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1 pounds, exemplified by 35 and 36, display nM potency against 12-LOX, excellent selectivity over relat
2 the majority of which exhibit submicromolar potency against 3'-end processing and strand transfer, t
3 ), was synthesized and tested for inhibitory potency against [(3)H]WIN35,428, [3H]citalopram, and [3H
4 d human 5-lipoxygenase (5-LOX) with improved potency against 5-LOX due to its reduction of the iron c
6 from milk and plasma had equal neutralizing potencies against a tier 1 virus (r = 0.65; P < 0.0001),
7 ical development that demonstrates excellent potency against a broad range of dimorphic and filamento
9 Both compounds exhibited higher inhibitory potency against a COX-2 R120A variant than against the W
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
14 ne P2' moiety maintained excellent antiviral potency against a panel of multidrug-resistant HIV-1 str
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 ed systemically to mice and displays greater potency against a spectrum of human cancer cell lines th
20 compound 1C8 as displaying strong anti-HIV-1 potency against a variety of clinical strains in vitro.
21 l peptoid mimics which exhibit high in vitro potency against a variety of Gram-positive and Gram-nega
23 hermore, this inhibitor maintains impressive potency against a wide spectrum of HIV including a varie
28 K inhibitors, PF-06463922 displayed superior potency against all known clinically acquired ALK mutati
31 Although shishijimicin A and its extreme potencies against an array of cancer cell lines have bee
34 ndoxifen (10), displayed elevated inhibitory potency against aromatase and enhanced affinity for estr
35 otent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease,
36 g of 26 compounds revealed 22 with nanomolar potency against axenically cultured bloodstream trypanos
37 nt to anti-CD19 immunotherapy, demonstrating potency against B-ALL comparable to that of CD19-CAR at
39 ftazidime-avibactam demonstrated significant potency against Bcc and B. gladioli isolated from the sp
42 MRSA, and VanA and VanB VRE) and impressive potencies against both vancomycin-sensitive and vancomyc
45 om triazine to purine, improved the in vitro potency against both cruzain and rhodesain by 350-fold,
46 zinone (BTZ) inhibitors have shown nanomolar potency against both drug-susceptible and multidrug-resi
48 emporin B improves its membrane activity and potency against both Gram-negative and Gram-positive bac
51 droquinolines (HHQs) that show low nanomolar potency against both pathogenic and transmissible intra-
53 ain variant C184A showed the same inhibitory potency against both TACE forms as wild type TACE Pro.
57 ar potency against CA II and CA IV, and with potency against CA I one order of magnitude better than
58 olar potency against CA IX and sub-nanomolar potency against CA II and CA IV, and with potency agains
59 Very potent pan-inhibitors with nanomolar potency against CA IX and sub-nanomolar potency against
60 in the range 1.73-10.5 muM and exhibited low potencies against CaE (9.8-26% inhibition at 20 muM).
62 ole antifungal with an expanded spectrum and potency against Candida spp., Aspergillus spp., and othe
63 ole antifungal with an expanded spectrum and potency against Candida spp., Aspergillus spp., and othe
65 ernative lead candidate 4ab with a nanomolar potency against CDK2 and CDK9 and potent antiproliferati
66 nhibition of ATP-dependent kinases, and good potency against Cdks has been reported for representativ
67 azahypoxanthine skeleton exhibited nanomolar potencies against cell lines representing cancers with d
68 nds are more toxic than baicalein, and their potency against cell growth is compromised by the presen
69 both also enhanced anti-P-gp170 activity and potency against cell growth; however, the presence of P-
70 acid residues that greatly diminish the VCC potency against cells and investigated the interplay bet
73 nalogues (e.g., Tb14), some with exceptional potencies against certain cell lines [e.g., Tb32 with IC
74 any of the compounds tested showed excellent potency against chloroquine sensitive and resistant stra
76 ility of 1 was associated with (i) decreased potency against cIAP2 and affinity for XIAP BIR3 and (ii
77 ave arrived at two leads possessing improved potency against clinical VRE strains from MIC = 2 mug/mL
78 amides as HCV protease inhibitors addressing potency against clinically relevant resistant variants.
80 s (BKIs) that have nearly identical in vitro potency against Cryptosporidium but display divergent PK
82 e-2-carboxamides with low nanomolar in vitro potency against DHODH from P. falciparum, P. vivax, and
83 ate important determinants for Btk inhibitor potency against different signaling pathways and provide
85 part, but also displayed improved inhibitory potency against DNA methyltransferase 1, improved select
86 e newly synthesized compounds exhibited high potency against DNA-PK and potentiated the cytotoxicity
87 necarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprotein (
88 3-position of P2 quinoxaline maintain better potency against drug resistant variants, likely due to r
89 esent a novel class of compounds with strong potency against drug sensitive and resistant P. falcipar
90 HSP targeted DOC conjugates exhibited high potency against DU145 cells with an IC(5)(0) of 2.4 nM.
91 Indole 24 is nontoxic and showed increased potency against dynamin I and II in vitro and in cells (
93 which demonstrated excellent selectivity and potency against effector human memory T cells (subnanomo
94 mor cell lines and showed superior antitumor potency against EGFR-positive tumor xenografts as compar
101 quester Y551 was an important determinant of potency against FcepsilonR signaling as Y551 sequesterin
103 -folate and demonstrated its selectivity and potency against folate receptor 1 (FOLR1)-expressing ova
105 set of furin inhibitors with nanomolar range potency against furin when assayed in a biochemical clea
107 idity of BILN 2061, while conferring greater potency against genotype 1, rendered it more sensitive t
108 in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genoty
109 ric inhibitors, the 93-series, shows greater potency against GluN1-GluN2B NMDA receptors in such low
110 ed to 4-methyl hexanoic acid, having similar potency against Gram negative and Gram positive pathogen
111 ative chemistry efforts improved biochemical potency against gram-negative isozymes 300-fold and affo
114 Synthetic araiosamines were shown to exhibit potency against Gram-positive and -negative bacteria des
116 ve inhibitor, CCG258747, which has nanomolar potency against GRK2 and excellent selectivity over othe
120 Compound 5 g shows low nanomolar inhibitory potency against HDAC6 and a selectivity of approximately
121 omolar concentrations and displays excellent potency against hepatitis B virus (HBV) and varicella-zo
122 type-specific immune responses with limited potency against heterologous viral strains and genotypes
125 pounds show single-digit nanomolar antiviral potencies against HIV vectors that carry wild-type (WT)
127 Several ProTide compounds showed substantial potency against HIV-1 at low micromolar range while the
129 lecule HIV capsid inhibitor with exceptional potency against HIV-2 and all major HIV-1 types, includi
133 Although both compounds display similar potencies against human topoisomerase IIalpha and IIbeta
136 ry carbon atom, with up to 40-fold increased potency against human class I HDACs (e.g., JT86, IC(50)
139 abrogating the previously reported antiviral potency against human immunodeficiency virus (HIV-1).
140 3b would preserve transport selectivity and potency against human tumor cells, 3b regioisomers with
142 zed pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNas
143 5-substituted analogs exhibit low micromolar potency against in vitro cultures of drug-resistant and
144 ning only a salicylic acid showed inhibitory potency against IN, none of the compounds containing onl
145 up (e.g. 5-13) showed significant inhibitory potency against IN, while the presence of either salicyl
146 ion of an emerging lead compound, displaying potency against intracellular bacteria in the low microm
149 erating compound E67-2) has no effect on the potency against KIAA1718 but, unexpectedly, lost inhibit
151 ted extraordinary neutralization breadth and potency against large panels of cross-clade pseudoviruse
152 , a first generation lead with low nanomolar potency against life MeV and attractive physical propert
153 gesting that neratinib possessed therapeutic potency against liver fibrosis and the potential for app
154 igands demonstrated significant antiandrogen potency against LNCaP and Enzalutamide-resistant prostat
156 ion with front-line antibiotics enhanced the potency against M. tuberculosis by more than 100-fold, t
159 ear whether these antibodies exhibit similar potency against mature dendritic cell (mDC)-mediated HIV
160 g a (14)C-lactate transport assay, and their potency against MCT1-expressing human tumor cells was es
162 These reverse amides also exhibited less potency against monoamine oxidase (MAO) enzymes and thus
164 drophobic surface, providing a basis for its potency against MRSA known to deploy positively charged
165 uinolone-class compounds that have increased potency against Mtb and the ability to overcome resistan
167 of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compr
168 f these taxoids exhibited exceptionally high potency against multidrug-resistant cell lines, and seve
169 C220, KW-2449, sorafenib, and sunitinib) for potency against mutant and wild-type FLT3, as well as fo
171 e effect in patients despite displaying poor potency against Mycobacterium tuberculosis (Mtb) in vitr
172 2-carboxamide analog (1), had low micromolar potency against Mycobacterium tuberculosis (Mtb), high m
173 This analogue exhibited moderate inhibitory potency against Mycobacterium tuberculosis thymidylate k
174 one with improved in vitro and intracellular potency against Mycobacterium tuberculosis, including mu
177 f protoxin II-NHCH3, a molecule with greater potency against Nav1.7 channels (IC50=42 pM) than the or
178 ctive metabolite of 1, has retained in vitro potency against newly emerging antifolate-resistant mala
181 PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the
183 These compounds were assessed for their potency against P-gp and another transporter (MRP1), for
186 was to identify indolequinones with improved potency against pancreatic cancer and to define their me
188 Several new PIs exhibit nanomolar antiviral potencies against patient-derived wild-type viruses from
190 ty in rats, dogs, and monkeys while the high potency against PDE5 and desirable selectivity versus ot
191 Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the i
192 ounds, 7 and 8 showed the highest inhibitory potency against Pf enoyl-ACP-reductase (PfFabI), followe
193 the basis for developing novel PIs with high potency against PI-resistant HIV-1 variants with a high
194 properties and PK parameters, low nanomolar potency against PI3Kalpha and mTOR, and excellent inhibi
196 We sought to identify compounds with higher potency against Plasmodium DHODH while showing greater s
197 ances over azithromycin in vitro in terms of potency against Plasmodium falciparum (over 100-fold) an
198 e (23) analogues exhibited improved in vitro potency against Plasmodium falciparum compared to the pa
201 , transition state analogs that exhibit high potency against PNP in the malaria parasite Plasmodium f
202 alogues with improved antibacterial in vitro potency against polymyxin resistant recent clinical isol
204 d that possesses increased cytotoxicological potency against prokaryotic cells compared to eukaryotic
205 ) = 58 muM), which has reasonable inhibition potency against Pseudomonas aeruginosa TMK (PaTMK), was
206 o)benzoic acid (27), showing a submicromolar potency against purified CK2alpha (IC(50) = 0.6 muM).
207 e rounds of optimization to improve compound potency against purified enzyme and intracellular Plasmo
209 plasmin in the subnanomolar range, and their potency against related trypsin-like serine proteases in
210 ately improved ( approximately 2- to 4-fold) potencies against replicating Mycobacterium tuberculosis
213 ci (VRE), and fluoroquinolones with improved potency against respiratory pathogens and multidrug-resi
214 y reported; however, the greater decrease in potency against rlDHFR compared to pcDHFR and tgDHFR res
215 1 RT in the micromolar range while retaining potency against RT variants carrying one of three major
216 nds studied, 46a,b showed not only very good potency against RXRalpha (K(i) = 6 nM) but was also foun
217 n of natural products that display nanomolar potency against select isoforms of eukaryotic voltage-ga
221 revir showed submicromolar-to-low-micromolar potency against several recently circulating neurotropic
223 ells in monolayers, 033-F had notably weaker potency against spheroids despite potency levels of MMAE
224 in-based inhibitors with 9-18-fold increased potency against Staphylococcus aureus (Sa) and Bacillus
225 rotein kinase inhibitors that show nanomolar potency against T. brucei bloodstream forms, Leishmania
226 lead compound, 17b, that exhibited nanomolar potency against T. brucei with excellent selectivity for
228 diaminopyrimidine-based inhibitors with good potency against T790M-containing mutants of EGFR, high s
230 effective compound, 22 (MN-64), showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and
231 cidal activity was developed on the basis of potency against TbcatB and various calculated physical p
234 yrosine kinase inhibitors with low nanomolar potencies against the members of the VEGFR and PDGFR kin
236 ounds from this series demonstrated in vitro potency against the 3D7 and Dd2 strains of P. falciparum
237 high bioavailability and its nanomolar-range potency against the antiangiogenic receptor tyrosine kin
238 8b, and 11b showed good in vitro inhibition potency against the CAs IX and XII, with K(I) values in
239 lular calcium mobilization and a much higher potency against the chemerin(149-157) nonapeptide-induce
240 ts have shown a 40-fold and 200-fold loss in potency against the CRFR1 H199V and M276I mutant recepto
241 ized compounds, 22 showed excellent in vitro potency against the cultured parasites (W2 IC(50) = 13 n
242 tifolate, trimethoprim, because of a lack of potency against the dihydrofolate reductase enzyme.
243 refore, the retained and improved inhibitory potency against the drug-resistant variants A156T, D168V
245 taxoids exhibited virtually no difference in potency against the drug-sensitive and drug-resistant ce
247 , have demonstrated profound selectivity and potency against the FLT3 target, and are currently being
248 based on paroxetine, demonstrates increased potency against the GRK2 subfamily and favorable pharmac
254 on of inhibitors with significantly improved potency against the key resistant variants and with incr
255 he optimized compounds display low nanomolar potency against the mast cell target and several hundred
256 re were prepared that possessed subnanomolar potency against the NS3 protease in a subgenomic replico
257 pectrum antimicrobial activity, and enhanced potency against the opportunistic human pathogen Acineto
258 revealed that an inhibitor with insufficient potency against the p110beta isoform was less effective
259 ies of noncovalent inhibitors with nanomolar potency against the papain-like protease (PLpro) from th
261 yclic inhibitors displayed 20-50-fold higher potency against the PDF active site (K(I) as low as 70 p
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
273 ynergistic effect and significantly enhanced potency against three esophageal adenocarcinoma cell lin
274 hienopyrimidinone derivatives with nanomolar potency against TrmD in vitro and discovered a novel act
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
280 s analogs with 3~8-fold and 2~4-fold greater potency against vancomycin resistant Enterococcus faecal
283 ainst HIV strains with wild-type RT but lose potency against variants with single Y181C and double K1
284 le round replication assay and have improved potency against vectors harboring the major forms of dru
285 The molecule was evaluated both in vitro for potency against VEGF and in ocular VEGF-driven efficacy
286 scovery of second generation inhibitors with potency against viral strains bearing drug resistant IN
287 ough these prototype inhibitors have similar potencies against wild-type c-Met (K(i) = 6-7 nM), signi
290 Such adaptations appear to be critical for potency against wild-type and a wide range of drug-resis
291 cussed, focusing on optimization of cellular potency against wild-type and drug resistant parasites a
292 on of 8e (MK-4965), which has high levels of potency against wild-type and key mutant viruses, excell
294 critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and know
298 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