ライフサイエンスコーパス: potent inhibitor

1 fen has only a marginal effect and is a less potent inhibitor.

2 sed angiotensin II receptor antagonist, as a potent inhibitor.

3 tructure of E. coli LpxA in a complex with a potent inhibitor.

4 e features can enable the rational design of potent inhibitors.

5 l structures, which led to several extremely potent inhibitors.

6 date the inhibitory mechanisms of a group of potent inhibitors.

7 Therefore, there is a need for further potent inhibitors.

8 ophenyl derivatives 3i proved to be the most potent inhibitors.

9 in, and is capable of binding substrates and potent inhibitors.

10 ic target for diabetes and cancer but has no potent inhibitors.

11 rs, it is necessary to develop selective and potent inhibitors.

12 ric sites and the way forward to design more-potent inhibitors.

13 tivity relationships led to the discovery of potent inhibitors 10 and chemical probe VH298, with diss

14 12431) or S (10r, PSB-12553) yielded equally potent inhibitors (10q, 9.20 nM; 10r, 9.50 nM).

15 focused set of compounds that revealed three potent inhibitors (19a, 19b, and 20a) with remarkably lo

16 ls' broncho-alveolar lavage fluid was a less potent inhibitor (51% [23-66%] of inhibition), whereas n

17 EBOV GP and uncovered evidence that the most potent inhibitors act through multiple mechanisms.

18 y derived molecule called carmaphycin B is a potent inhibitor against both the asexual and sexual blo

19 l acetamide, has been identified as a novel, potent inhibitor against human 11beta-hydroxysteroid deh

20 ylamino]-thiazol-5-yl}phenyl)urea (10a) as a potent inhibitor against unactivated and activated c-KIT

21 for the rational design of specific and more potent inhibitors against activated GLI3 with a special

22 and cytosolic isozymes, identified nanomolar-potent inhibitors against both classes and several compo

23 The study identified several low nanomolar potent inhibitors against CA IX, with lipophilicities sp

24 nal heptad repeat (NHR) of HIV-1 gp41 can be potent inhibitors against viral entry when presented in

25 The two more potent inhibitors also suppress slow cooperative unfoldi

26 the Amazon rain forest, was identified as a potent inhibitor and reducer of both beta-amyloid fibril

27 mia (FA) factors active in the S/G2 phase as potent inhibitors and regulators of L1 activity.

28 ludes lipid substrates for enzymatic assays, potent inhibitors, and chemical probes to detect, track,

29 As only a few potent inhibitors are known, new compounds based on a 4-

30 the development of drug candidates that are potent inhibitors, but ineffective at treating the disea

31 The most potent inhibitor (C31) bound CypD with high affinity and

32 cribe a detailed characterization of a known potent inhibitor containing a 9H-pyrimido[4,5-b]indole s

33 e SET8-NQO1/TRXR1 axis with its specific and potent inhibitors could lead to promising host-directed

34 exemplifies as a cautionary tale how a more potent inhibitor does not necessarily generate more pote

35 t gene encoding the Notch effector Hey2 as a potent inhibitor for Schwann cell differentiation.

36 o the identification of LEI-301, a nanomolar potent inhibitor for the PLAAT family members.

37 id toward the structure-based drug design of potent inhibitors for AC, providing the detailed mechani

38 ber of Angiomotin family proteins, which are potent inhibitors for the Hippo pathway effector YAP.

39 y disrupted complex formation, with the most potent inhibitor having an IC(50) of 5 mum.

40 r the development of a novel class of highly potent inhibitors having a sulfamide zinc-binding motif.

41 efforts have led to the discovery of several potent inhibitors; however, so far no highly selective t

42 testinal Caco-2 cells with GT being the most potent inhibitor (IC(50) : 0.077 mg/mL), followed by OT

43 The most potent inhibitors (IC50 </= 50 nM) significantly decreas

44 tetrazole-containing derivatives were highly potent inhibitors in both assays, with complete inhibiti

45 In particular, compounds 13 and 14 are very potent inhibitors in that they demonstrated the lowest I

46 er exhibit poor amyloid formation and act as potent inhibitors in trans of simple polyQ peptide aggre

47 assays also showed that the scaffold of this potent inhibitor, in contrast to one of our previously r

48 The most potent inhibitors induced demethylation of CDKN2A promot

49 The most potent inhibitor is competitive against histone substrat

50 The most potent inhibitor is well-structured in water and success

51 ne (isopentane), the analogous alkane of the potent inhibitor isoamyl alcohol (isopentanol), did not.

52 linker is the optimal and produces the most potent inhibitor (K(i,app) = 130 +/- 40 pM) for NTMT1 to

53 oeuromycin, which is revealed to be the most potent inhibitor (KD 13 nM for Bacteroides xylanisolvens

54 zidobutyl)carboxamide moiety, proved to be a potent inhibitor (Ki = 8.2 nM) of the Thermotoga maritim

55 Fluorosulfate was identified as a potent inhibitor of (99m)TcO4(-) uptake via hNIS in vitr

56 tly confirmed that quercetin is reasonably a potent inhibitor of 3CLpro.

57 50 MPa/5 min and 650 MPa/5 min) was the most potent inhibitor of AGEs in the BSA-GLU model (6.52 mg/m

58 sistance can be surmounted by indomethacin a potent inhibitor of AKR1C3.

59 2,5-dihydroxybenzoic acid was found to be a potent inhibitor of alpha-amylase with an IC50 value of

60 action assay, was less cytotoxic, and a more potent inhibitor of alpha-smooth muscle actin protein ex

61 c analyses clearly show that vitamin K1 is a potent inhibitor of ALR2 and this inhibition is primaril

62 PEDF (pigment epithelium-derived factor), a potent inhibitor of angiogenesis and known regulator of

63 to a cell-autonomous function of miR-26 as a potent inhibitor of APC differentiation.

64 do)benzamide (6ad) proved to be an extremely potent inhibitor of APN activity in vitro, selective aga

65 ive pGC-A activators, that CRRL269 is a more potent inhibitor of apoptosis in renal cells and induced

66 ompound known to be toxic to Plasmodium is a potent inhibitor of apPOL, suggesting that apPOL is a vi

67 taining 0.006% SC-435, a minimally absorbed, potent inhibitor of ASBT, providing, on average, 11 mg/k

68 preserved in ESCs treated with Hesperadin, a potent inhibitor of Aurora B/C kinases.

69 assays showed that c-CA, and not t-CA, is a potent inhibitor of auxin efflux.

70 Ileal Fgf15 is a potent inhibitor of BA synthesis.

71 We have recently developed a novel potent inhibitor of BET proteins, 1, which exerts a stro

72 V) minor structural proteins VP2/3 that is a potent inhibitor of BKV infection with no observable cel

73 Sclerostin has been proposed as a potent inhibitor of bone formation.

74 receptor, compound 5, and alendronic acid, a potent inhibitor of bone resorption, optimally linked th

75 ndronate (ALN) is an aminobisphosphonate and potent inhibitor of bone resorption.

76 ify the small molecule Ailanthone (AIL) as a potent inhibitor of both full-length AR (AR-FL) and cons

77 Overall, the hC3Nb3 nanobody represents a potent inhibitor of both the alternative pathway and the

78 Proanthocyanidin B2 was also a potent inhibitor of brain inflammation as shown by reduc

79 its payload intracellularly, and is a highly potent inhibitor of brain, breast, ovarian, and pancreat

80 n-1-one (callunene) from heather nectar as a potent inhibitor of C. bombi.

81 derivatives, compound 21b, was found to be a potent inhibitor of C. difficile spore germination and p

82 at helenalin acetate is a significantly more potent inhibitor of C/EBPbeta than of NF-kappaB.

83 Compound 55 was identified as a potent inhibitor of CA XII ( K(i) = 0.56 nM) and was inv

84 verted into inorganic pyrophosphate (PPi), a potent inhibitor of calcification.

85 cturally related to CQ but is a 14-fold more potent inhibitor of cell proliferation.

86 (ES9), a novel mitochondrial uncoupler, is a potent inhibitor of clathrin-mediated endocytosis (CME)

87 ally led to the discovery of compound 21b, a potent inhibitor of Clk1 and -4 (IC50 = 7 and 2.3 nM, re

88 by a thick capsular polysaccharide that is a potent inhibitor of complement deposition via the altern

89 ical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CL(pro) with suitable pharmac

90 We previously identified 666-15 as a potent inhibitor of CREB with efficacious anti-cancer ac

91 Unfortunately, the compound is a potent inhibitor of cytochrome P450 enzymes, probably du

92 rans-4,4'-dihydroxystilbene), that acts as a potent inhibitor of DNA replication.

93 ith the 2-thiophenyl compound 2p as the most potent inhibitor of eqBChE (KC = 14.3 nM) and also of hB

94 lbutyrate (4-PBA), a chemical chaperon and a potent inhibitor of ER stress, significantly reduced ske

95 om the plant Phyllanthus engleri as the most potent inhibitor of EWS-FLI1 induced luciferase reporter

96 Thus, MSNBA is a selective and potent inhibitor of fructose transport via GLUT5, and th

97 rphane derivative Glupin was identified as a potent inhibitor of glucose uptake by selectively target

98 We demonstrate that RgA is a potent inhibitor of GLUT1 as well as GLUT3 and GLUT4, wi

99 honomethylpentanedioic acid (1, 2-PMPA) is a potent inhibitor of glutamate carboxypeptidase II which

100 ion to methylarsenite (MAs(III)), which is a potent inhibitor of glycerol-3-phosphate dehydrogenase.

101 dated decitabine, an FDA-approved drug, as a potent inhibitor of growth in pancreatic cancer cells an

102 lly, we found that treating CHO cells with a potent inhibitor of GSL biosynthesis increases the sialy

103 ano-2,2'-stilbenedisulfonic acid (DIDS) as a potent inhibitor of HCMV replication.

104 In particular, the Rh complex was a potent inhibitor of HDAC6 over HDAC1 and HDAC8.

105 ing transforming growth factor (TGF)-beta, a potent inhibitor of hepatocyte proliferation.

106 22 is facilitated where it functions as a bi-potent inhibitor of HIF-1alpha and TGF-beta activities,

107 tein in the Fe(II)-NO and Fe(III) forms is a potent inhibitor of HnoK.

108 Compound 24 is a nanomolar potent inhibitor of human 17beta-HSD2 (IC(50) of 6.1 nM)

109 inhibitory assays demonstrated that it was a potent inhibitor of human cathepsins B, K, and L ( Ki =

110 2, a natural phosphonic acid, functions as a potent inhibitor of human enolase.

111 Our data support that mTORi is a potent inhibitor of humoral immunity through suppression

112 arin derivative, 4-methylumbelliferone, as a potent inhibitor of hyaluronan biosynthesis, due in part

113 d gene target assays identified MLN4924 as a potent inhibitor of intestinal epithelial NF-kappaB.

114 rate, a prominent bacterial metabolite, as a potent inhibitor of intestinal stem/progenitor prolifera

115 olipase C (PC-PLC) of L. monocytogenes, is a potent inhibitor of intra- and extracellular LLO activit

116 ive E2f-mediated transactivation of Socs3, a potent inhibitor of Jak2 signaling, in cycling HSCs.

117 estigation of GW296115 has confirmed it as a potent inhibitor of kinases including BRSK1 and BRSK2 th

118 Unlike KCNE4S, KCNE4L was a potent inhibitor of Kv4.2 and Kv4.3; co-expression of cy

119 for multi-drug resistant tuberculosis, is a potent inhibitor of Leishmania donovani both in vitro an

120 These results suggest that vitamin K1 is a potent inhibitor of lens aldose reductase enzyme and we

121 ken together, our results identify 5-HT as a potent inhibitor of lipid peroxidation and offer a diffe

122 inhibitor than gadolinium and a particularly potent inhibitor of mechano-gated Piezo channels, reduce

123 CD59 is a potent inhibitor of membrane attack complex that mediate

124 Minocycline, a potent inhibitor of microglia activation, successfully p

125 n is known to bind to alpha-tubulin and is a potent inhibitor of microtubule polymerization.

126 istration of cipemastat, an orally available potent inhibitor of MMP-7, could reduce pulmonary cavita

127 rved mitochondria identified ER-000444793, a potent inhibitor of mPTP opening.

128 holate siderophore released by E. coli, is a potent inhibitor of myeloperoxidase (MPO), a bactericida

129 that enhanced expression of A20 (TNFAIP3), a potent inhibitor of NF-kappaB.

130 d 9 (IC50 = 15.6 muM) was assessed as a more potent inhibitor of NMDAR-induced currents than the know

131 Tea has been shown to be a potent inhibitor of nonheme iron absorption, but it rema

132 asvir is a direct-acting antiviral agent and potent inhibitor of NS5A, which is involved in replicati

133 asvir is a direct-acting antiviral agent and potent inhibitor of NS5A, which is involved in replicati

134 40, a common azo dye excipient and a potent inhibitor of OATP2B1, decreased the plasma level

135 development of SBD, zoledronic acid (Zol), a potent inhibitor of osteoclast activity/osteoclastogenes

136 AND First, we identified spironolactone as a potent inhibitor of Panx1 in an unbiased small molecule

137 9 is a promiscuous tankyrase inhibitor and a potent inhibitor of PARP1 in vitro and in cells, whereas

138 Avibactam is a potent inhibitor of PenA1 (apparent inhibitory constant

139 QAW039 was also a potent inhibitor of PGD2-induced cytokine release in hum

140 ads to intoxication by 6-phosphogluconate, a potent inhibitor of phosphoglucose isomerase (PGI).

141 of licorice, which contains glycyrrhizin (a potent inhibitor of placental 11beta-hydroxysteroid dehy

142 e results suggest HC-HA/PTX3 is a non-toxic, potent inhibitor of proliferation and EMT of RPE in vitr

143 ed the MPT antagonist tigecycline (TIG) as a potent inhibitor of Rb/p53-deficient tumor cell prolifer

144 e have identified an inhibitor of ACSLs as a potent inhibitor of RPE65 that competes with the atRE su

145 ibosyltransferases, was shown to be the most potent inhibitor of Scabin.

146 Here we show that xanthurenic acid is a potent inhibitor of sepiapterin reductase (SPR), the fin

147 eoxyriboside triphosphate, in vivo creates a potent inhibitor of several human DNA polymerases that c

148 Here, we describe the discovery of the most potent inhibitor of sirtuin 5 (SIRT5) reported to date.

149 n assessment of tungstate as a selective and potent inhibitor of SRM.

150 These results show that VPA is a potent inhibitor of STAT3 phosphorylation and demonstrat

151 At 200-300 nM concentrations, IB is a potent inhibitor of STAT5 through liberation of endogeno

152 Zinc pyrithione is the most potent inhibitor of sulfidogenesis that we identified, a

153 zolium compound YM155, first discovered as a potent inhibitor of Survivin, effectively kills many car

154 form the mitotic checkpoint complex (MCC), a potent inhibitor of the anaphase-promoting complex (APC/

155 tion of fragment hit 5b to 13-d as a biased, potent inhibitor of the BRD of the BRPFs with excellent

156 NA metabolism in cells, thereby serving as a potent inhibitor of the gene expression pathway.

157 -2'-spirooxetane uridine triphosphate (8), a potent inhibitor of the HCV NS5B polymerase.

158 ibrary, we identified that UNC0638, a highly potent inhibitor of the histone methyltransferases G9a a

159 y activity toward serine proteases but was a potent inhibitor of the major secreted cathepsin L cyste

160 fter LPS treatment, whereas treatment with a potent inhibitor of the mitochondrial pyruvate carrier (

161 Further studies revealed SLAMF7 to be a potent inhibitor of the monocyte-derived proinflammatory

162 It is a potent inhibitor of the mRNA decapping scavenger enzyme

163 A20 is a potent inhibitor of the NF-kappaB signaling pathway.

164 d it also activates TRPM8 and functions as a potent inhibitor of the noxious chemical receptor TRPA1.

165 MDM2, an E3 ubiquitin ligase, is a potent inhibitor of the p53 tumor suppressor and is elev

166 tion to Wee1 and Wee2, MK-1775 is an equally potent inhibitor of the polo-like kinase PLK1.

167 This compound is a potent inhibitor of the sarcoplasmic-endoplasmic reticul

168 ng cells (IC50 = 230 nM), providing the most potent inhibitor of the sonic hedgehog/patched interacti

169 hydroid isolated from Garveia annulata, is a potent inhibitor of the tryptophan catabolizing enzyme i

170 Compound 18 represents the most potent inhibitor of the WDR5-MLL interaction reported to

171 We have designed the first potent inhibitor of this enzyme by mimicking its natural

172 The most potent inhibitor of this work, BH267.meta, killed cultur

173 he Kallithea virus-encoded protein gp83 as a potent inhibitor of Toll signalling, suggesting that Tol

174 Here we show that active Gtr1/2 is a potent inhibitor of TORC1-body formation, but cells miss

175 Tuberous sclerosis complex (TSC) is a potent inhibitor of TORC1.

176 2][PF6] (AubipyOMe) was found to be the most potent inhibitor of TRAP5a and 5b activity reported to d

177 Entrectinib is a potent inhibitor of tropomyosin receptor kinase (TRK) A,

178 e Icat and EA-induced cytotoxicity whereas a potent inhibitor of TRPC4/C1 channels (Pico145) strongly

179 osertib contains approximately 5% ON01500, a potent inhibitor of tubulin polymerization.

180 functions of basophils and identify NMB as a potent inhibitor of type 2 inflammation.

181 G15, such as human ISG15, stabilize USP18, a potent inhibitor of type I interferon (IFN)-I.

182 Cediranib (AZD2171) is a potent inhibitor of tyrosine kinase activity associated

183 onyl hydroxamate-based compound LPC-058 is a potent inhibitor of UDP-3-O-(R-3-hydroxymyristoyl)-N-ace

184 Matrix Gla protein (MGP) is a potent inhibitor of vascular calcification.

185 Purpose Cabozantinib is an oral potent inhibitor of vascular endothelial growth factor r

186 Although recombinant EC1 is a potent inhibitor of viral infection, there is no molecul

187 ly, we proved that deleting the Sost gene (a potent inhibitor of WNT signaling) or blocking sclerosti

188 hese results demonstrate that HNPs1-3 may be potent inhibitors of ADAMTS13 activity, likely by bindin

189 racts of Black Prince tomatoes were the most potent inhibitors of AGEs in BSA-GLU (7.20mg/mL) and BSA

190 These prefibrillar CysC oligomers were potent inhibitors of aggregation of the Alzheimer's-rela

191 nates found in brown seaweeds appeared to be potent inhibitors of alpha-amylase activity with an IC50

192 multiple antioxidant activities and are also potent inhibitors of alpha-amylase and alpha-glucosidase

193 be moderate inhibitors of alpha-amylase, but potent inhibitors of alpha-glucosidase, showing low-micr

194 These compounds were previously shown to be potent inhibitors of BMP signaling by binding to the BMP

195 ropyran-based compounds such as 6 and 21 are potent inhibitors of both DNA gyrase and topoisomerase I

196 Tolcapone and entacapone are potent inhibitors of catechol-O-methyl transferase (COMT

197 herwise have minimal effects in cells become potent inhibitors of cellular signaling.

198 ery approach, which resulted in novel highly potent inhibitors of ChoKalpha.

199 TDZ derivatives (HETDZ and 3FMTDZ) are very potent inhibitors of CKX and are promising candidates fo

200 Such potent inhibitors of class I HDACs may show benefits in

201 n the identification and characterization of potent inhibitors of CysM, a critical enzyme in cysteine

202 to the discovery of soluble, selective, and potent inhibitors of DGAT1.

203 alogues synthesized in this study are highly potent inhibitors of DHODH in an enzymatic assay, while

204 of heart failure and atrial arrhythmia, are potent inhibitors of DNA double-strand break (DSB) repai

205 lted in quinazoline-quinoline derivatives as potent inhibitors of DNMT3A and DNMT1, some showing cert

206 mM), which makes this series among the more potent inhibitors of dynamin and CME yet reported.

207 Altogether, 14 new potent inhibitors of E. coli ClpP were identified.

208 cid and derivatives thereof were found to be potent inhibitors of endonuclease.

209 ethyl) phenol (compound 4), were shown to be potent inhibitors of ERCC1-XPF activity in vitro.

210 tial, we targeted our efforts at identifying potent inhibitors of FXIa with a focus on discovering an

211 All ARBs were found to be potent inhibitors of G protein activation at the AT(1)R.

212 nd GAC with comparable activities, were less potent inhibitors of GAB, and were moderately selective

213 ningitidis Cas9 (NmeCas9) and can be used as potent inhibitors of genome editing by this system in hu

214 that both YM-254890 and FR900359 are highly potent inhibitors of Gq signalling, with FR900359 being

215 mize a series of salicylamide derivatives as potent inhibitors of HAdV infection.

216 nserved glycine residues (G335 and G338) are potent inhibitors of helical extension and helix-helix i

217 The prodrugs were potent inhibitors of HIV-1/2 in cultures of infected CEM

218 xploited in the design of selective and more potent inhibitors of HpalphaCA that may lead to novel an

219 around MCV lesions suggests the presence of potent inhibitors of human antiviral immunity and inflam

220 BTK-targeting drugs are potent inhibitors of IgE-dependent histamine release in

221 This work identifies TGF-beta1 and BMP-2 as potent inhibitors of IL-34 expression in RA synovial fib

222 5H-imidazo[5,1-a]isoindoles are described as potent inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1

223 ypromine (TCPA) derivatives (14a-k, 15, 16), potent inhibitors of KDM1A.

224 Compounds 34 and 39 are also potent inhibitors of KDM5C (JARID1C) (RFMS IC50 = 100-12

225 e food samples (T. terrestris, chickpea) are potent inhibitors of key enzymes in digestion of carbohy

226 interaction identified 4-Aminoquinolines as potent inhibitors of MAGE-A11 that show selective cytoto

227 enabled the discovery of the first series of potent inhibitors of mitochondrial branched-chain aminot

228 l products harzianopyridone and atpenins are potent inhibitors of mitochondrial complex II.

229 Seed proteins include potent inhibitors of MMP-9, particularly low molecular m

230 nzisothiazolinone (BTZ) derivatives that are potent inhibitors of monoacylglycerol lipase (MGL), the

231 in use in humans, digoxin and digitoxin, are potent inhibitors of multiple adenovirus species.

232 ane 1 and indoline-5-sulfonamides 2 and 3 as potent inhibitors of mycobacterial growth.

233 To identify more potent inhibitors of NAPE-PLD, here we used a quenched f

234 gnificance, these compounds were found to be potent inhibitors of organic cation transporter 2 (OCT2)

235 press the transcription factor Foxp3 and are potent inhibitors of osteoclasts.

236 tors do not inhibit serine proteases but are potent inhibitors of parasite cathepsins L and host lyso

237 laparib, rucaparib, and talazoparib are more potent inhibitors of PARP1 but are less selective.

238 Using specific and potent inhibitors of Plasmodium PKG and CDPK4, we demons

239 All derivatives 1a-c were determined to be potent inhibitors of protein phosphatase-1 with similar

240 of the V(H)Hs, V2A11, V8E6, and V2G10, were potent inhibitors of RTA in vitro and protected Vero cel

241 Here we describe three potent inhibitors of SauCas9 that we name AcrIIA13, AcrI

242 es of new benzohydroxamates were prepared as potent inhibitors of Schistosoma mansoni histone deacety

243 The most potent inhibitors of SGLT2 (IC50 = 9-23 nM) were conside

244 We have discovered that Egr2 and 3 are potent inhibitors of T-bet function in CD4 and CD8 effec

245 lic peptides produced by cyanobacteria, were potent inhibitors of TAFIa with IC50 values as low as 1.

246 ydroxamic acid-containing analogues that are potent inhibitors of the APN homologue from the malarial

247 tment of this highly aggressive disease with potent inhibitors of the BCR-ABL kinase such as dasatini

248 lurides bearing sulfonamide as selective and potent inhibitors of the beta-class carbonic anhydrase (

249 Several compounds were found to be potent inhibitors of the enzyme in biochemical and cell-

250 te the generation of pArg mimetics as highly potent inhibitors of the enzymes that catalyze arginine

251 urthermore, the compounds are reversible and potent inhibitors of the extracellular production of sup

252 inhibitors of metalloproteinases (TIMPs) are potent inhibitors of the many matrixins (MMPs), except t

253 isochromanone core of the ajudazols, highly potent inhibitors of the mitochondrial respiratory chain

254 mical determination of the ajudazols, highly potent inhibitors of the mitochondrial respiratory chain

255 Cardiotonic steroids (CTSs) are specific and potent inhibitors of the Na(+),K(+)-ATPase, with highest

256 demonstrate the utility of these scaffolds, potent inhibitors of the serine/threonine-protein kinase

257 In contrast, potent inhibitors of the sonic hedgehog/patched interact

258 ine-2,4-dione as a useful scaffold to obtain potent inhibitors of the tumor-associated human carbonic

259 major part of these new derivatives acted as potent inhibitors of the tumor-associated isoform hCA XI

260 phosphinic pseudotripeptides can constitute potent inhibitors of this group of enzymes.

261 nase inhibitors (BKIs) have been shown to be potent inhibitors of Toxoplasma gondii calcium-dependent

262 Moreover, the CCl2-analogues were potent inhibitors of translation in rabbit reticulocyte

263 ity and tubulin inhibition assays and led to potent inhibitors of tubulin polymerization.

264 diffusible signal factors (DSFs), are highly potent inhibitors of virulence functions.

265 cts of the mode of action and binding of two potent inhibitors of VMAT2: reserpine binds the cytoplas

266 e report details behind the discovery of new potent inhibitors of wild type and resistant mutant endo

267 evels of the universal methyl donor SAM were potent inhibitors of Wnt signaling and of Wnt-induced di

268 tetracycline family of antibiotics were more potent inhibitors of Zika virus infection than the prote

269 The potent inhibitor oleoyl-d-lysine (33) is also resistant

270 iquitination of RACK1 and identified a novel potent inhibitor providing a balance between growth inhi

271 rget CRAF, yet kinase-selective and cellular potent inhibitors remain challenging to identify.

272 cture of Eis in complex with one of the most potent inhibitors revealed that the inhibitor bound Eis

273 of LSD1 inactivation by a selective and more potent inhibitor, RN-1, in a sickle cell disease (SCD) m

274 oresis resulted in the identification of two potent inhibitors (SM09 and SM15) that mask the critical

275 27 was a weak DNA ligand, analog 5, the most potent inhibitor, strongly interacted with DNA.

276 24 and 25 muM respectively (similar range as potent inhibitors such as diclofenac and indomethacin in

277 utyl)-N'-(2-methoxyethyl)guanidine (8a) is a potent inhibitor targeting the hDDAH-1 active site (K(i)

278 nd designated CSL040, was found to be a more potent inhibitor than all other truncation variants test

279 D-ring derivatives were less potent inhibitors than lead compound 1, whereas steroida

280 nservation, whereas toxic hydroxylamine is a potent inhibitor that needs to be rapidly removed.

281 These studies led to the identification of a potent inhibitor that showed selectivity for AtIPCS2 ove

282 2,4-pyridinedicarboxylic acid (2,4-PDCA) are potent inhibitors, they exhibit limited selectivity.

283 ctures reveal routes to rapidly develop more potent inhibitors through merging of covalent and non-co

284 ) value of 1.6 +/- 0.3 nM, which is the most potent inhibitor to date.

285 low Km for ATP and therefore requires a very potent inhibitor to effectively block the kinase activit

286 hlights the opportunity to develop more cell-potent inhibitors to elucidate the function of NTMTs in

287 In inhibition tests, the most potent inhibitor was found to be ascorbic acid followed

288 The most potent inhibitor was further characterized for Gtf bindi

289 The most potent inhibitor was NFLP, which had a competitive (with

290 The most potent inhibitors were produced by replacements at C7, i

291 Among the most potent inhibitors were the 5'- O-[(phosphonomethyl)phosp

292 7 or PF-367) has been identified as a highly potent inhibitor, which is among the most selective anta

293 by 10-fold, affording LEI-401 as a nanomolar potent inhibitor with drug-like properties.

294 no)ethyl]benzamide hydrochloride is the most potent inhibitor with IC50 at 7.96 muM and selectivity i

295 s series leading to 4a (PF-06761281), a more potent inhibitor with suitable in vivo pharmacokinetic p

296 IC(50) = 257 nM), resulted in several highly potent inhibitors with IC(50) values lower than 20 nM fo

297 hyl)phosphonic acid] (15, 16) being the most potent inhibitors with K(i) values toward human CD73 of

298 ocycle at the 4 position of the phenyl ring, potent inhibitors with oral exposure were obtained.

299 Cocrystal structures of potent inhibitors with PvSHMT were solved at 2.6 A resol

300 initiated a program to design and synthesize potent inhibitors with selective activity against fungal