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1 IC50 values for (S)-orteronel were identical for blockin
2 IC50 values of the hydrolysates were between 27 and 39mg
5 32 nM; 3b, IC50 approximately 9 nM; and 14, IC50 approximately 35 nM) inhibit ATX-dependent invasion
7 , risedronate (IC50 > 100 muM) or GGTI-2133 (IC50 > 25 muM) inhibited the growth of ovarian cancer ce
8 xypyridin-3-yl)methyl)-3-phenylisoxazole 25 (IC50 = 2 nM, 14-fold selectivity over CYP11B2), exhibiti
9 he results demonstrated that T. daenensis-3 (IC50=273.36), T. vulgaris (IC50=289.3), and T. fedtschen
10 ulgaris (IC50=289.3), and T. fedtschenkoi-3 (IC50=339.22) possessed higher antioxidant activities tha
11 5-methyl-3-phenylisoxazole-4-carboxamide (3, IC50 = 3 muM), exhibited no activity on the protein kina
12 f 8TQ yielded a small molecule compound (35, IC50 value approximately 400 nM) that is a potent and se
15 analogues (3a, IC50 approximately 32 nM; 3b, IC50 approximately 9 nM; and 14, IC50 approximately 35 n
16 Two of the most potent compounds, 3b and 3f (IC50 approximately 84 nM), lack inhibitory action on ENP
17 ound 21b, a potent inhibitor of Clk1 and -4 (IC50 = 7 and 2.3 nM, respectively), exhibiting an unprec
19 on needed to suppress palmitate flux by 50% (IC50(palmitate)f).In the omega-3 group, the EPA and DHA
22 beteus nigricolor, potently inhibits NaV1.7 (IC50 0.9 nM) with at least 40-1000-fold selectivity over
23 pyridin-3-yl)methyl)-2-phenylpyridine Ref 7 (IC50= 2 nM) exhibited promutagenic potential as well as
24 s (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value approximately 2.5 muM) displayed strong inhib
25 ivity on L-type calcium channels, i.e. A7r5 (IC50 = 0.18 +/- 0.02 and 0.25 +/- 0.63 mug/ml, respectiv
29 statin (IC50 = 0.6-14 muM), zoledronic acid (IC50 = 21-57 muM), risedronate (IC50 > 100 muM) or GGTI-
31 sing compounds such as DRI-C21045, activity (IC50) in the low micromolar range has been confirmed in
32 24 displayed excellent inhibitory activity (IC50 of 0.82 +/- 0.18 muM and 1.3 +/- 0.22 muM, respecti
33 anced alpha-glucosidase inhibitory activity (IC50=6.15mug/mL), with castalagin (7) as the main consti
35 is supported by its agr-quenching activity (IC50 2-32 mug mL(-1)) in transcriptional reporters, dire
39 publicly disclosed, submicromolar-affinity (IC50 = 0.2 muM), small-molecule inhibitor of the inward
40 sensitive to PhTX-12 along with alpha3beta4 (IC50 values of 100 nM) with alpha4beta4, alpha4beta2, al
41 ty to low concentrations of 4-aminopyridine (IC50 <100 mum) and block by the peptide inhibitor blood
42 d inhibitory activity against alpha-amylase, IC50 0.74+/-0.02mg/ml and 0.81+/-0.03mg/ml, respectively
43 n the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth
45 ne-2-sulfonate (PSB-16133, 61) exhibited an IC50 value of 233 nM, selectivity versus other P2Y recep
49 ),1-Nal(4),Thr(8)]ghrelin(1-8), possessed an IC50 value of 0.11 nM that is a 28-fold improvement comp
52 % of the small molecules prepared showed an IC50 value of less than 100 mum, and approximately 25 %
55 inhibitors of alpha-amylase activity with an IC50 of (0.075+/-0.010-0.103+/-0.017) mg/ml, also a mixe
56 ibition of cell recruitment in vitro with an IC50 of 0.5 nm but demonstrated little efficacy in vario
57 eric modulator of GABArho1 receptors with an IC50 of 1.6 microM, an enhancer of alpha7 nicotinic rece
59 nt at inhibiting chemotaxis in vitro with an IC50 of 21 nm Furthermore, we observed that 1B6 displaye
60 and selective GRK2 inhibitor, 14as, with an IC50 of 30 nM against GRK2 and greater than 230-fold sel
63 740 was also five times more potent, with an IC50 of 5 muM, in a fibroblast-mediated collagen contrac
64 sses expression of gamma2 late genes with an IC50 of 5 mum, which is at least 10 times lower than the
65 ich is a very potent, dual inhibitor with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1 BD2, and 106 n
69 the highest ACE inhibitory activity, with an IC50 value of 0.54mg/ml, while the SP hydrolysate exhibi
70 Compound 18 (MM-589) binds to WDR5 with an IC50 value of 0.90 nM (Ki value <1 nM) and inhibits the
71 selective irreversible inhibitor 45a with an IC50 value of 1 nM against the EGFR L858R/T790M double m
74 ted DPPH radical scavenging activity with an IC50 value of 20.02+/-0.14muM which was better than asco
77 nhibition of cell proliferation, yielding an IC50 value of 356 +/- 21 nM in neuroblastoma SHSY5Y cell
80 strate and inhibitor enzyme kinetics (Km and IC50), (2) its amino acid sequence and (3) its ability t
86 he sensitivity of the biosensor, measured as IC50 value, was 1.51U/mL and 0.32U/mL, for anti-TRIM21 a
89 M1 enzymatic activity in biochemical assays (IC50 = 6 nM) with broad selectivity against other histon
90 discovered that d-ShK has a near-background IC50 value approximately 50,000 times lower than that of
96 ry safety and high therapeutic indices (CC50/IC50 > 180), and thus representing potential promising l
98 73) that exhibited high potency toward CDK2 (IC50 0.044 muM) but was approximately 2000-fold less act
99 n selective cytotoxicity against V-C8 cells (IC50 17 microg/ml) compared to V79 cells (IC50 26 microg
100 sistant A2780Cis human ovarian cancer cells (IC50 74 muM, blue light) with a photocytotoxic index <2,
101 in reduced peak SCN5A currents in HEK cells (IC50=110+/-3 mumol/L) and Na(+) current in mouse ventric
102 ntrolled gene transcription in living cells (IC50 = 230 nM), providing the most potent inhibitor of t
105 y, led to compound 9b, exhibiting a cellular IC50 for NF-kappaB inhibition of 0.3 muM while retaining
106 kyrase 1 and 2 with biochemical and cellular IC50 values of 29 nM, 6.3 nM and 19 nM, respectively, an
107 HCl] (8) selectively blocked Kv1.1 channels (IC50 approximately 15 muM) recombinantly expressed in ma
108 SY5Y (i.e. both L-type and T-type channels) (IC50 = 8 +/- 0.23 and 10 +/- 0.18 mug/ml, respectively)
109 = 10.6 +/- 1.3 to 1.6 +/- 0.3 muM) and CME (IC50(CME) = 65.9 +/- 7.7 to 3.7 +/- 1.1 mM), which makes
110 ce) showed improved inhibition for collagen (IC50 = 6.7 muM), CRP-XL (IC50 = 53.5 muM), and convulxin
111 han any of its enantiomers S (6c) (collagen, IC50 = 25.3 muM; CRP-XL, IC50 = 181.4 muM; CVX, IC50 = 9
112 uM; CVX, IC50 = 9 muM) and R (6d) (collagen, IC50 = 126.3 muM; CRP-XL, IC50 > 500 muM; CVX, IC50 = 86
113 ion as compared to losartan (LOS) (collagen, IC50 = 10.4 muM; CRP-XL, IC50 = 158 muM; CVX, IC50 = 11
115 PP-IV half maximal inhibitory concentration (IC50) of H4, a potent sample, was maintained following s
116 hibited 50% growth inhibitory concentration (IC50) values that were less than 20 muM in HeLa cells, i
117 mivir half-maximal inhibitory concentration (IC50), and E119D conferred the highest zanamivir IC50.
118 tion [half maximal inhibitory concentration (IC50): 3.8muM] and ATP synthesis (IC50: 0.9muM), and add
120 ing potential (50% inhibitory concentration, IC50 approximately 0.59mg/mL) than commercially availabl
121 P-IV half maximal inhibitory concentrations (IC50) of 87.0+/-3.2 and 93.3+/-8.0microM, respectively.
122 001) half-maximal inhibitory concentrations (IC50) than did donor isolates, and their odds of replica
125 o piperaquine 50% inhibitory concentrations (IC50s), and tested whether these genetic variants are ma
126 P-XL (IC50 = 53.5 muM), and convulxin (CVX) (IC50 = 5.7 muM) mediated platelet aggregation as compare
127 C50 = 10.4 muM; CRP-XL, IC50 = 158 muM; CVX, IC50 = 11 muM) than any of its enantiomers S (6c) (colla
129 0 = 25.3 muM; CRP-XL, IC50 = 181.4 muM; CVX, IC50 = 9 muM) and R (6d) (collagen, IC50 = 126.3 muM; CR
130 thermore, compound 25 inhibited rat CYP11B1 (IC50 = 2 muM) and showed a high oral bioavailability (F
133 h significantly associated with daunorubicin IC50 values in a panel of lymphoblastoid cell lines.
134 , IL-8, and MIP-1beta) by monocytes and DCs (IC50 < 1 muM) and prevented DC maturation upon TLR4 acti
136 For assay validation, we finally determined IC50 values for three unlabeled peptides, that is: (i) l
137 , outperforming the standard drug donepezil (IC50 = 11 nM), most of the corresponding 1,4-dihydropyri
138 as least sensitive because they showed drug IC50 value greater than the cell panel median and lacked
139 he "standard" inhibitor 1 (XAV939)(5), i.e., IC50 = 100 pM vs TNKS2 and IC50 = 6.5 muM vs PARP1 for 1
141 V from black soybean was the most effective (IC50: 0.25mg/mL) against alpha-amylase; Fraction V from
143 , this compound was still not potent enough (IC50 approximately 53 nM) to enter preclinical studies.
144 d dehydrogenase type 1 (11beta-HSD1) enzyme (IC50 3.0 nM) with >10000-fold selectivity over human 11b
145 ion from T4, respectively, with an estimated IC50 of 160 nM; no statistically significant inhibition
149 be highly potent dual binding site hAChEIs (IC50 up to 3 nM), outperforming the standard drug donepe
151 roacetamide at the thiophene 2-position, had IC50 of approximately 30 nM, approximately 3.6-fold more
153 phoramidate prodrugs of these compounds have IC50 values in the low micromolar range in Pf lines and
156 representing IKr (CHO cells expressing hERG; IC50=219+/-21 mumol/L) and IKs (CHO cells expressing KCN
157 he growth of HCC cells, although at a higher IC50 as compared with breast cancer cells, likely due to
158 ve submicromolar inhibitor of BuChE (huBuChE IC50 = 0.443 muM) with high permeability in the PAMPA-BB
159 IDPR inhibit CD38-mediated cADPR hydrolysis (IC50 7 muM and 21 microM respectively) with 8-Br-L-cIDPR
160 icromolar inhibition against both dynamin I (IC50 = 10.6 +/- 1.3 to 1.6 +/- 0.3 muM) and CME (IC50(CM
162 pounds displayed a similar decrease (30%) in IC50 for inhibition of [(3)H]DA uptake by cocaine in WT
163 rug-material combination, and an increase in IC50 of approximately 4.3x was observed in PDMS devices
164 ToF-SIMS data showed the bias observed in IC50 values found in PDMS devices was directly related t
169 e IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM) and favorable pharmacokinetic and toxicol
173 ) and IKs (CHO cells expressing KCNQ1+KCNE1; IC50=184+/-12 mumol/L), whereas azithromycin suppressed
174 alpha-amylase, alpha-glucosidase and lipase (IC50: 0.38mg/mL, 0.87mug/mL and 15mug/mL, respectively).
176 ibitors in that they demonstrated the lowest IC50 values (2 muM) ever observed among all indole-based
177 inhibition zone diameter, the half maximal (IC50) and the minimal (MIC) inhibitory concentrations.
178 falciparum laboratory-adapted strains (mean IC50 32 nM), Ugandan field isolates (mean ex vivo IC50 6
180 Axl receptor activation with low micromolar IC50s in cell-based reporter assays, inhibit Gas6-induci
182 fractions of CO7 cultivar of foxtail millet (IC50, 22.37 and 57.26microg/ml) and CO4 cultivar of litt
183 icrog/ml) and CO4 cultivar of little millet (IC50, 18.97 and 55.69microg/ml) displayed strong inhibit
184 ys acceptable antituberculosis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patie
185 a(++) currents (rabbit ventricular myocytes, IC50=66.5+/-4 mumol/L) and IK1 (HEK cells expressing Kir
186 46, 49, and 50 showed single-digit nanomolar IC50 values for in vitro inhibition of KDM1A, with high
188 most interesting compound 9 showed nanomolar IC50 values for both proteins, membrane permeability, an
190 igh in vitro activity against C. neoformans (IC50 = 0.35 mug/mL, MIC = MFC = 0.63 mug/mL) with a sele
192 f nitrate with strong pi affinity nullified (IC50 = 2.2 mM) the responsiveness of anion-pi catalysts
194 s ranged from 52.5 to 67.2mug/mL in terms of IC50 values following fermentation, while the alpha-gluc
195 Compounds 11 and 12 showed the values of IC50 at 11.9 and 17.2 muM against neglected Chagas' dise
196 606120 is a selective antagonist for P2X7Rs (IC50 of 10 nM) and ineffective at the P2X1R (at 10 muM)
202 rate model to predict resistance phenotypes (IC50) quantitatively from a unique combination of the in
203 els exhibited more potent photocytotoxicity (IC50 3 muM, blue light) with a photocytotoxic index >5.
204 C50 > 200 muM) and showed low phototoxicity (IC50 > 100 muM, 1.5 J/cm(2)) toward human HEp2 cells.
208 nd imazalil (enilconazole)-showed potencies (IC50) in the range between 175 and 1,500 nM, similar to
211 from black turtle bean was the most potent (IC50: 0.25mug/mL) against alpha-glucosidase; Fraction IV
212 5-lipoxygenase (5-LOX) inhibition potential (IC50 0.76-0.92mg/mL) of the polyketides in consonant wit
215 itor of anthrax lethal factor (LF) protease (IC50 = 390 +/- 20 nM, Ki = 365 +/- 20 nM) and a weak inh
216 agement was demonstrated, with LRRK2-pSer935 IC50 values for 22 in mouse brain and kidney being 1.3 a
217 inhibits the JNK3 in the subnanomolar range (IC50 = 0.3 nM), shows high metabolic stability in human
218 e 22.4-40.6muM) and myeloperoxidase release (IC50 in the range 22.2-32.2muM) from stimulated human ne
219 s as potent blockers of TGF-beta1 responses (IC50 50 nM), Snail1 expression, and collagen deposition
220 ther characterization of ciproxifan revealed IC50 values in a micromolar concentration range for huma
221 dronic acid (IC50 = 21-57 muM), risedronate (IC50 > 100 muM) or GGTI-2133 (IC50 > 25 muM) inhibited t
222 ith excellent recovery and high sensitivity, IC50 = 0.28 mug/L, with a limit of detection that is wel
227 ound displays nanomolar in vitro and in situ IC50 values and fully inhibits ABHD3 activity in human c
228 Exposure of HeLa cells to Cu(PyBD).SO4 (IC50 = 10 muM) results in a G2/M arrest compared with un
230 lized), BeauIII selectively inhibited SOAT1 (IC50; 5.0 microM (SOAT1) vs >90 microM (SOAT2)), while i
231 t the production of reactive oxygen species (IC50 in the range 22.4-40.6muM) and myeloperoxidase rele
232 ch inhibited the enzyme with a submicromolar IC50 (0.162 muM), capable of inhibiting the target in ce
233 entration (IC50): 3.8muM] and ATP synthesis (IC50: 0.9muM), and additional findings supported inhibit
241 more potent than its congener GL331 and the IC50 values are from 0.34 +/- 0.21 to 3.54 +/- 0.54 micr
242 ure for envisioned clinical application, the IC50 of MEAN was not significantly changed in several dr
243 lowing knockdown of MARCKS in RCC cells, the IC50 of the multikinase inhibitor regorafenib was reduce
245 Under hypoxic conditions, a decrease in the IC50 of MTX and MTX-loaded MSNR was observed when compar
246 up, there were no significant changes in the IC50(palmitate)f (19 +/- 2 compared with 24 +/- 3 muIU/m
247 g so, we reveal how classic metrics like the IC50 and minimal inhibitory concentration (MIC) are dubi
249 s reduced cell proliferation and reduced the IC50 inhibitory concentration of chemotherapeutic drugs
250 leukemic cytokine secretion and reduced the IC50 of chemotherapeutic drug treatments in AML cells.
251 m, which is at least 10 times lower than the IC50 value required for inhibition of expression of earl
252 of PARP inhibitor >1000-fold higher than the IC50 were required to ablate both ADP-ribosylation and X
258 t potent compound, has an excellent in vitro IC50 (0.056 nM) and improved aqueous solubility as well
260 t disrupt the EthR-DNA interaction in vitro (IC50 =460-610 mum) and bind to the hydrophobic channel o
261 32 nM), Ugandan field isolates (mean ex vivo IC50 64 nM), and murine P. berghei and P. falciparum inf
262 t T. daenensis-3 (IC50=273.36), T. vulgaris (IC50=289.3), and T. fedtschenkoi-3 (IC50=339.22) possess
263 losis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM
264 tumors, is a bona fide PORCN inhibitor whose IC50 for inhibition of Wnt fatty acylation in vitro clos
265 ibits JAK1 and HDACs 1, 2, 3, 6, and 10 with IC50 values of less than 20 nM, is <100 nM potent agains
267 owed the best ACE-inhibitory activities with IC50 values of 53.31 and 75.05microg/ml, respectively.
268 tency (inhibiting PARP1 enzyme activity with IC50 = 0.079 muM), as well as inhibiting PARP-modulated
272 e and alpha-amylase inhibitory activity with IC50=1.1+/-0.1mug/ml and IC50=19.3+/-1.1mug/ml, respecti
273 he greatest antiproliferative activity, with IC50 values of 0.35-4.6 nM (4g) and 0.5-20.2 nM (4i), wh
274 erial and human salivary alpha-amylases with IC50 values of 0.11 and 0.04mumol, respectively, whereas
276 activity against MCF-7 and HL-60 cells with IC50 of 6.13 +/- 0.64 and 4.43 +/- 0.35, respectively.
277 liferative effects against cancer cells with IC50 range of 4.43 +/- 0.35 to 49.63 +/- 3.59 microM, bu
279 histamine release were dose dependent, with IC50 values ranging between 0.001 and 0.5 mumol/L, and t
280 potent compound is the 4-F derivative, with IC50 in the 10(-8) M range and selectivities around 1000
281 activity against Plasmodium falciparum with IC50 values of 1.84, 8.36, and 6.95 muM, respectively.
283 well as significant inhibition of HDAC6 with IC50 values in the submicromolar concentration range.
292 had 50- to 1000-fold lower sensitivity, with IC50 values of 2402 +/- 334 nM and 344 +/- 64 nM, respec
296 ition for collagen (IC50 = 6.7 muM), CRP-XL (IC50 = 53.5 muM), and convulxin (CVX) (IC50 = 5.7 muM) m
298 an (LOS) (collagen, IC50 = 10.4 muM; CRP-XL, IC50 = 158 muM; CVX, IC50 = 11 muM) than any of its enan
299 s S (6c) (collagen, IC50 = 25.3 muM; CRP-XL, IC50 = 181.4 muM; CVX, IC50 = 9 muM) and R (6d) (collage
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