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1 EC50s for the metabolite mixtures formed by ELW1 were lo
3 lations between functional output, such as 1/EC50, and effective kinetic constants for a range of dif
4 ara-methoxyphenyl at C-8 led to compound 12 (EC50 = 0.022 muM), twice as potent as its para-bromo ana
5 luoro-1H-indole-3-yl)methane (38, PSB-15160, EC50 80.0 nM) and di(5,7-difluoro-1H-indole-3-yl)methane
8 ervatives reduce proteinase activity by 50% (EC50) at a much lower concentration than their acceptabl
9 AIMP (9; EC50 of 6.4 muM) and analogs 52-56 (EC50 of 0.4-4.7 muM), which contain one or two 2'-fluoro
11 onship modeling yielded analogues (i.e., 8n: EC50 = 0.06 muM, SI 500) that establish a platform for t
12 y cytokines: for the former, 3',3'-cAIMP (9; EC50 of 6.4 muM) and analogs 52-56 (EC50 of 0.4-4.7 muM)
13 lar potency and selectivity to salvinorin A (EC50 = 0.6 +/- 0.2 nM at kappa; >10000 nM at mu and delt
15 ydrogen peroxide scavenger than gallic acid (EC50 838 mug/mL) and was equally strong as quercetin in
16 ) than their corresponding phosphonic acids (EC50 = 50-343 nM) in protection of cells from the viral
17 nM, D3 = 1.15 nM) and full agonist activity (EC50 (GTPgammaS); D2 = 3.23 and D3 = 1.41 nM) at both D2
18 ts with higher initial antioxidant activity (EC50 values: 214 and 272mg.mL(-1)) that decreased after
21 pound 15c displayed low micromolar activity (EC50 value of ca. 2 muM) and limited cytotoxic liability
23 selected for development based on activity (EC50 = 0.21 muM, selectivity index (SI) 40) and scaffold
26 ouse endothelial PECAM-1 with high affinity (EC50 1.5 and 3.8 nM, respectively), and codelivery induc
27 b, and 8c) are better anti-influenza agents (EC50 = 19-89 nM) than their corresponding phosphonic aci
28 0.63 nM) and highly selective kappa agonist (EC50 = 1.8 nM) selective for the periphery with dose-dep
30 MP-2; 200 ng), 1 muM CGS21680 (A2AR agonist, EC50 = 160 nM), or 1 muM dipyridamole (EC50 = 32 nM) pro
32 y of nine compounds that were MC3R agonists (EC50 < 1000 nM) and MC4R antagonists (5.7 < pA2 < 7.8).
33 otubes treated with MR agonist (aldosterone; EC50 1.3 nM) or antagonist (spironolactone; IC50 1.6 nM)
36 ing an EC50 of 4.69 muM against HIV-1 and an EC50 value of 0.5 muM against HBV, whereas completely la
37 compound 32, with a Kd value of 32 nM and an EC50 value of 0.67 muM in a surrogate cellular biomarker
38 With a K(+)/Na(+) selectivity of 9.8 and an EC50 value of 6.2 muM for K(+) ion, 5F8 is clearly among
39 nd impaired HIV-1 infection of T cells at an EC50 of 36 mum The identified lead compound, with a rela
40 -methyl compound (+)-15a, which displayed an EC50 of 23 nM in the calcium flux assay while showing no
42 h an IC50 value of 14 nM, which displayed an EC50 value of 2.1 muM against H1N1 influenza virus in MD
43 with potent antiviral activity displaying an EC50 of 4.69 muM against HIV-1 and an EC50 value of 0.5
44 was explored, leading to compounds having an EC50 as low as 25 nM against T. b. brucei and being more
45 le-phenyl analogue RP-13s (IDX899) having an EC50 of 11 nM against the Y181C/K103N double mutant.
48 he N-benzyl compound (+)-19, which showed an EC50 of 24 nM at the 5-HT2C receptor, is fully selective
54 ed the highest antioxidant capacity, with an EC50 of 0.97mg/mL, and total flavonoids (44.7 epicatechi
56 ted PARylation in a whole-cell assay with an EC50 of 2.51 nM and prevents proliferation of cancer cel
59 epidermal cancer stem cell invasion with an EC50 of 3.9 muM, representing a significant improvement
60 l)-NAADP was shown to release Ca(2+) with an EC50 of 31 muM and to compete with NAADP for receptor bi
62 nductance regulator (CFTR) activator with an EC50 of approximately 200 nM and demonstrated its therap
64 2-fold at a concentration of 300 muM with an EC50 value of 159 muM, whereas no potentiation of the gl
65 l-based assays of virus replication, with an EC50 value of 3.4 muM at DENV-2 and 15.5 muM at WNV for
66 in a concentration-dependent manner with an EC50 value of approximately 0.2 microM and maximal cGMP
67 as also quantitatively assessed, yielding an EC50 value that agrees well with conventional biochemica
69 aximum effect at approximately 50 nmol/L and EC50 values for both cytokines of approximately 10 nmol/
73 stimulation with 100 nm ACh ( approximately EC50), [Ca(2+)]i increased as V(m) hyperpolarized below
74 , we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 12
76 eptor internalization in a cell-based assay (EC50 = 0.05 muM), but has poor physical properties and m
78 aging plate reader (FLIPR) functional assay (EC50, 36 nM) and carbachol in a hippocampal slice electr
79 ency in the beta-arrestin recruitment assay (EC50 0.9 nM) compared with the G alphai-activation assay
81 lioblastoma (GBM) cells and with astonishing EC50 value (38 pM) when loaded with a PI3K-mTOR inhibito
82 (-1)), Ag internalized by the algal cells at EC50 was similar (0.8 to 3.6 ngAg mL(-1)) for all AgNP t
83 er half-maximal effective concentration (AUC:EC50) of 108.6 is estimated to result in a negative GMI
84 ly, corrected pore-water-concentration-based EC50 values were calculated by equilibrium partitioning
86 to explain the observed discrepancy between EC50 and Kd These results indicate that the mechanism by
88 synthesis of antimalarial compound BRD3914 (EC50 = 15 nM) that hinges on a Pd-catalyzed, directed C(
89 activity against Trypanosoma brucei brucei (EC50 = 2.97 muM), thus being considered as a novel lead
90 two dioxin-like chemicals and the calculated EC50 values were concordant with domestic avian species
93 antileukemic activity against M9-ENL1 cells (EC50 = 0.57-2.90 muM) when compared to parthenolide (EC5
98 Ca(2+) influx through TRPA1 cation channels (EC50 ca. 200 nM), thereby explaining its ability to stim
99 at much lower exposures in the PB cocktail (EC50: 0.94 vs 6.06 mug/mL; P < 0.01), whereas the KW coc
100 ion of half-maximum effective concentration (EC50) across tested NPs (5.4 to 300 ngAg mL(-1)), Ag int
101 decrease in the 50% effective concentration (EC50) for activation through CD16, and a 38% decrease in
104 at ASM half-maximum effective concentration (EC50) or Vmax contribute to AHR in asthma, but, because
105 The half-maximal effective concentration (EC50) value of the time-resolved fluorescence resonance
106 PAR1 (effective half-maximal concentration (EC50), 8.4 +/- 1.1 versus 4.3 +/- 1.1 mum) and glycoprot
107 observed at the highest test concentration (EC50 > 3397 mumol L(-1) and >4892 mumol kg(-1) dry weigh
108 sensitivities (50% effective concentration [EC50]) of mutant and wild-type viruses to nine FDA-appro
109 ition (half maximal effective concentration [EC50]: 0.21 +/- 0.18 vs. 1.38 +/- 0.54 nM) and receptor
111 ce, richness, and biomass at concentrations (EC50's ranged from 197.6 to 233.5 ng bifenthrin/g organi
113 ity of ILs, median effective concentrations (EC50) and critical micelle concentrations (CMC) were det
116 A549, MCF-7) with effective concentrations (EC50) typically below 5 nM, at least an order of magnitu
117 Mean half maximal inhibitory concentrations (EC50) for calcium, magnesium and zinc were 270+/-18, 253
118 V-1(WT)), with 50% effective concentrations (EC50s) of 3.0 to 49 nM, and exhibited minimal cytotoxici
121 luded that the proposed model for converting EC50 into TEAC values and TEAC into EC50 values works pr
123 10 (MRS7232) esters enhanced binding at DAT (EC50 approximately 35 nM) and at the norepinephrine tran
126 alpha3-beta4-alpha3-alpha3, LYPD6B decreased EC50 from 631 to 79 muM, reduced Imax by at least 59%, a
130 re observed between the results of the DPPH (EC50=0.6-1105.3 mug/ml) and FRAP (0.1-8.5 mmol/g) assays
131 V for ERG3 (EC50 = 374 nM), -28 mV for EAG1 (EC50 = 1.18 muM), and more than -100 mV for ELK1 (EC50 =
132 ffort identified 4b (GS-5734) with anti-EBOV EC50 = 86 nM in macrophages as the clinical candidate.
133 pyridone amides that are highly efficacious (EC50 </= 100 nM) in attenuating infectivity across multi
135 t activation of currents by -14 mV for ERG1 (EC50 = 414 nM), -20 mV for ERG3 (EC50 = 374 nM), -28 mV
136 V for ERG1 (EC50 = 414 nM), -20 mV for ERG3 (EC50 = 374 nM), -28 mV for EAG1 (EC50 = 1.18 muM), and m
138 c responses was xDP > xFP > waDP (e.g., EROD EC50s were lower for xDP compared to xFP and waDP).
142 tween the calculated Kd and the experimental EC50 on HIV-infected cells confirmed the reliability of
143 with results from voltage-clamp experiments (EC50 values for alpha4beta3delta, alpha1beta3gamma2, and
146 ated within the activity-toxicity framework: EC50 and LC50 values for all three taxa correlated gener
149 lling and the selective agonist GSK1016790A (EC50 approximately 33 nM) induced sustained transmembran
152 ty of the mixture with the experimental 96 h EC50 for the antibiotic mixture being 0.248 mumol/L comp
153 922-0796, F1609-0442, and F1750-0048) having EC50 (50% effective concentration) values of 4.8 +/- 2.3
154 potent and selective NS5A inhibitor of HCV (EC50 = 4.6 nM), with greater therapeutic index (CC50/EC5
156 ), which is 16-fold selective for the hMC1R (EC50 = 4.5 nM) versus other melanocortin receptors.
158 tivation through CD16, and a 38% decrease in EC50 for NK group 2 member D (NKG2D)-mediated activation
161 tration required for half-maximal induction (EC50) of GR-mediated gene expression by acting at a mini
163 was a stronger alpha-glucosidase inhibitor (EC50 2.9 mug/mL) than quercetin, with weak antiamylase a
164 4-phenylthiazole 18, a modest HCV inhibitor (EC50 = 9440 nM), a series of structurally related thiazo
167 8 +/- 0.54 nM) and receptor internalization (EC50: 41.9 +/- 29.8 vs. 455 +/- 299 nM) than Cu-DA(IR800
170 oratory and primary clinical HIV-1 isolates (EC50: 0.0014-0.0028 muM) with minimal cytotoxicity (CC50
173 nists ATP-magnesium salt (Mg-ATP; 100 mg/kg, EC50 approximately 1.32 mM) and benzoylbenzoyl-ATP (Bz-A
174 M) and benzoylbenzoyl-ATP (Bz-ATP; 10 mg/kg, EC50 approximately 285 muM), and antagonist oxidized ATP
176 id residues in Gag correlated with lopinavir EC50 (p < 0.01), of which 380 K and 389I showed modest i
177 IC50 ranging from 0.021 to 0.041 mg/mg, low EC50 from 0.92 to 1.78 mg/mg DPPH, high ARP values (56.1
180 etagogues, we found that PGE2 had the lowest EC50 value with regard to the induction of swelling of t
181 was significantly correlated with the lowest EC50 values for all the tested antioxidant activity assa
184 on of influenza virus encoding wild-type M2 (EC50 = 2.3 microM), both 27: and tert-butyl 4'-(carbamim
186 The various applications of the Deltalog(max/EC50) scale are described for each pharmacologic applica
190 8-negative T-cells, the third highest median EC50, and significant correlations with frequencies of t
191 D28-negative T-cells with the highest median EC50, and the least differentiated, high-frequency Tc su
192 amide scaffold provided 17e, a potent (mGlu1 EC50 = 31.8 nM) and highly CNS penetrant (brain to plasm
193 selective agonist activity profile at mGlu2 (EC50 in the micromolar range), whereas 2c/2d were both s
196 ased MMP-13 expression dose [1-10 microg/ml (EC50 0.5-1 mug/ml)] and time (24-72 h) dependently, sign
197 t (Mps1 Ki = 0.09 +/- 0.02 nM; cellular Mps1 EC50 = 6.5 +/- 0.5 nM), highly selective, and orally act
198 y range from low micromolar to sub-nanomolar EC50, the most interesting compounds being 15 (0.97 nM),
201 onist discovered so far (Ki hA2AAR = 4.8 nM, EC50 hA2AAR = 4.9 nM, Ki hA1AR > 10000 nM, Ki hA3AR = 14
207 5 versus 0.26 +/- 0.21 mug/ml) but not PAR4 (EC50, 50 +/- 1 versus 58 +/- 1 mum) signal transduction.
208 .57-2.90 muM) when compared to parthenolide (EC50 = 6.0) and showed potent antileukemic activity agai
209 antioxidant activity after the same period (EC50 values, 0days: 106mg.mL(-1); 7days: 48.7mg.mL(-1)),
210 rtuin 1 (SIRT1) levels in MCECs before PGE2 (EC50 approximately 2.5 mM) or CSE/IL-1beta exposure.
212 structures, MAIT cell activation potencies (EC50 3-500 pM), and chemical stabilities are described.
214 21 displayed a significantly higher potency (EC50 = 40 +/- 4 muM) and a similar efficacy when compare
215 selectively and differentially the potency (EC50) and efficacy (E(max)) of hUII and URP ex vivo in a
216 Arg-(pI)DPhe-DNal(2')-NH2] were more potent (EC50 < 73 nM) than the melanocortin tetrapeptide Ac-His-
217 ad therapeutic window: identified as potent [EC50 < 0.02 mg/kg siRNA against FVII (siFVII)] in dose-r
221 CH2)2-CONH2) displayed the desired profiles (EC50 (hGLP-2R) < 100 pM, CL in rat <0.3 mL/min/kg, selec
224 he breast adenocarcinoma cell line, reaching EC50 values of 34.8 and 60.3 mug/ml for Willamette and M
225 tion associated with half-maximal reduction (EC50) of CD154 expression was calculated for 36 T-cell s
227 centration approximately 15 times the drug's EC50 when treatment is given prophylactically starting a
228 o methoxamine being attenuated (mean +/- SEM EC50 decreased from 5.7 +/- 0.63 mum to 1.6 +/- 0.23 mum
229 to acetylcholine (ACh): agonist sensitivity (EC50), maximal agonist-induced current (Imax), and time
230 is capable of binding with high sensitivity (EC50 of 0.1 to 0.4 mug/mL depending on assay format) whi
231 the most potent H4R agonist in this series (EC50 11 nM; H4R vs H3R, >100-fold selectivity; H1R, H2R,
233 gly, all of these receptors had very similar EC50 values for GABA in the presence of the neurosteroid
235 unds from this study exhibited submicromolar EC50 values against S31N-containing A/WSN/33 influenza v
236 ranked by median EC50, and by whether subset EC50 was correlated with and therefore could be represen
238 e inhibition occurred in standard ISO tests (EC50 values of 15-200 mg Pt/L), but also in a double-via
246 s in the [(3)H]PT-1284 binding assay and the EC50 values of these ligands in a FLIPR functional poten
247 analysis, and in transactivation assays, the EC50 for TCDD was 23 nM, similar to X. laevis AHR1beta (
249 odel to examine the relationship between the EC50 for activation of the GABA type A (GABAA) receptor
250 cant variation was also observed between the EC50 values for the two assays, with robust levels of re
251 ld, whereas the R655C mutation decreased the EC50 5-fold, increased the Vmax 2.1-fold, and decreased
254 also resulted in predictable changes in the EC50 Finally, we altered the number of GABA-binding site
256 utophosphorylation) by 6-fold and lowers the EC50 for Ca(2+)/CaM binding to activated eEF-2K (Thr-348
258 vity will result in identical effects on the EC50 We examined receptor activation by GABA while chang
259 CR4 agonists (CXCL12, ubiquitin) reduced the EC50 of the phenylephrine-induced blood pressure respons
260 all differently coated AgNP suspensions, the EC50 values calculated as a function of Agbioav were com
261 This Kd is 50-100 times greater than the EC50 for Galphaq-mediated PLC-beta3 activation and for t
262 least an order of magnitude better than the EC50 values obtained for the clinically approved photose
263 equires its C2C and C2E domains and that the EC50 of such binding is in the low micromolar Ca(2+) ran
266 species to waterborne nickel (Ni), with the EC50 for the development of fully formed pluteus larvae
268 versus 4.3 +/- 1.1 mum) and glycoprotein VI (EC50, 1.61 +/- 0.85 versus 0.26 +/- 0.21 mug/ml) but not
269 than PLTX in reducing HaCaT cells viability (EC50 = 1.1 x 10(-9) M vs 1.8 x 10(-11) M, MTT test) in a
272 f cancer cells carrying mutant BRCA1/2, with EC50 = 0.3 nM (MX-1) and 5 nM (Capan-1), respectively.
273 d CFTR activation potency compared to 4 with EC50 down to 21 nM and with greater metabolic stability.
274 sive stepping distance decreases 40-60% with EC50 values <100 nM propofol without an effect on veloci
275 ngeners that elicited alpha7 activation with EC50 values of 70 nM and Kd values for AChBP in a simila
276 hocyanidin A1 proved to be more active, with EC50 value for DPPH radical scavenging of 18.25 mug/mL a
277 with interesting antioxidant activities with EC50 values of up to 0.08 mg/L or values of TEAC of 0.67
280 gregate size and specific surface area, with EC50 values for reproduction ranging from 4 to 29 mg Fe
281 srupted preformed A. fumigatus biofilms with EC50 values similar to those obtained for Sph3h In contr
283 several leukemia and solid tumor cells with EC50 values as low as 280 nM, while they had negligible
284 ne CFTRact-K089 (1) that activated CFTR with EC50 approximately 250 nM, which when delivered topicall
285 lly activated CFTR chloride conductance with EC50 approximately 30 nM, without causing cAMP or calciu
288 , fully activated CFTR in cell cultures with EC50 approximately 250 nM and produced an approximately
289 otencies are enhanced compared with DCS with EC50 values in the low nanomolar range (1.7 nM at GluN1/
290 ant bactericidal activity was evidenced with EC50 values of 16.8+/-1.2muM for MTP1 and 109+/-7.0muM f
292 phenylalanine (L-Phe) activated GPR139, with EC50 values in the 30- to 300-muM range, consistent with
293 exhibited exceptional potency profiles with EC50 values </=5 nM against major drug resistant HCV var
296 nes on F. candida in soil were similar, with EC50 values ranging from 2119 to 2559 mumol kg(-1) dry w
297 es (Pcs) and tetrapyrazinoporphyrazines with EC50 values as low as 5 nM (MCF-7 cells) for the best co
299 monotonic and inverted U-shaped pattern with EC50s that were approximately 10(5)-fold lower than thos
300 pinavir was observed across 20 viruses, with EC50s ranging 0.71-6.95 nM for atazanvir and 0.64-8.54 n
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