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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
3 IC50 values were 0.22 +/- 0.09 nM for Y537S-ER (P = 0.97
6 32 nM; 3b, IC50 approximately 9 nM; and 14, IC50 approximately 35 nM) inhibit ATX-dependent invasion
8 , risedronate (IC50 > 100 muM) or GGTI-2133 (IC50 > 25 muM) inhibited the growth of ovarian cancer ce
10 xypyridin-3-yl)methyl)-3-phenylisoxazole 25 (IC50 = 2 nM, 14-fold selectivity over CYP11B2), exhibiti
11 he results demonstrated that T. daenensis-3 (IC50=273.36), T. vulgaris (IC50=289.3), and T. fedtschen
12 ulgaris (IC50=289.3), and T. fedtschenkoi-3 (IC50=339.22) possessed higher antioxidant activities tha
13 5-methyl-3-phenylisoxazole-4-carboxamide (3, IC50 = 3 muM), exhibited no activity on the protein kina
14 f 8TQ yielded a small molecule compound (35, IC50 value approximately 400 nM) that is a potent and se
17 analogues (3a, IC50 approximately 32 nM; 3b, IC50 approximately 9 nM; and 14, IC50 approximately 35 n
18 Two of the most potent compounds, 3b and 3f (IC50 approximately 84 nM), lack inhibitory action on ENP
19 ound 21b, a potent inhibitor of Clk1 and -4 (IC50 = 7 and 2.3 nM, respectively), exhibiting an unprec
20 on needed to suppress palmitate flux by 50% (IC50(palmitate)f).In the omega-3 group, the EPA and DHA
23 beteus nigricolor, potently inhibits NaV1.7 (IC50 0.9 nM) with at least 40-1000-fold selectivity over
24 pyridin-3-yl)methyl)-2-phenylpyridine Ref 7 (IC50= 2 nM) exhibited promutagenic potential as well as
25 s (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value approximately 2.5 muM) displayed strong inhib
26 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
38 publicly disclosed, submicromolar-affinity (IC50 = 0.2 muM), small-molecule inhibitor of the inward
39 ty to low concentrations of 4-aminopyridine (IC50 <100 mum) and block by the peptide inhibitor blood
40 d inhibitory activity against alpha-amylase, IC50 0.74+/-0.02mg/ml and 0.81+/-0.03mg/ml, respectively
41 n the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth
42 ne-2-sulfonate (PSB-16133, 61) exhibited an IC50 value of 233 nM, selectivity versus other P2Y recep
46 ),1-Nal(4),Thr(8)]ghrelin(1-8), possessed an IC50 value of 0.11 nM that is a 28-fold improvement comp
49 % of the small molecules prepared showed an IC50 value of less than 100 mum, and approximately 25 %
52 inhibitors of alpha-amylase activity with an IC50 of (0.075+/-0.010-0.103+/-0.017) mg/ml, also a mixe
54 ibition of cell recruitment in vitro with an IC50 of 0.5 nm but demonstrated little efficacy in vario
56 nt at inhibiting chemotaxis in vitro with an IC50 of 21 nm Furthermore, we observed that 1B6 displaye
57 and selective GRK2 inhibitor, 14as, with an IC50 of 30 nM against GRK2 and greater than 230-fold sel
59 740 was also five times more potent, with an IC50 of 5 muM, in a fibroblast-mediated collagen contrac
60 ich is a very potent, dual inhibitor with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1 BD2, and 106 n
61 Q-1 reduced tumor cell proliferation with an IC50 of ~1.0 muM and decreased tumor growth rate in mous
65 the highest ACE inhibitory activity, with an IC50 value of 0.54mg/ml, while the SP hydrolysate exhibi
66 Compound 18 (MM-589) binds to WDR5 with an IC50 value of 0.90 nM (Ki value <1 nM) and inhibits the
67 selective irreversible inhibitor 45a with an IC50 value of 1 nM against the EGFR L858R/T790M double m
69 ted DPPH radical scavenging activity with an IC50 value of 20.02+/-0.14muM which was better than asco
72 nhibition of cell proliferation, yielding an IC50 value of 356 +/- 21 nM in neuroblastoma SHSY5Y cell
75 strate and inhibitor enzyme kinetics (Km and IC50), (2) its amino acid sequence and (3) its ability t
82 he sensitivity of the biosensor, measured as IC50 value, was 1.51U/mL and 0.32U/mL, for anti-TRIM21 a
87 s the strongest cytotoxic activity on BT474 (IC50 = 55.5 nM, BRCA2 and TP53 co-mutant) compared to MC
90 that no direct method exists for calculating IC50 values, we resort to a combination of atomistic mod
91 ry safety and high therapeutic indices (CC50/IC50 > 180), and thus representing potential promising l
93 73) that exhibited high potency toward CDK2 (IC50 0.044 muM) but was approximately 2000-fold less act
94 n selective cytotoxicity against V-C8 cells (IC50 17 microg/ml) compared to V79 cells (IC50 26 microg
95 sistant A2780Cis human ovarian cancer cells (IC50 74 muM, blue light) with a photocytotoxic index <2,
96 wer concentration than to lung cancer cells (IC50 = 59.1 mug/mL), and L-PTX demonstrated a comparable
97 ntrolled gene transcription in living cells (IC50 = 230 nM), providing the most potent inhibitor of t
100 y, led to compound 9b, exhibiting a cellular IC50 for NF-kappaB inhibition of 0.3 muM while retaining
101 kyrase 1 and 2 with biochemical and cellular IC50 values of 29 nM, 6.3 nM and 19 nM, respectively, an
102 HCl] (8) selectively blocked Kv1.1 channels (IC50 approximately 15 muM) recombinantly expressed in ma
103 SY5Y (i.e. both L-type and T-type channels) (IC50 = 8 +/- 0.23 and 10 +/- 0.18 mug/ml, respectively)
104 = 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
105 ce) showed improved inhibition for collagen (IC50 = 6.7 muM), CRP-XL (IC50 = 53.5 muM), and convulxin
106 han any of its enantiomers S (6c) (collagen, IC50 = 25.3 muM; CRP-XL, IC50 = 181.4 muM; CVX, IC50 = 9
107 uM; CVX, IC50 = 9 muM) and R (6d) (collagen, IC50 = 126.3 muM; CRP-XL, IC50 > 500 muM; CVX, IC50 = 86
108 ion as compared to losartan (LOS) (collagen, IC50 = 10.4 muM; CRP-XL, IC50 = 158 muM; CVX, IC50 = 11
111 PP-IV half maximal inhibitory concentration (IC50) of H4, a potent sample, was maintained following s
113 hibited 50% growth inhibitory concentration (IC50) values that were less than 20 muM in HeLa cells, i
115 mivir half-maximal inhibitory concentration (IC50), and E119D conferred the highest zanamivir IC50.
116 tion [half maximal inhibitory concentration (IC50): 3.8muM] and ATP synthesis (IC50: 0.9muM), and add
118 arum (half maximal inhibitory concentration [IC50] = 1-2 uM), suggesting that BCH070 acts via a novel
119 ing potential (50% inhibitory concentration, IC50 approximately 0.59mg/mL) than commercially availabl
120 P-IV half maximal inhibitory concentrations (IC50) of 87.0+/-3.2 and 93.3+/-8.0microM, respectively.
121 001) half-maximal inhibitory concentrations (IC50) than did donor isolates, and their odds of replica
126 o piperaquine 50% inhibitory concentrations (IC50s), and tested whether these genetic variants are ma
127 P-XL (IC50 = 53.5 muM), and convulxin (CVX) (IC50 = 5.7 muM) mediated platelet aggregation as compare
128 C50 = 10.4 muM; CRP-XL, IC50 = 158 muM; CVX, IC50 = 11 muM) than any of its enantiomers S (6c) (colla
130 0 = 25.3 muM; CRP-XL, IC50 = 181.4 muM; CVX, IC50 = 9 muM) and R (6d) (collagen, IC50 = 126.3 muM; CR
131 thermore, compound 25 inhibited rat CYP11B1 (IC50 = 2 muM) and showed a high oral bioavailability (F
134 , IL-8, and MIP-1beta) by monocytes and DCs (IC50 < 1 muM) and prevented DC maturation upon TLR4 acti
137 as least sensitive because they showed drug IC50 value greater than the cell panel median and lacked
138 he "standard" inhibitor 1 (XAV939)(5), i.e., IC50 = 100 pM vs TNKS2 and IC50 = 6.5 muM vs PARP1 for 1
140 V from black soybean was the most effective (IC50: 0.25mg/mL) against alpha-amylase; Fraction V from
141 The study analyzed the inhibitory effects (IC50) of crude and purified extracts from Maliniak, Ceri
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
151 roacetamide at the thiophene 2-position, had IC50 of approximately 30 nM, approximately 3.6-fold more
152 phoramidate prodrugs of these compounds have IC50 values in the low micromolar range in Pf lines and
155 representing IKr (CHO cells expressing hERG; IC50=219+/-21 mumol/L) and IKs (CHO cells expressing KCN
156 he growth of HCC cells, although at a higher IC50 as compared with breast cancer cells, likely due to
157 IDPR inhibit CD38-mediated cADPR hydrolysis (IC50 7 muM and 21 microM respectively) with 8-Br-L-cIDPR
158 icromolar inhibition against both dynamin I (IC50 = 10.6 +/- 1.3 to 1.6 +/- 0.3 muM) and CME (IC50(CM
160 pounds displayed a similar decrease (30%) in IC50 for inhibition of [(3)H]DA uptake by cocaine in WT
161 ional options in achieving relative error in IC50 within 5-fold for test cases and 20-fold for protei
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
174 ) and IKs (CHO cells expressing KCNQ1+KCNE1; IC50=184+/-12 mumol/L), whereas azithromycin suppressed
176 alpha-amylase, alpha-glucosidase and lipase (IC50: 0.38mg/mL, 0.87mug/mL and 15mug/mL, respectively).
179 ibitors in that they demonstrated the lowest IC50 values (2 muM) ever observed among all indole-based
180 inhibition zone diameter, the half maximal (IC50) and the minimal (MIC) inhibitory concentrations.
181 BRCA2 and TP53 co-mutant) compared to MCF7 (IC50 = 7.7 muM, both BRCA2 and TP53 wild type) and MDA-M
182 a 42-pseudovirus panel with a geometric mean IC50 of 0.055 ug/mLl and SHIVAD8 with an IC50 of 0.028 u
183 falciparum laboratory-adapted strains (mean IC50 32 nM), Ugandan field isolates (mean ex vivo IC50 6
185 Axl receptor activation with low micromolar IC50s in cell-based reporter assays, inhibit Gas6-induci
186 fractions of CO7 cultivar of foxtail millet (IC50, 22.37 and 57.26microg/ml) and CO4 cultivar of litt
187 icrog/ml) and CO4 cultivar of little millet (IC50, 18.97 and 55.69microg/ml) displayed strong inhibit
188 ys acceptable antituberculosis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patie
189 a(++) currents (rabbit ventricular myocytes, IC50=66.5+/-4 mumol/L) and IK1 (HEK cells expressing Kir
190 46, 49, and 50 showed single-digit nanomolar IC50 values for in vitro inhibition of KDM1A, with high
192 most interesting compound 9 showed nanomolar IC50 values for both proteins, membrane permeability, an
193 igh in vitro activity against C. neoformans (IC50 = 0.35 mug/mL, MIC = MFC = 0.63 mug/mL) with a sele
195 f nitrate with strong pi affinity nullified (IC50 = 2.2 mM) the responsiveness of anion-pi catalysts
197 Compounds 11 and 12 showed the values of IC50 at 11.9 and 17.2 muM against neglected Chagas' dise
198 itaxel was toxic to cell of neuronal origin (IC50 = 18.4 mug/mL) at a lower concentration than to lun
199 606120 is a selective antagonist for P2X7Rs (IC50 of 10 nM) and ineffective at the P2X1R (at 10 muM).
205 els exhibited more potent photocytotoxicity (IC50 3 muM, blue light) with a photocytotoxic index >5.
206 C50 > 200 muM) and showed low phototoxicity (IC50 > 100 muM, 1.5 J/cm(2)) toward human HEp2 cells.
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 aused by large fractions of VRC01-resistant (IC50>50 mug/mL) circulating strains or rather a global r
220 s as potent blockers of TGF-beta1 responses (IC50 50 nM), Snail1 expression, and collagen deposition
221 ther characterization of ciproxifan revealed IC50 values in a micromolar concentration range for huma
222 dronic acid (IC50 = 21-57 muM), risedronate (IC50 > 100 muM) or GGTI-2133 (IC50 > 25 muM) inhibited t
223 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
238 more potent than its congener GL331 and the IC50 values are from 0.34 +/- 0.21 to 3.54 +/- 0.54 micr
239 ure for envisioned clinical application, the IC50 of MEAN was not significantly changed in several dr
240 lowing knockdown of MARCKS in RCC cells, the IC50 of the multikinase inhibitor regorafenib was reduce
242 stable EVG concentrations that exceeded the IC50 for wild-type HIV, suggesting that EVG achieves the
244 Under hypoxic conditions, a decrease in the IC50 of MTX and MTX-loaded MSNR was observed when compar
245 up, there were no significant changes in the IC50(palmitate)f (19 +/- 2 compared with 24 +/- 3 muIU/m
246 Neural Network) to predict the value of the IC50 (by regression), or if the antibody binds or not to
248 s reduced cell proliferation and reduced the IC50 inhibitory concentration of chemotherapeutic drugs
249 leukemic cytokine secretion and reduced the IC50 of chemotherapeutic drug treatments in AML cells.
250 of PARP inhibitor >1000-fold higher than the IC50 were required to ablate both ADP-ribosylation and X
251 ichotomous resistance outcome of whether the IC50 neutralization titer of VRC01 for a given Env pseud
257 t potent compound, has an excellent in vitro IC50 (0.056 nM) and improved aqueous solubility as well
260 ound to be extremely potent with an in vitro IC50 ~ 100x lower than folate SMDCs constructed with var
261 t disrupt the EthR-DNA interaction in vitro (IC50 =460-610 mum) and bind to the hydrophobic channel o
262 32 nM), Ugandan field isolates (mean ex vivo IC50 64 nM), and murine P. berghei and P. falciparum inf
263 t T. daenensis-3 (IC50=273.36), T. vulgaris (IC50=289.3), and T. fedtschenkoi-3 (IC50=339.22) possess
264 losis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM
265 tumors, is a bona fide PORCN inhibitor whose IC50 for inhibition of Wnt fatty acylation in vitro clos
266 ibits JAK1 and HDACs 1, 2, 3, 6, and 10 with IC50 values of less than 20 nM, is <100 nM potent agains
268 owed the best ACE-inhibitory activities with IC50 values of 53.31 and 75.05microg/ml, respectively.
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 RSM-932A and MN58b that were discovered with IC50 of 0.5 and 150 muM, respectively, and were shown to
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.
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