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1 (50 compounds) identified approximately 100 hits and four distinct chemotypes, the most promising of
4 e associated with PH-HFpEF, we developed a 2-hit PH-HFpEF model in rats with multiple features of met
5 ological activity in vitro, we identified 21 hit compounds which inhibited IMPalpha/beta1:C binding w
7 irtual screening campaign yielded a high 32% hit rate, identifying novel fragment-like and lead-like
8 brary of 5,195 small molecules identified 34 hit compounds that interact with the regulatory cyclic n
16 thiazole (1), which had been identified as a hit against Trypanosoma brucei, the causative agent of h
20 in, we report the optimization process for a hit compound that has emerged from a phenotypic screen r
24 ide evidence that maternal immune activation hits a key neurodevelopmental process, the excitatory-to
26 e than 100 compounds and revealed additional hits and temporal profiles in good correlation with repo
28 Herein, we describe the identification and hit-to-lead optimization of a novel class of tricyclic s
31 in cell cycle regulation, were identified as hits in four different RNAi screens and we therefore stu
34 cer activity in a functional reporter assay, hits were confirmed in cell culture, and an optimized Gl
35 These profiles allow teams to quickly assess hit series for desirable ADMET properties or suspected l
39 t our lead optimization of a benzoxazepinone hit from a DNA-encoded library and the discovery and pro
43 hologues computed from reciprocal best BLAST hits or OrthoMCL, and DAGchainer, and outputs an overvie
44 s faster than a popular artificial centering hit-and-run algorithm, enabling reliable and tractable s
46 creening of candidates returned 14 confirmed hits with activities in the nano- to low-micromolar rang
51 od is that the contribution of each database hit to the taxonomic assignment of the query sequence is
54 lowest common ancestors of multiple database hits for each query sequence, and further classification
55 tein target is a key component when defining hit-finding strategies or when prioritize among drug tar
56 applicable process for identifying degrader hits based on the serine/threonine kinase TANK-binding k
59 his hemisphere as a consequence of a "double-hit" phenomenon because of preexisting alterations in co
61 ll lymphoma, have been referred to as double-hit lymphomas (or triple-hit lymphomas if all 3 rearrang
62 slocation of MYC and BCL2, so-called "double-hit lymphoma," has been associated with a high risk of c
63 nd/or BCL6 rearrangements, so-called "double-hit" lymphomas (HGBL-DH), are aggressive lymphomas that
64 re no published prospective trials in double-hit lymphoma, however retrospective studies strongly sug
65 Surprisingly, under conditions of LPS double-hit an interference of a postulated alpha7nAChR - ferrop
66 ch to the evaluation and treatment of double-hit lymphoma, with an eye toward future clinical trials
73 algorithm is based on the provably efficient hit-and-run random walk and crucially uses a preprocessi
77 to be inactive in 50 or more assays, exhibit hit rates that are comparable to those of compounds test
78 gh-throughput screening paradigm facilitated hit identification, while structure-based design and mul
80 and early progenitor clones with the "first hit" mutation in APC that subsequently gave rise to both
82 astic leukemia (cALL) functioning as a first-hit mutation that initiates a clinically silent pre-leuk
88 els to generate in silico ADMET profiles for hit series to enable more complete characterizations of
94 l structure of caspase-7 bound to a fragment hit and a thorough kinetic characterization of a zymogen
96 e in lipophilic efficiency from the fragment hit, excellent kinase selectivity, and pharmacokinetic p
102 chment for an inputted list of genes (e.g., 'hits' from a screen) and search for additional genes wit
106 me-wide association studies revealed 28 GWAS hits in potential candidate genes likely to affect trait
108 s provide great supporting evidence for GWAS hits and important insights into the regulatory pathways
113 imization of high-throughput screening (HTS) hit 1 led to the identification of 3, which demonstrated
114 biochemical high-throughput screening (HTS) hits led to the discovery of a series of ligands that bi
116 a first screening experiment, we identified hit 13 as able to inhibit STAT5 phosphorylation and leuk
117 ry of 107 FDA-approved compounds to identify hits that prevented the age-dependent functional deterio
118 sults from the 2015 contest show an improved hit rate when compared to results from the 2014 contest.
119 NMR binding assays are routinely applied in hit finding and validation during early stages of drug d
122 rein, we describe optimization of an initial hit 2, resulting in identification of racemic-trans-(3-(
123 ationships from identification of an initial hit in a high-throughput screen through selection of taz
124 report the discovery of a promising initial hit compound targeting the Fanconi anemia ubiquitin-conj
125 ined the TAR binding affinity of the initial hit and displaced a Tat-derived peptide with an IC50 of
126 ther 70 compounds that comprised the initial hit chemotypes were subsequently sourced from the full C
128 from the SAR exploration around the initial hits, the optimization process focused on the improvemen
130 -cell RNA sequencing (RNA-seq) technology is hitting its stride and is beginning to be widely adopted
133 cused on validating endosome/Golgi-localized hits specific for STx2 and found that depletion of UNC50
135 t a concentration of 10 muM, there were many hits for JJC8-016, binding affinities in the range of it
136 ng the HSQC spectrum, and the top metabolite hits are then validated against the TOCSY-type experimen
138 y in a ligand-efficient manner, a micromolar hit identified from a screen of a Pfizer fragment librar
142 e Markov chain models that capture the multi-hit initiation-promotion-malignant-conversion hypothesis
144 We also searched for potential "multiple-hit" cases; one proband carried a rare AUTS2 variant in
146 ed on the thesis that a series of mutational hits (1st Hit) at the stem-cell level generates a clone
147 viewing LIP-associated autoimmunity as an n-hit model, we suggest a more quantitative view of lympho
150 cted VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC
152 Instruction compliance (R-hits minus NR-hits) was significantly related to negative coupling bet
156 fatal accidents, it did decrease the rate of hit and run accidents, suggesting that the policy reduce
158 cidation of the mechanism of action (MoA) of hits from these noisy high-throughput screens remain dif
163 stance mechanism of M. smegmatis against one hit, 3-bromo-N-(5-nitrothiazol-2-yl)-4-propoxybenzamide
164 a collection of beta-lactones, we found one hit with potent anti-mycobacterial and bactericidal acti
165 oic acid (WTA) inhibitors, we identified one hit, which was expanded through chemical synthesis into
166 proliferation of cancer cells and optimized hits for potency and selectivity, both in vitro and in c
167 stematic series of analogues of the original hit using a structure-based drug design strategy, which
168 present, per se or in association with other hits, a risk factor for developing psychotic-like sympto
173 T interaction domain identified one positive hit compound and two analogs of the hit with high cytoto
175 shunt that greatly minimizes false-positive hits, we identify mitoxantrone out of more than 600 clin
178 ositives by selectively identifying positive hits exclusively when a ligand at the binding site of in
181 obtained X-ray structures of the most potent hit (compound 19, IC50 = 2.9 muM) in complex with the en
183 en against porcupine revealed several potent hits that were confirmed to be Wnt pathway inhibitors in
184 ss this concern, here we developed a potent "hit" compound, VSP-51, which is a novel selective PPARga
185 al and approved drugs): 28% of the predicted hits were reported in literature as ligands of SULT1E1.
189 m a weakly potent, nonselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomai
194 of structure-based drug design enabled rapid hit to lead progression in a program to identify pan-iso
200 to PFI-3 from an initial fragment screening hit is described in detail, and additional analogues wit
201 sp(3) character of high-throughput screening hit 40 afforded a novel morpholinopyrimidone mGlu5 NAM s
202 ic inhibitors, the high-throughput screening hit anthranilic acid 4, the known benzofuran analogue 5,
203 d optimization, a 5 microM virtual screening hit was transformed to a series of very potent nanomolar
204 rcity of historical ADMET data for screening hits limits our understanding of early hit compounds.
205 SAR investigations around the screening hits provided a diverse set of potent agonists at 5-HT2C
206 more ring structures dominated the screening hits, including nitroaromatic compounds that induce subs
207 The molecular combination of these screening hits led to compound 22a (PF-543) with 2 orders of magni
209 e gastrointestinal C. muridarum, as a second hit, to transmucosally convert tubal repairing - initiat
210 dren with syndromic ASD and if mGluR "second hit" confers additional risk for ASD in 22q11.2 Deletion
211 fy additional genetic factors (i.e., "second hits") that may contribute to schizophrenia expression.
213 set of the offspring also received a second 'hit' of lipopolysaccharide (LPS), which simulates a bact
214 ed, such as excessive inflammation, a second-hit insult, or an imbalance between pro- and anti-inflam
216 discovery cohort, one genomewide significant hit located in phosphodiesterase 4D, cAMP-specif (PDE4D)
217 GWAS identified one genome-wide significant hit (Affymetrix id 1:64178756_C_T; P=1.36 x 10(-11)).
225 tabolites are emerging as promising starting hit compounds to modulate human targets, hence triggerin
226 In winter 2013/14 a succession of storms hit the UK leading to record rainfall and flooding in ma
227 ated with AF populations, with the strongest hits clustering on chromosome 4q25, close to the gene fo
229 Potency optimization of the sulfonamide hit compounds was undertaken as informed by docking stud
232 trol continuum, measuring interventions that hit clinically related targets, and leveraging technolog
234 nstantly encodes the visual information that hits the retina, leading to a stimulus-specific activati
237 s at EAAT1 compared to that displayed by the hit, it provided a detailed insight into structural requ
238 placement term can substantially improve the hit rates and ligand geometries from docking screens, al
239 ing design would have missed, increasing the hit frequency from the chemical library three-fold.
241 positive hit compound and two analogs of the hit with high cytotoxic, pro-apoptotic and anti-mitotic
248 s on transcriptional regulation such as the "hit-and-run" model and transcription bursting that could
256 mpound libraries identified more than thirty hits that increased MBNL1 expression greater than double
257 in adulthood: only mice exposed to all three hits showed deficits in this aspect of social behavior.
260 and structure-activity relationships through hit expansion guided by three-dimensional structures of
261 stability problem for PSCs and allow them to hit the market as a serious low-cost competitor to silic
265 i-randomly mutated Oryza sativa FNR, the top hit enabled a 60 % increase in NADPH-driven H2 productio
266 ning data, we focused our studies on the top hit from our screen, the lipid kinase phosphatidylinosit
275 egative pathway components and validated top hits using multiple signaling and differentiation assays
277 ferred to as double-hit lymphomas (or triple-hit lymphomas if all 3 rearrangements are present).
278 e) out of seven tested candidates ( 40% true hit rate) as direct inhibitors of VCP/p97 and ERAD.
279 the view of LIP-driven autoimmunity as a two hit model; however, not all cofactors have equal ability
283 /obliterative arteriopathy induced via a two-hit pathophysiological mechanism without hypoxia provide
287 LI): LPS-induced inflammatory injury and two-hit ALI caused by suboptimal mechanical ventilation and
288 These findings challenge the assumed two-hit model of Emu-Myc lymphoma and demonstrate a function
291 , we say that a set of k-mers is a universal hitting set (UHS) if every possible L-long sequence must
292 pers to use an ordering based on a universal hitting set or, if not possible, a randomized ordering,
294 ll, the generated models can support various hit identification tasks, including virtual screening, c
299 activated the default mode network, whereas hits in the picture memory test preferentially engaged t
300 t but also illustrated a unique way in which hits from orthogonal screening approaches complemented e
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