acrosome reaction in mammalian spermatozoa.
Arlt, E; Arndt, L; Biel, M; Boekhoff, I; Borth, H; Breit, A; Castonguay, J; Gudermann, T; Hassan, S; Klugbauer, N; Meyer, D; Wahl-Schott, C; Wennemuth, G; Zierler, S, 2014
)
0.4
" The results implicate a serine hydrolase in regulating ER calcium release and highlight the importance of careful dose-response studies with pyrrophenone to study cPLA2α function."( Off-target effect of the cPLA2α inhibitor pyrrophenone: Inhibition of calcium release from the endoplasmic reticulum.
Ewing, H; Gelb, MH; Lee, H; Leslie, CC; Yun, B, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzoxazoleCompounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.
[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 (82)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency6.30960.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.74070.140911.194039.8107AID2451
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency12.58930.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency11.90470.177814.390939.8107AID2147
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency35.48130.125919.1169125.8920AID2549
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID2323
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
endonuclease IVEscherichia coliPotency3.98110.707912.432431.6228AID1708
glp-1 receptor, partialHomo sapiens (human)Potency2.23870.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency21.47680.100020.879379.4328AID488772; AID488773; AID588453; AID588456
ClpPBacillus subtilisPotency27.28241.995322.673039.8107AID743245
ATAD5 protein, partialHomo sapiens (human)Potency15.95780.004110.890331.5287AID493106; AID493107; AID504467
Fumarate hydrataseHomo sapiens (human)Potency7.07950.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency46.94500.031637.5844354.8130AID540327
GLS proteinHomo sapiens (human)Potency9.69850.35487.935539.8107AID624146; AID624170
TDP1 proteinHomo sapiens (human)Potency0.10470.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency23.73590.180013.557439.8107AID1460
TSHR proteinHomo sapiens (human)Potency11.50530.338119.046637.9330AID602292; AID602441
Smad3Homo sapiens (human)Potency3.65420.00527.809829.0929AID588855; AID720534; AID720536; AID720537
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency3.98110.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency19.95260.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency19.01150.001318.074339.8107AID488980; AID504821
regulator of G-protein signaling 4Homo sapiens (human)Potency63.33980.531815.435837.6858AID504845
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency14.43260.28189.721235.4813AID2326
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency11.68690.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823
polyproteinZika virusPotency7.07950.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency3.03000.00018.4406100.0000AID720579; AID720580
glucocerebrosidaseHomo sapiens (human)Potency35.48130.01268.156944.6684AID2101
ParkinHomo sapiens (human)Potency29.09290.819914.830644.6684AID720573
arylsulfatase AHomo sapiens (human)Potency8.49211.069113.955137.9330AID720538
IDH1Homo sapiens (human)Potency1.45810.005210.865235.4813AID686970
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency1.69770.016525.307841.3999AID504836; AID602332
serine-protein kinase ATM isoform aHomo sapiens (human)Potency39.81070.707925.111941.2351AID485349
Bloom syndrome protein isoform 1Homo sapiens (human)Potency15.84890.540617.639296.1227AID2364; AID2528
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency35.48130.036619.637650.1187AID2100
hexokinase-4 isoform 1Homo sapiens (human)Potency2.81842.511913.800328.1838AID743205
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency146.02550.01262.451825.0177AID485313
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency6.012023.934123.934123.9341AID1967
D(1A) dopamine receptorHomo sapiens (human)Potency0.37640.02245.944922.3872AID488981; AID488983
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.18380.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency44.66840.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency0.00600.006026.168889.1251AID488953
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency1.15820.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency28.18383.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.16230.01789.637444.6684AID588834
glucokinase regulatory proteinHomo sapiens (human)Potency2.81842.511913.800328.1838AID743205
huntingtin isoform 2Homo sapiens (human)Potency0.89130.000618.41981,122.0200AID1688
mitogen-activated protein kinase 1Homo sapiens (human)Potency26.96800.039816.784239.8107AID1454
flap endonuclease 1Homo sapiens (human)Potency2.99350.133725.412989.1251AID588795
ras-related protein Rab-9AHomo sapiens (human)Potency31.01450.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency5.27460.00378.618923.2809AID2660; AID2666; AID2667; AID2668
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency18.88760.168316.404067.0158AID720504
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.11870.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.12200.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency1.12200.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.12200.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency1.25890.00798.23321,122.0200AID2546
gemininHomo sapiens (human)Potency11.05030.004611.374133.4983AID463097; AID504364; AID624296; AID624297
VprHuman immunodeficiency virus 1Potency12.58931.584919.626463.0957AID651644
survival motor neuron protein isoform dHomo sapiens (human)Potency8.91250.125912.234435.4813AID1458
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.95260.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency2.99040.891312.067628.1838AID1459; AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency3.77950.015812.3113615.5000AID1461; AID1489; AID1491; AID2567; AID2568
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency46.77916.309660.2008112.2020AID720707; AID720709
Alpha-synucleinHomo sapiens (human)Potency6.51310.56239.398525.1189AID652106
D(1A) dopamine receptorSus scrofa (pig)Potency1.46890.00378.108123.2809AID2667
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.94331.995325.532750.1187AID624288
TAR DNA-binding protein 43Homo sapiens (human)Potency10.00001.778316.208135.4813AID652104
Ataxin-2Homo sapiens (human)Potency3.16230.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.02390.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
XBP1Homo sapiens (human)IC50 (µMol)1.41000.16005.404910.0000AID504313
type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)40.00002.22108.230418.7980AID463214
apelin receptorHomo sapiens (human)IC50 (µMol)40.00001.75003.39008.3500AID2784
DNA damage-inducible transcript 3 proteinMus musculus (house mouse)IC50 (µMol)0.16000.16003.995910.0000AID504322
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
electroneutral potassium-chloride cotransporter KCC2Homo sapiens (human)EC50 (µMol)12.68000.48101.53032.3100AID1723; AID1736
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)0.06000.06008.9128130.5170AID1902
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC501.07400.19503.667918.6960AID540270
HSP40, subfamily A [Plasmodium falciparum 3D7]Plasmodium falciparum 3D7AbsAC1000_uM0.66200.12904.116911.3160AID540271
heat shock protein 90, putativePlasmodium falciparum 3D7AC500.81300.19504.992098.5000AID540268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (190)

Processvia Protein(s)Taxonomy
angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 3Homo sapiens (human)
signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 3Homo sapiens (human)
associative learningRap guanine nucleotide exchange factor 3Homo sapiens (human)
Rap protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of actin cytoskeleton organizationRap guanine nucleotide exchange factor 3Homo sapiens (human)
negative regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
intracellular signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of GTPase activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of angiogenesisRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of protein export from nucleusRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of stress fiber assemblyRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
positive regulation of syncytium formation by plasma membrane fusionRap guanine nucleotide exchange factor 3Homo sapiens (human)
establishment of endothelial barrierRap guanine nucleotide exchange factor 3Homo sapiens (human)
cellular response to cAMPRap guanine nucleotide exchange factor 3Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 3Homo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
cognitionAmyloid-beta precursor proteinHomo sapiens (human)
G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglial cell activationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
suckling behaviorAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activation involved in immune responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of translationAmyloid-beta precursor proteinHomo sapiens (human)
protein phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
intracellular copper ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
endocytosisAmyloid-beta precursor proteinHomo sapiens (human)
response to oxidative stressAmyloid-beta precursor proteinHomo sapiens (human)
cell adhesionAmyloid-beta precursor proteinHomo sapiens (human)
regulation of epidermal growth factor-activated receptor activityAmyloid-beta precursor proteinHomo sapiens (human)
Notch signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
axonogenesisAmyloid-beta precursor proteinHomo sapiens (human)
learning or memoryAmyloid-beta precursor proteinHomo sapiens (human)
learningAmyloid-beta precursor proteinHomo sapiens (human)
mating behaviorAmyloid-beta precursor proteinHomo sapiens (human)
locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
axo-dendritic transportAmyloid-beta precursor proteinHomo sapiens (human)
cholesterol metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of cell population proliferationAmyloid-beta precursor proteinHomo sapiens (human)
adult locomotory behaviorAmyloid-beta precursor proteinHomo sapiens (human)
visual learningAmyloid-beta precursor proteinHomo sapiens (human)
regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of gene expressionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
microglia developmentAmyloid-beta precursor proteinHomo sapiens (human)
axon midline choice point recognitionAmyloid-beta precursor proteinHomo sapiens (human)
neuron remodelingAmyloid-beta precursor proteinHomo sapiens (human)
dendrite developmentAmyloid-beta precursor proteinHomo sapiens (human)
regulation of Wnt signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
extracellular matrix organizationAmyloid-beta precursor proteinHomo sapiens (human)
forebrain developmentAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection developmentAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of chemokine productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-1 beta productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of interleukin-6 productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of tumor necrosis factor productionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of multicellular organism growthAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of neuron differentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of glycolytic processAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of mitotic cell cycleAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of JNK cascadeAmyloid-beta precursor proteinHomo sapiens (human)
astrocyte activationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAmyloid-beta precursor proteinHomo sapiens (human)
collateral sprouting in absence of injuryAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of inflammatory responseAmyloid-beta precursor proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationAmyloid-beta precursor proteinHomo sapiens (human)
regulation of synapse structure or activityAmyloid-beta precursor proteinHomo sapiens (human)
synapse organizationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular process controlling balanceAmyloid-beta precursor proteinHomo sapiens (human)
synaptic assembly at neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of protein metabolic processAmyloid-beta precursor proteinHomo sapiens (human)
neuron apoptotic processAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulum calcium ion homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
neuron cellular homeostasisAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAmyloid-beta precursor proteinHomo sapiens (human)
response to interleukin-1Amyloid-beta precursor proteinHomo sapiens (human)
modulation of excitatory postsynaptic potentialAmyloid-beta precursor proteinHomo sapiens (human)
NMDA selective glutamate receptor signaling pathwayAmyloid-beta precursor proteinHomo sapiens (human)
regulation of spontaneous synaptic transmissionAmyloid-beta precursor proteinHomo sapiens (human)
cytosolic mRNA polyadenylationAmyloid-beta precursor proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of long-term synaptic potentiationAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionAmyloid-beta precursor proteinHomo sapiens (human)
cellular response to amyloid-betaAmyloid-beta precursor proteinHomo sapiens (human)
regulation of presynapse assemblyAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
amyloid fibril formationAmyloid-beta precursor proteinHomo sapiens (human)
neuron projection maintenanceAmyloid-beta precursor proteinHomo sapiens (human)
positive regulation of T cell migrationAmyloid-beta precursor proteinHomo sapiens (human)
central nervous system developmentAmyloid-beta precursor proteinHomo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
protein domain specific bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 3Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
DNA bindingAmyloid-beta precursor proteinHomo sapiens (human)
serine-type endopeptidase inhibitor activityAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
heparin bindingAmyloid-beta precursor proteinHomo sapiens (human)
enzyme bindingAmyloid-beta precursor proteinHomo sapiens (human)
identical protein bindingAmyloid-beta precursor proteinHomo sapiens (human)
transition metal ion bindingAmyloid-beta precursor proteinHomo sapiens (human)
receptor ligand activityAmyloid-beta precursor proteinHomo sapiens (human)
PTB domain bindingAmyloid-beta precursor proteinHomo sapiens (human)
protein serine/threonine kinase bindingAmyloid-beta precursor proteinHomo sapiens (human)
signaling receptor activator activityAmyloid-beta precursor proteinHomo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (68)

Processvia Protein(s)Taxonomy
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
cortical actin cytoskeletonRap guanine nucleotide exchange factor 3Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
microvillusRap guanine nucleotide exchange factor 3Homo sapiens (human)
endomembrane systemRap guanine nucleotide exchange factor 3Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 3Homo sapiens (human)
lamellipodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
filopodiumRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular exosomeRap guanine nucleotide exchange factor 3Homo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
dendriteAmyloid-beta precursor proteinHomo sapiens (human)
extracellular regionAmyloid-beta precursor proteinHomo sapiens (human)
extracellular spaceAmyloid-beta precursor proteinHomo sapiens (human)
nuclear envelope lumenAmyloid-beta precursor proteinHomo sapiens (human)
cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
mitochondrial inner membraneAmyloid-beta precursor proteinHomo sapiens (human)
endosomeAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
endoplasmic reticulum lumenAmyloid-beta precursor proteinHomo sapiens (human)
smooth endoplasmic reticulumAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
Golgi lumenAmyloid-beta precursor proteinHomo sapiens (human)
Golgi-associated vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cytosolAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
clathrin-coated pitAmyloid-beta precursor proteinHomo sapiens (human)
cell-cell junctionAmyloid-beta precursor proteinHomo sapiens (human)
synaptic vesicleAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
membraneAmyloid-beta precursor proteinHomo sapiens (human)
COPII-coated ER to Golgi transport vesicleAmyloid-beta precursor proteinHomo sapiens (human)
axonAmyloid-beta precursor proteinHomo sapiens (human)
growth coneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule lumenAmyloid-beta precursor proteinHomo sapiens (human)
neuromuscular junctionAmyloid-beta precursor proteinHomo sapiens (human)
endosome lumenAmyloid-beta precursor proteinHomo sapiens (human)
trans-Golgi network membraneAmyloid-beta precursor proteinHomo sapiens (human)
ciliary rootletAmyloid-beta precursor proteinHomo sapiens (human)
dendritic spineAmyloid-beta precursor proteinHomo sapiens (human)
dendritic shaftAmyloid-beta precursor proteinHomo sapiens (human)
perikaryonAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
apical part of cellAmyloid-beta precursor proteinHomo sapiens (human)
synapseAmyloid-beta precursor proteinHomo sapiens (human)
perinuclear region of cytoplasmAmyloid-beta precursor proteinHomo sapiens (human)
presynaptic active zoneAmyloid-beta precursor proteinHomo sapiens (human)
spindle midzoneAmyloid-beta precursor proteinHomo sapiens (human)
recycling endosomeAmyloid-beta precursor proteinHomo sapiens (human)
extracellular exosomeAmyloid-beta precursor proteinHomo sapiens (human)
receptor complexAmyloid-beta precursor proteinHomo sapiens (human)
early endosomeAmyloid-beta precursor proteinHomo sapiens (human)
membrane raftAmyloid-beta precursor proteinHomo sapiens (human)
cell surfaceAmyloid-beta precursor proteinHomo sapiens (human)
Golgi apparatusAmyloid-beta precursor proteinHomo sapiens (human)
plasma membraneAmyloid-beta precursor proteinHomo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
AID1478484Cytotoxic activity against human HeLa cells at 1.91 uM by cytological profiling assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Naphthablins B and C, Meroterpenoids Identified from the Marine Sediment-Derived Streptomyces sp. CP26-58 Using HeLa Cell-Based Cytological Profiling.
AID562241Antimycobacterial activity against Mycobacterium smegmatis grown in carbon-limited broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID562245Antimycobacterial activity against Mycobacterium smegmatis grown in nitrogen -limited broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID562244Antimycobacterial activity against Mycobacterium smegmatis grown in carbon-limited broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID562243Antimycobacterial activity against Mycobacterium smegmatis grown in Luria-Bertani broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID562240Antimycobacterial activity against Mycobacterium smegmatis grown in Luria-Bertani broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID755632Activation of human BKCA alpha channel expressed in HEK293 cells assessed as increase in intracellular calcium level at 10 uM after 30 mins2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Large conductance Ca(2+)-activated K(+) channel (BKCa) activating properties of a series of novel N-arylbenzamides: Channel subunit dependent effects.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
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.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1478480Cytotoxic activity against human HeLa cells at 0.382 uM by cytological profiling assay2017Journal of natural products, 03-24, Volume: 80, Issue:3
Naphthablins B and C, Meroterpenoids Identified from the Marine Sediment-Derived Streptomyces sp. CP26-58 Using HeLa Cell-Based Cytological Profiling.
AID562242Antimycobacterial activity against Mycobacterium smegmatis grown in nitrogen -limited broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11,609)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905166 (44.50)18.7374
1990's4553 (39.22)18.2507
2000's1381 (11.90)29.6817
2010's431 (3.71)24.3611
2020's78 (0.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials40 (0.33%)5.53%
Reviews118 (0.99%)6.00%
Case Studies43 (0.36%)4.05%
Observational1 (0.01%)0.25%
Other11,744 (98.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficacy of Oocyte Activation With Two Types of Ca2+ Ionophore: a Prospective Randomized Study. [NCT06106412]44 participants (Anticipated)Interventional2024-01-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]