コーパス検索結果 (1語後でソート)
通し番号をクリックするとPubMedの該当ページを表示します
1 pounds, exemplified by 35 and 36, display nM potency against 12-LOX, excellent selectivity over relat
3 the majority of which exhibit submicromolar potency against 3'-end processing and strand transfer, t
4 ), was synthesized and tested for inhibitory potency against [(3)H]WIN35,428, [3H]citalopram, and [3H
5 d human 5-lipoxygenase (5-LOX) with improved potency against 5-LOX due to its reduction of the iron c
7 from milk and plasma had equal neutralizing potencies against a tier 1 virus (r = 0.65; P < 0.0001),
8 ical development that demonstrates excellent potency against a broad range of dimorphic and filamento
11 for compound 5i) and low micromolar cellular potency against a mutant BRAF melanoma cell line, WM266.
13 ike the parent molecules, display no loss of potency against a panel of clinically important PI-resis
15 inactive form kinase inhibitors due to equal potency against a panel of oncogenic activating mutation
17 50), 0.6 muM), which exhibited high in vitro potency against a panel of prostate and breast cancer ce
19 and displayed submicromolar to low nanomolar potency against a panel of TKs, including receptor (plat
21 ed systemically to mice and displays greater potency against a spectrum of human cancer cell lines th
22 compound 1C8 as displaying strong anti-HIV-1 potency against a variety of clinical strains in vitro.
23 l peptoid mimics which exhibit high in vitro potency against a variety of Gram-positive and Gram-nega
25 hermore, this inhibitor maintains impressive potency against a wide spectrum of HIV including a varie
26 8, 10, 12, 14) structures possessed similar potencies against AChE, but the latter structures were m
28 t tactile allodynia and showed diminished in potency against acute nociception without supraspinal/sp
30 K inhibitors, PF-06463922 displayed superior potency against all known clinically acquired ALK mutati
31 ibitor (Cinn-GEE) of substantially increased potency against all three enzymes (e.g., K(I) = 5.4 micr
33 ndoxifen (10), displayed elevated inhibitory potency against aromatase and enhanced affinity for estr
34 g of 26 compounds revealed 22 with nanomolar potency against axenically cultured bloodstream trypanos
35 nt to anti-CD19 immunotherapy, demonstrating potency against B-ALL comparable to that of CD19-CAR at
39 MRSA, and VanA and VanB VRE) and impressive potencies against both vancomycin-sensitive and vancomyc
41 om triazine to purine, improved the in vitro potency against both cruzain and rhodesain by 350-fold,
42 zinone (BTZ) inhibitors have shown nanomolar potency against both drug-susceptible and multidrug-resi
45 droquinolines (HHQs) that show low nanomolar potency against both pathogenic and transmissible intra-
48 ain variant C184A showed the same inhibitory potency against both TACE forms as wild type TACE Pro.
53 ole antifungal with an expanded spectrum and potency against Candida spp., Aspergillus spp., and othe
54 ole antifungal with an expanded spectrum and potency against Candida spp., Aspergillus spp., and othe
56 ernative lead candidate 4ab with a nanomolar potency against CDK2 and CDK9 and potent antiproliferati
57 nhibition of ATP-dependent kinases, and good potency against Cdks has been reported for representativ
58 azahypoxanthine skeleton exhibited nanomolar potencies against cell lines representing cancers with d
59 nds are more toxic than baicalein, and their potency against cell growth is compromised by the presen
60 both also enhanced anti-P-gp170 activity and potency against cell growth; however, the presence of P-
61 acid residues that greatly diminish the VCC potency against cells and investigated the interplay bet
63 nalogues (e.g., Tb14), some with exceptional potencies against certain cell lines [e.g., Tb32 with IC
64 any of the compounds tested showed excellent potency against chloroquine sensitive and resistant stra
66 ility of 1 was associated with (i) decreased potency against cIAP2 and affinity for XIAP BIR3 and (ii
67 amides as HCV protease inhibitors addressing potency against clinically relevant resistant variants.
69 s (BKIs) that have nearly identical in vitro potency against Cryptosporidium but display divergent PK
71 Compounds 1-6 showed moderate inhibitory potency against DHFR from Pneumocystis carinii, Toxoplas
72 e-2-carboxamides with low nanomolar in vitro potency against DHODH from P. falciparum, P. vivax, and
73 ate important determinants for Btk inhibitor potency against different signaling pathways and provide
74 5-deaza methotrexate (MTX) on the inhibitory potency against dihydrofolate reductase (DHFR) from diff
76 mely 4a and 4e, have been screened for their potency against DNA topoisomerase II, and it has been ob
77 e newly synthesized compounds exhibited high potency against DNA-PK and potentiated the cytotoxicity
78 necarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprotein (
79 3-position of P2 quinoxaline maintain better potency against drug resistant variants, likely due to r
80 esent a novel class of compounds with strong potency against drug sensitive and resistant P. falcipar
81 HSP targeted DOC conjugates exhibited high potency against DU145 cells with an IC(5)(0) of 2.4 nM.
82 Indole 24 is nontoxic and showed increased potency against dynamin I and II in vitro and in cells (
87 which demonstrated excellent selectivity and potency against effector human memory T cells (subnanomo
88 mor cell lines and showed superior antitumor potency against EGFR-positive tumor xenografts as compar
93 effective vaccine into one with significant potency against established E7-expressing metastatic tum
96 quester Y551 was an important determinant of potency against FcepsilonR signaling as Y551 sequesterin
98 -folate and demonstrated its selectivity and potency against folate receptor 1 (FOLR1)-expressing ova
100 set of furin inhibitors with nanomolar range potency against furin when assayed in a biochemical clea
102 idity of BILN 2061, while conferring greater potency against genotype 1, rendered it more sensitive t
103 in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genoty
104 ed to 4-methyl hexanoic acid, having similar potency against Gram negative and Gram positive pathogen
105 ative chemistry efforts improved biochemical potency against gram-negative isozymes 300-fold and affo
108 Synthetic araiosamines were shown to exhibit potency against Gram-positive and -negative bacteria des
109 idue antimicrobial peptide with bactericidal potency against Gram-positive bacteria such as Listeria.
113 Compound 5 g shows low nanomolar inhibitory potency against HDAC6 and a selectivity of approximately
115 omolar concentrations and displays excellent potency against hepatitis B virus (HBV) and varicella-zo
116 type-specific immune responses with limited potency against heterologous viral strains and genotypes
119 pounds show single-digit nanomolar antiviral potencies against HIV vectors that carry wild-type (WT)
121 Several ProTide compounds showed substantial potency against HIV-1 at low micromolar range while the
122 d to synthesize compounds with: (1) improved potency against HIV-1 integrase, (2) improved anti-HIV e
126 Although both compounds display similar potencies against human topoisomerase IIalpha and IIbeta
129 abrogating the previously reported antiviral potency against human immunodeficiency virus (HIV-1).
130 ective DNA vaccine into one with significant potency against human papillomavirus type 16 E7-expressi
131 3b would preserve transport selectivity and potency against human tumor cells, 3b regioisomers with
133 side aryl ring, while having good inhibitory potencies against IN in extracellular assays, are not an
134 zed pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNas
135 5-substituted analogs exhibit low micromolar potency against in vitro cultures of drug-resistant and
136 r in the thiazole ring appears important for potency against IN, as its replacement with an oxygen or
137 ning only a salicylic acid showed inhibitory potency against IN, none of the compounds containing onl
138 up (e.g. 5-13) showed significant inhibitory potency against IN, while the presence of either salicyl
141 erating compound E67-2) has no effect on the potency against KIAA1718 but, unexpectedly, lost inhibit
143 ted extraordinary neutralization breadth and potency against large panels of cross-clade pseudoviruse
144 (20), resulting in an 18-fold improvement in potency against lck and a 50-fold increase in potency in
145 , a first generation lead with low nanomolar potency against life MeV and attractive physical propert
146 igands demonstrated significant antiandrogen potency against LNCaP and Enzalutamide-resistant prostat
148 ion with front-line antibiotics enhanced the potency against M. tuberculosis by more than 100-fold, t
151 taining potent TACE inhibition, but reducing potency against matrix metalloproteases (MMPs) thus incr
152 ear whether these antibodies exhibit similar potency against mature dendritic cell (mDC)-mediated HIV
153 g a (14)C-lactate transport assay, and their potency against MCT1-expressing human tumor cells was es
155 time in this series, 16a' provided nanomolar potency against MMP-1, -7, and -9 (IC(50)'s = 110, 140,
156 These reverse amides also exhibited less potency against monoamine oxidase (MAO) enzymes and thus
158 drophobic surface, providing a basis for its potency against MRSA known to deploy positively charged
159 uinolone-class compounds that have increased potency against Mtb and the ability to overcome resistan
161 of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compr
162 f these taxoids exhibited exceptionally high potency against multidrug-resistant cell lines, and seve
163 C220, KW-2449, sorafenib, and sunitinib) for potency against mutant and wild-type FLT3, as well as fo
165 2-carboxamide analog (1), had low micromolar potency against Mycobacterium tuberculosis (Mtb), high m
166 one with improved in vitro and intracellular potency against Mycobacterium tuberculosis, including mu
168 f protoxin II-NHCH3, a molecule with greater potency against Nav1.7 channels (IC50=42 pM) than the or
169 ctive metabolite of 1, has retained in vitro potency against newly emerging antifolate-resistant mala
173 PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the
175 These compounds were assessed for their potency against P-gp and another transporter (MRP1), for
177 l spectrum of activity, exhibiting excellent potency against P. aeruginosa (MIC(90), 2 microg/ml) and
179 was to identify indolequinones with improved potency against pancreatic cancer and to define their me
180 Several new PIs exhibit nanomolar antiviral potencies against patient-derived wild-type viruses from
182 ersely, N-terminal acetylation increased the potency against PC2 nearly 3-fold, whereas C-terminal am
184 ty in rats, dogs, and monkeys while the high potency against PDE5 and desirable selectivity versus ot
185 Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the i
186 ounds, 7 and 8 showed the highest inhibitory potency against Pf enoyl-ACP-reductase (PfFabI), followe
187 properties and PK parameters, low nanomolar potency against PI3Kalpha and mTOR, and excellent inhibi
189 We sought to identify compounds with higher potency against Plasmodium DHODH while showing greater s
190 ances over azithromycin in vitro in terms of potency against Plasmodium falciparum (over 100-fold) an
192 , transition state analogs that exhibit high potency against PNP in the malaria parasite Plasmodium f
193 alogues with improved antibacterial in vitro potency against polymyxin resistant recent clinical isol
195 d that possesses increased cytotoxicological potency against prokaryotic cells compared to eukaryotic
197 ) = 58 muM), which has reasonable inhibition potency against Pseudomonas aeruginosa TMK (PaTMK), was
198 eversible, slow-binding inhibitors of modest potency against PTP1B, SHP-1, and a dual-specificity pho
199 resveratrol has a broad range of inhibitory potencies against purified PKC that depend on the nature
200 e rounds of optimization to improve compound potency against purified enzyme and intracellular Plasmo
201 L-chicoric acid (3) which are important for potency against purified HIV-1 integrase and for reporte
202 h the parent tetracycline exhibited marginal potency against purified IN, all substituted tetracyclin
204 meric D-chicoric acid (4) retains inhibitory potency against purified integrase equal to its L-counte
206 e region (analogue 3) doubled the inhibitory potency against recombinant human (rh) DHFR (IC(50) = 0.
207 plasmin in the subnanomolar range, and their potency against related trypsin-like serine proteases in
208 ately improved ( approximately 2- to 4-fold) potencies against replicating Mycobacterium tuberculosis
211 ci (VRE), and fluoroquinolones with improved potency against respiratory pathogens and multidrug-resi
212 y reported; however, the greater decrease in potency against rlDHFR compared to pcDHFR and tgDHFR res
213 1 RT in the micromolar range while retaining potency against RT variants carrying one of three major
215 nds studied, 46a,b showed not only very good potency against RXRalpha (K(i) = 6 nM) but was also foun
218 d 3 demonstrated increased growth inhibitory potency against several human tumor cell lines in cultur
219 ilino)-6,7-dimethoxyquinazoline, had a 15 nM potency against Src TK and was selective over receptor t
220 in-based inhibitors with 9-18-fold increased potency against Staphylococcus aureus (Sa) and Bacillus
221 ed by its ability to impart greater relative potency against stromelysin when larger hydrophobic grou
222 lead compound, 17b, that exhibited nanomolar potency against T. brucei with excellent selectivity for
224 diaminopyrimidine-based inhibitors with good potency against T790M-containing mutants of EGFR, high s
226 effective compound, 22 (MN-64), showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and
227 cidal activity was developed on the basis of potency against TbcatB and various calculated physical p
228 et of inhibitors designed to possess varying potencies against the deformylase enzyme revealed a line
229 t the tumor cells, but some of them had high potencies against the L1210 cells and were more potent a
230 yrosine kinase inhibitors with low nanomolar potencies against the members of the VEGFR and PDGFR kin
231 have been synthesized and tested for binding potencies against the three cloned human NT receptors (h
233 ounds from this series demonstrated in vitro potency against the 3D7 and Dd2 strains of P. falciparum
234 high bioavailability and its nanomolar-range potency against the antiangiogenic receptor tyrosine kin
235 lular calcium mobilization and a much higher potency against the chemerin(149-157) nonapeptide-induce
236 ts have shown a 40-fold and 200-fold loss in potency against the CRFR1 H199V and M276I mutant recepto
237 ized compounds, 22 showed excellent in vitro potency against the cultured parasites (W2 IC(50) = 13 n
238 tifolate, trimethoprim, because of a lack of potency against the dihydrofolate reductase enzyme.
239 refore, the retained and improved inhibitory potency against the drug-resistant variants A156T, D168V
241 taxoids exhibited virtually no difference in potency against the drug-sensitive and drug-resistant ce
242 because (i) a 65828 analogue with much lower potency against the enzymatic activity of ANG failed to
243 ring resulted in inhibitors of equal or less potency against the enzyme and decreased efficacy in a c
245 , have demonstrated profound selectivity and potency against the FLT3 target, and are currently being
246 otency (IC(50) = 0.42 microM) as well as the potency against the growth inhibition of tumor cells in
253 on of inhibitors with significantly improved potency against the key resistant variants and with incr
254 he optimized compounds display low nanomolar potency against the mast cell target and several hundred
255 re were prepared that possessed subnanomolar potency against the NS3 protease in a subgenomic replico
256 pectrum antimicrobial activity, and enhanced potency against the opportunistic human pathogen Acineto
257 revealed that an inhibitor with insufficient potency against the p110beta isoform was less effective
258 ies of noncovalent inhibitors with nanomolar potency against the papain-like protease (PLpro) from th
260 yclic inhibitors displayed 20-50-fold higher potency against the PDF active site (K(I) as low as 70 p
261 microM), but a more substantial increase in potency against the rat liver DHFR led to a reduction in
262 be nzothiophen-1-yl]acetamide) combined high potency against the target enzyme (DNA-PK IC = 8 nM) wit
264 on of the series scaffold to further enhance potency against the target while also improving pharmaco
265 ciating rate, thus increasing its anti-HIV-1 potency against the temporarily exposed target in NHR an
271 ed against the full-length human enzyme, the potency against the yeast enzyme has decreased significa
272 rmation to that of IGF-1R/IR, explaining the potency against these two structurally distinct kinase f
274 ynergistic effect and significantly enhanced potency against three esophageal adenocarcinoma cell lin
277 cells), demonstrating 3- to 10-fold greater potency against tumor cell lines when compared with norm
278 ession correlates negatively with phagocytic potency against tumour cells, and blockade of PD-1-PD-L1
282 ainst HIV strains with wild-type RT but lose potency against variants with single Y181C and double K1
283 le round replication assay and have improved potency against vectors harboring the major forms of dru
284 The molecule was evaluated both in vitro for potency against VEGF and in ocular VEGF-driven efficacy
285 scovery of second generation inhibitors with potency against viral strains bearing drug resistant IN
286 ough these prototype inhibitors have similar potencies against wild-type c-Met (K(i) = 6-7 nM), signi
289 Such adaptations appear to be critical for potency against wild-type and a wide range of drug-resis
290 cussed, focusing on optimization of cellular potency against wild-type and drug resistant parasites a
291 on of 8e (MK-4965), which has high levels of potency against wild-type and key mutant viruses, excell
293 critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and know
297 w analogue compound 2 that maintains greater potency against Y181C and K103N/Y181C variants and bette
299 , we now demonstrate that KP1019 retains its potency against yeast carrying the hypermorphic alleles
WebLSDに未収録の専門用語(用法)は "新規対訳" から投稿できます。