ライフサイエンスコーパス: potency

1 a treated) and intensity (application rate x potency).

2 body against a broad range of H3N2 with high potency.

3 that endow AFGPs with their exceptional IRI potency.

4 induced IL-6 and IL-8 levels with comparable potency.

5 properties, such as lipophilicity, and also potency.

6 ns showed loss of neutralisation breadth and potency.

7 l studies are generally associated with weak potency.

8 that vadadustat inhibits AspH with moderate potency.

9 oding molecule that positively controls 2CLC potency.

10 ement of target affinity as well as cellular potency.

11 up significantly attenuated K18 antagonistic potency.

12 feature that results in a leap in anticancer potency.

13 the DFG loop and significantly improved cell potency.

14 sight into MAIT cell antigen specificity and potency.

15 better understand its potential toxicity and potency.

16 tinct mechanism of action and in a different potency.

17 ermine unbound drug exposure as well as drug potency.

18 iruses, which overestimate bNAb coverage and potency.

19 sed clonal lineage-specific ADCC breadth and potency.

20 ificantly improved peptidomimetic inhibitory potency.

21 ing in a significant decrease in IgE-binding potency.

22 omaterials that can be engineered to enhance potency.

23 arbonate (2APT-D6) was selected for its high potency.

24 off-target side effects and increasing drug potency.

25 nalogs with improved solubility and enhanced potency.

26 s that controls MERVL for expanded stem cell potency.

27 with activation of 2C genes and an expanded potency.

28 ility; heating and/or freezing impairs their potency.

29 roperties and maintained enzyme and cellular potency.

30 o assays to measure drugs' bilayer-modifying potency.

31 cent bulge, affording a 100-fold increase in potency.

32 ility of human insulin while maintaining its potency.

33 ally affect multiple proteins with different potencies.

34 nship and delivered analogues with nanomolar potencies.

35 rboxamide analogues that have sub-micromolar potencies.

36 ted in compounds with low- to sub-micromolar potencies.

37 -EU-1180-453 was found to increase glutamate potency 2-fold, increase the response to maximally effec

38 tem significantly improved GnRH-R antagonist potencies across several species, mandatory for a succes

39 reactive protein, with potentially different potency across vascular beds.

40 H-CoVnb-112 retains structural integrity and potency after nebulization.

41 ave arrived at two leads possessing improved potency against clinical VRE strains from MIC = 2 mug/mL

42 ve inhibitor, CCG258747, which has nanomolar potency against GRK2 and excellent selectivity over othe

43 GHP-88309 showed nanomolar potency against HPIV3 isolates in well-differentiated hu

44 ry carbon atom, with up to 40-fold increased potency against human class I HDACs (e.g., JT86, IC(50)

45 ol-5-yl)pyrogallol, with a 300-fold improved potency against human GS.

46 the basis for developing novel PIs with high potency against PI-resistant HIV-1 variants with a high

47 natural product with reported sub-nanomolar potency against several cancer cell lines.

48 an produced antibodies retaining exceptional potency against some subtype C viruses.

49 rotein kinase inhibitors that show nanomolar potency against T. brucei bloodstream forms, Leishmania

50 based on paroxetine, demonstrates increased potency against the GRK2 subfamily and favorable pharmac

51 9 contributes to its significantly enhanced potency, along with excellent selectivity over other ami

52 of aryl hydrocarbon receptor-mediated toxic potencies among homologues of chrysene with structural m

53 have pinpointed DBPs with the greatest toxic potency, analytical methods have been lacking for quanti

54 epothilone analogues aiming to improve their potencies and other pharmacological properties as part o

55 2018;140:3454-3460] that their potencies and specificities are related to differential

56 t demonstrates subnanomolar HDAC6 inhibitory potency and a hundred- to a thousand-fold HDAC6 selectiv

57 which are shown to effectively modulate both potency and absorption, distribution, metabolism, and ex

58 ive state, opening new opportunities to tune potency and agonism of allosteric effectors.

59 ly relevant model to enhance its therapeutic potency and avoid off-target effects.

60 a full agonist in Ca(2+)-release assays; its potency and binding affinity for Ins(1,4,5)P(3)R were si

61 e most active TH on PPARgamma with nanomolar potency and binding affinity.

62 The neutralizing potency and breadth of the bNAbs tested was significantl

63 d several compounds with increased antiviral potency and broadened activity.

64 tutions at residue 38 (I38T/F/M) reduced BXM potency and caused virus rebound in treated patients, al

65 ts into the impact of structural features on potency and chemical stability, informing future utility

66 ds, positively influencing pharmacokinetics, potency and conformation.

67 akes a balanced look at the problems of drug potency and drug resistance.

68 in morphine-tolerant mice restores morphine potency and efficacy, whereas the onset of opioid withdr

69 terminals is a key factor determining their potency and efficacy.

70 f JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivity.

71 otease and a serine hydrolase with nanomolar potency and exceptional specificity.

72 , there is a pressing need for greater sgRNA potency and generalizability across various experimental

73 n of compound 4 with desired FXIa inhibitory potency and good oral bioavailability but high in vivo c

74 log, GAT592 (9j), exhibited moderate ago-PAM potency and improved aqueous solubility with therapeutic

75 -dimethyl-l-tyrosine (MACE4) showed the best potency and in vivo antinociceptive activity of this ser

76 and alpha3beta4 receptors, albeit with lower potency and less desensitizing effect.

77 opioid receptor but that have high analgesic potency and low risk of adverse effects, particularly no

78 resentatives combined submicromolar cellular potency and nanomolar target affinity with balanced phys

79 identification of compound 42 with excellent potency and pharmacokinetic profile are discussed.

80 meric separation, as well as improvements in potency and pharmacokinetics were desirable for discover

81 clic amine inhibitors displaying exceptional potency and PK properties.

82 However, challenges related to weak potency and poor pharmacokinetic properties have hampere

83 rtunity against high-risk DLBCL tumors using potency and precision.

84 atures of TOP sequences that determine their potency and quantify these as a metric that accurately p

85 , analogues were synthesized to increase the potency and reduce metabolic liabilities of this series.

86 ication of immune cell therapies, increasing potency and safety and broadening their potential for tr

87 rality in the DNA gap region can enhance the potency and safety of gapmer ASOs modified with high-aff

88 th SphKs have been reported, improvements in potency and selectivity are still needed.

89 d diverse inhibitors with varying degrees of potency and selectivity for BRD9 over BRD7.

90 -IV consistently displayed the most improved potency and selectivity for Na(V)1.7, examined alongside

91 tivity of the peptide can improve gHwTx-IV's potency and selectivity for Na(V)1.7.

92 s of simplified analogues that retained both potency and selectivity for the inhibition of prokaryoti

93 The structural basis for differential potency and selectivity of BRD9 inhibitors is largely un

94 he first structure-activity relationships on potency and selectivity of several iminocyclitols (2-7)

95 The key to balancing potency and selectivity while minimizing P-gp mediated e

96 This includes the increase in target potency and selectivity, alternative chemical scaffolds,

97 The impact of spirocycles on potency and selectivity, including the aspect of stereoc

98 d substituent of iminocyclitols affect their potency and selectivity.

99 a derivative, Irresistin-16, with increased potency and showed its efficacy against Neisseria gonorr

100 The ENRIs determine the potency and specificity of nuclear RNAi responses by gat

101 We have determined agonist potency and specificity profiles for rat P2X2 receptors;

102 ication of novel GSK3beta inhibitors of high potency and specificity.

103 Hits can be profiled to determine potency and the site of crosslinking, and subsequently d

104 died the effects on progression of treatment potency and time-of-first treatment after infection.

105 blot analyses, were performed to assess the potency and to characterize the binding mode of the newl

106 cellular uptake, intracellular trafficking, potency and toxicity.

107 providing a quantitative measurement of drug potency and tumor-related cachexia.

108 GluN2D are currently underdeveloped with low potency and uncharacterized binding modes.

109 explored trial outcomes by reducing in vivo potency and varying the distribution of sensitivity to V

110 n isoforms that differ in tissue expression, potency, and function, particularly in cellular prolifer

111 rapeutic potential due to their specificity, potency, and low toxicity.

112 ater solubility, brain penetration, high EP2 potency, and selectivity.

113 en provided evidence that changes in cocaine potency are associated with alterations in DAT affinity

114 tal design, we posit that changes in cocaine potency are driven by alterations in dopamine neuron act

115 vidence suggests that differences in cocaine potency are linked to several symptoms of cocaine use di

116 sed on our results we propose gene-signature potencies as a novel valid alternative for the quantitat

117 as the molecular underpinnings for both the potency aspects and the limitation sides of the OSKM rep

118 immunodiffusion (SRID), the accepted vaccine potency assay.

119 However, in contrast to cIPV, potency assays for sIPV have not been standardized, no i

120 th Raman spectroscopy for the development of potency assays.

121 ral crest cells have different developmental potencies at different levels along the body axis of the

122 e differences that might explain the gain of potency at alpha3beta2 nAChRs.

123 lation uniquely enhanced binding and agonist potency at alpha7 receptors.

124 0 new agonist chemotypes with sub-micromolar potency at MT receptors, with compound 21 reaching EC(50

125 ing a possible relationship between in vitro potency at Na(V)1.7 and affinity for lipid bilayers.

126 ing sensitization-related changes in cocaine potency at the DAT, consistent with an incentive-sensiti

127 ng IntA influences cocaine use and cocaine's potency at the DAT.

128 ing interaction with IDO1, to the inhibitory potency at the low nanomolar level in several tumoral se

129 oxaliplatin, Rh-PPO displays ninefold higher potency at tumor sites.

130 nd 23h) were identified with nanomolar range potency based on a systematic structure-activity relatio

131 urrent practice of starting from the highest potency binder is an ineffective method for discovering

132 Agonist potency, binding affinity, and relevant pharmacological

133 h abolished IgE binding and anaphylactogenic potency but retained T-cell activation was generated.

134 hat APA regulates HSC self-renewal and multi-potency by affecting stem cell activation and glutaminol

135 The molecular basis for the retention of potency by this G-quadruplex ligand has been examined us

136 everal analogs exhibited improved functional potency (cAMP, beta-arrestin 2), metabolic stability, an

137 This study shows that high CD73 inhibitory potency can be achieved by simply introducing a small su

138 The use of high-potency cannabis is associated with cannabis use disorde

139 exhibiting ProT(QQQ) affinity and activation potency comparable with WT SC(1-246).

140 lower dissociation rate and 4-24-fold higher potency compared to those of the monovalent peptides for

141 Its potency compares well with established MIF inhibitors, w

142 in-drug conjugates demonstrates that a lower potency compound is more effective in vivo than other ag

143 OAE, whose potency did not differ from SAE, protected ROS-exposed C

144 volume spheroids, likely contributing to the potency differences.

145 that showed further improvements in Na(v)1.7 potency (E1N, E4D, Y33W, Q34S-Na(v)1.7 pIC(50) = 8.1 +/-

146 erential binding affinity and neutralization potency (E393D).

147 on of lead compounds, being used to increase potency, enhance selectivity, improve pharmacokinetic pr

148 erapeutics but also highlights dramatic drug potency enhancement via halogen substitution.

149 nt epothilone B analogues, demonstrating the potency enhancing effects of the fluorine residues and t

150 Our aims were to determine the TTR-binding potency for contaminant mixtures as found in house dust,

151 dose-specific ratios to provide the correct potency for each component, and yet the formulations mus

152 erize novel compounds with specific cellular potency for either WT or mutant SHP2.

153 The resulting compounds retain high potency for FKBP51 and excellent selectivity over the cl

154 ized and shown to give a 20-fold increase in potency for increasing FXN expression.

155 surprisingly, displayed up to 52-fold higher potency for the alpha3beta2 neuronal nAChR subtype (IC(5

156 4bs) bNAb with outstanding breadth (97%) and potency (GeoMean IC(50) = 0.048 mug/mL).

157 electively inhibited growth of C. acnes with potency greater than antibiotics commonly used in the tr

158 gues with aromatic side arms showed improved potency (half-maximal inhibitory concentration (IC(50))

159 ild-type SARS-CoV-2 in vitro with remarkable potency (half-maximal inhibitory concentration of <2 ng/

160 However, this therapeutic potency has not been well claimed when applied to human

161 ne series displayed more than 10-fold higher potencies; however, in the early project phase, this ser

162 l-molecule inhibitor of CLC-2 with nanomolar potency (IC(50) = 17 +/- 1 nM).

163 ntial structural replacements to improve the potency (IC(50)), pharmacokinetic properties including t

164 GFR(L858R/T790M/C797S) mutant with nanomolar potencies in a reversible binding mechanism.

165 The three peptides show greater inhibitory potencies in cellular and mucosal tissue pre-clinical mo

166 While mHAAs and mHAMs have similar potencies in reducing MTT activity, mHAMs induced greate

167 evaluate its pharmacokinetic parameters and potency in a CDI mouse model.

168 o retigabine, 23a and 24a showed also higher potency in activating heteromeric Kv7.2/Kv7.3 and homome

169 ed in our first antagonist with subnanomolar potency in AgrC-I, while analogs designed to contain a d

170 grase that exhibited low nanomolar antiviral potency in cell culture and encouraging PK properties.

171 low micromolar to upper nanomolar inhibitory potency in cell-based assays, are selective against othe

172 compound RJ-LC-07-48 which exhibited greater potency in drug-resistant NSCLC cells (IC(50) = 17 nM) a

173 bles the design of AZ1 analogs with enhanced potency in enzymatic assays.

174 topes, and measured functional activities as potency in inhibition of hemagglutination induced by cla

175 ) evaluate the transition of opioid dose and potency in the first 2 years from initial prescription,

176 id in vitro and enabled higher mRNA delivery potency in vivo at a low dose of 0.1 mg kg(-1) when form

177 ce, the neural processes that govern cocaine potency in vivo remain unclear.

178 n intramolecular interaction led to improved potency in whole blood.

179 rom a short in vivo half-life and suboptimal potency in whole blood.

180 cepts, coupled with optimization of cellular potency, in vitro drug-target residence times, and in vi

181 of these may reach levels of in vitro target potency, including brain and gut exposure of thimerosal

182 sulin analog-as a structurally minimal, full-potency insulin.

183 alysis revealed that the basis for this high potency is a unique sulfur-aromatic interaction network

184 Cannabis potency is determined by the concentration of Delta(9)-t

185 monstrate a novel mechanism by which cocaine potency is determined in vivo These studies identify a n

186 hibited C. thermarum NDH-2 activity, and its potency is higher in a membrane environment compared to

187 3(2H)-benzofuranone (BZF), whose antioxidant potency is notably higher than the antioxidant potency o

188 ever, an additional challenge in determining potency is to differentiate between vaccine antigens in

189 Compound 34 has excellent potency, isoform selectivity, metabolic stability across

190 Many derivatives showed greater potency (K(I)s-CA IX 19.1-408.5 nM) and selectivity (II/

191 hat the purine 6-amino is essential for high potency, likely because of strong hydrogen bonding with

192 und to possess human PNMT (hPNMT) inhibitory potency <5 nM versus AdoMet.

193 ct thyroperoxidase and deiodinase inhibition potencies (methimazole, iopanoic acid, and propylthioura

194 r OATP2B1 inhibition and quantify inhibitory potencies necessary for extrapolation of clinical drug-d

195 phorylation of the DAT, and enhanced cocaine potency observed after periods of sleep.

196 ing that they can predict the cAMP-signaling potencies of AM and AM2/IMD chimeras.

197 Potencies of CXCL12/CXCL12(1)/CXCL12(2) were higher than

198 ing is a key to accurate assessment of toxic potencies of environmental pollutants.

199 The various bioactivity types and potencies of peptidic natural products (PNPs) are of hig

200 AHR-activating potencies of Turkish, filter, and instant coffee were de

201 lizing antibody showed an estimated relative potency of 454 IU/mg and minimal effective dose 50% (MED

202 studies demonstrate the enhanced therapeutic potency of a novel Dual-CAR T cell product with the pote

203 NA loading capacity, system versatility, and potency of action, ProSilic provides unique attributes a

204 The potency of adoptive T cell therapies targeting the cell

205 The potency of airway-delivered anti-HA bNAbs was highly dep

206 d that whole semen significantly reduces the potency of antibodies and microbicides that target glyca

207 esents a possible approach for enhancing the potency of ASOs with diverse nucleic acid modifications.

208 ated the phenotypic markers and chondrogenic potency of avascular and vascular meniscal cells and cho

209 -has been shown to dramatically increase the potency of biologically active molecules(1-3).

210 mediated through the nitric oxide scavenging potency of CFH, increasing basal vascular tone and impai

211 is change also leads to decreased inhibition potency of clavulanic acid.

212 We found that optimization beyond potency of degradation, including degradation efficiency

213 However, the apparent potency of different interventions can vary considerably

214 that may define binding affinity and agonist potency of formyl peptides.

215 enoid compounds as well as the antioxidative potency of fruit and their parts, such as peel, flesh, a

216 The greater UDB potency of GS-967 and eleclazine was attributed to the h

217 Treatment with IL-13 increased the potency of histamine, carbachol, and leukotriene D(4) as

218 to be able to predict the bilayer-perturbing potency of hydrophobic/amphiphilic drugs candidates.

219 and prospective trials have demonstrated the potency of immunotherapeutic approaches with antibody-dr

220 y aberrant enzyme would explain the superior potency of isavuconazole against A. castellanii.

221 In the presence of serum albumin, the potency of JMS-053 as an in vitro inhibitor of PTP4A3 an

222 ing a bioluminescent assay, the efficacy and potency of kappa opioids was determined.

223 The potency of latency reversal was significantly higher fol

224 in, we have improved the reproducibility and potency of LPS in the model using two injections distal

225 ugs from classical chemotherapeutics and the potency of mitotic kinase inhibitors to generate a class

226 it distinctly affected both the efficacy and potency of partial kappa agonists, such as the benzomorp

227 Our findings suggest that the potency of poorly neutralizing antibodies, which are com

228 e, we report the optimization of the in vivo potency of pyrazolopyrimidines, a class of highly select

229 tency is notably higher than the antioxidant potency of quercetin, was investigated in twenty quercet

230 ther, these results help to explain the high potency of RDV against RNA viruses in cell-based assays.

231 intervention strategies must target both the potency of SARS-CoV-2 and its evasiveness.

232 into the origins of regiospecific changes in potency of siRNAs and the increased protection against 5

233 ifications have been identified that enhance potency of small interfering RNAs (siRNAs) and that redu

234 city of monoclonal antibodies (mAb) with the potency of small molecule therapeutics, are one of the f

235 directly compared the in vitro chondrogenic potency of TGF-beta1 and KGN using a high resolution mic

236 However, the breadth and potency of the elicited responses have been less than op

237 racellular Ca(2+) increases the affinity and potency of the endogenous agonist alpha-melanocyte-stimu

238 tamase variants is associated with decreased potency of the inhibitor clavulanic acid, which is used

239 izing activity, and verified the therapeutic potency of the lead candidates in mice and non-human pri

240 fant serum; to study whether the TTR-binding potency of the mixtures follows the principle of concent

241 The extreme potency of the plant toxin, ricin, is due to its enzymat

242 The viability and potency of this approach are demonstrated with an electr

243 L12/CXCL12(1)/CXCL12(2) were higher than the potency of ubiquitin.

244 We also determined their potency on CGRP-induced relaxations in mouse and human v

245 ng metabolically stable inhibitors with high potency on enzymatic, NanoBRET, and whole blood assays,

246 ture-activity relationship enabled efficient potency optimization.

247 current BET inhibitors are limited by their potency or oral bioavailability.

248 In this "potency paradox", farmland in the central US has become

249 inities between ~1 and 650 nm and activation potencies ranging from 1.8-fold that of WT SC(1-246) to

250 nthesized and tested, revealing ligands with potencies ranging from 470 picomolar to 6 micromolar.

251 and coregulator recruitment that affects the potency rather than the efficacy of the receptor respons

252 437.44), which showed considerably improved potency, reaching an IC(50) value up to 100-fold lower t

253 y constrained alpha-RgIA analogues with high potency, receptor selectivity, and enhanced human serum

254 In this study, we show that Ag potency regulates the kinetics but not the magnitude of

255 r mechanism underlying such an expanded 2CLC potency remains elusive.

256 expression signature creation, drug reversal potency scoring and in silico validation.

257 Lead optimization involved modulating potency, selectivity, and ADME properties which led to t

258 terobivalent design strategy to modulate the potency, selectivity, and binding kinetics of Na(V) chan

259 ivity, lead optimization efforts focusing on potency, selectivity, and oral bioavailability led to th

260 , M4K2117, and M4K2163, each with a superior potency, selectivity, and/or blood-brain barrier (BBB) p

261 he lead compound 3a that displayed excellent potency, selectivity, safety profile, and efficacy in vi

262 nhibitor which shows a functionally relevant potency shift between human and preclinical species (e.g

263 e amino acid (I960 -> V) responsible for the potency shift.

264 the identification of (R)-27, which balanced potency, solubility, and lipophilicity to allow proof-of

265 in cannabis use and the availability of high-potency strains.

266 sent minimal toxicity and maintain anti-VEGF potency, suggesting that our approach may have the poten

267 on of JS230 cumulated into growth inhibitory potency superior to that of classical two- or three-drug

268 antly less potent HA for vaccine release and potency testing across the vaccine's shelf life.

269 216, GSK1278863, Bay85-3934) have the higher potency than DMOG.

270 ted tier 2 neutralizing antibodies of higher potency than noncomplexed trimers.IMPORTANCE Soluble for

271 h nirsevimab displaying significantly higher potency than palivizumab.

272 d16:1 S1P is an S1P(2) agonist, it has lower potency than the most abundant S1P species (d18:1 S1P).

273 first-in-class hit with nanomolar anti-RABV potency that blocks RABV G protein-mediated viral entry.

274 a specific bioactive compound with improved potency that inhibits pre-miR-21 processing, reducing ma

275 Milk of T buffaloes inhibited with greater potency the viability of human HCT116 and Cal 27 cancer

276 Despite their therapeutic potency, their ability to cause lymphocyte proliferation

277 In simulations, even a low potency therapy with a drug which reduces the replicatio

278 aryl regions revealed approaches to increase potency through substituents believed to enhance separat

279 that maintains hematopoietic stem cell (HSC) potency throughout life.

280 that, in some cases, greatly increase their potency to activate inflammatory signaling within immune

281 has previously been shown to have equivalent potency to gemcitabine in the pancreatic cancer cell lin

282 differentiation and exert high efficacy and potency to help Env trimer humoral immune responses.

283 Finally, we discuss mechanisms with the potency to impinge on the cellular organization of the C

284 and to extrapolate the in vitro TTR-binding potency to in vivo inhibition levels of T4-TTR binding i

285 arental bulk FG cells, PAWI-2 showed greater potency to inhibit cell viability and self-renewal capac

286 at later results in expanded differentiation potency to multiple lineages, as well as improved effici

287 a class of IspH inhibitors and refine their potency to nanomolar levels through structure-guided ana

288 prioritize small molecules that present high potency to reverse expression of signature genes for fur

289 apsaicin results in compounds with nanomolar potencies toward human acetylcholinesterase (AChE) and b

290 which was subsequently optimized in terms of potency toward both targets and metabolic stability.

291 oration of a thiazole core leads to improved potency toward LOXL2 inhibition via an irreversible bind

292 ognized side cavity that increased inhibitor potency toward SphK2.

293 Compounds with nanomolar potency versus Plasmodium DHODH and Plasmodium parasites

294 The bivalency of IgG antibodies can increase potency via avidity, but has never been described as ess

295 P2X1 antagonistic potency was assessed in 1321N1 astrocytoma cells stably

296 siRNA potency was maintained when these modifications were inc

297 The selected compounds showed an effect with potency, which correlated with the earlier observed anti

298 es show minimal affinity maturation and high potency, which is promising for vaccine design.

299 that have exceptionally high charge-reducing potencies with some molecules requiring 5-fold less than

300 Compound 28 showed good in vitro potency, with pharmacokinetic profile across species wit