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 lfated trimer 24 (IC50 0.82 muM) as the most potent inhibitor.

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

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

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

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

8 a distal phenyl group proved to be the most potent inhibitors.

9 action differences between highly and weakly potent inhibitors.

10 natural amino acid residues does not lead to potent inhibitors.

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

12 l structures, which led to several extremely 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 ries of E2-derivatives at position C3 of the potent inhibitor 16beta-(m-carbamoylbenzyl)-E2 to remove

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

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

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

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

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

21 The two more potent inhibitors also suppress slow cooperative unfoldi

22 ular modeling studies because it is the most potent inhibitor and corrector of P-gp.

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

24 irus (HCV), against which new generations of potent inhibitors are being developed.

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

26 The most potent inhibitor (compound 18, RX-37) obtained from this

27 The most potent inhibitor (compound 6) demonstrated limited selec

28 The most potent inhibitors contained a N(5)-isopropyl substituent

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

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

31 The most potent inhibitor does not bind to or inhibit human thior

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

33 NAcylation by administration of Thiamet-G, a potent inhibitor for O-GlcNAcase that removes O-GlcNAcyl

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

35 This work reports the discovery of novel and potent inhibitors for ACK1 tyrosine kinase (also known a

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

37 iscovery of orally available, selective, and potent inhibitors for the treatment of autoimmune disord

38 lecules led to the identification of several potent inhibitors for which bsNOS-inhibitor crystal stru

39 Sofosbuvir-based regimens characterized with potent inhibitors have been approved by the Food and Dru

40 nct inhibitors were identified with the most potent inhibitors having >10,000 min(-1) M(-1) k(inact)/

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

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

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

44 e crystal structure of mPGES-1 bound to four potent inhibitors in order to understand their structure

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

46 The most potent inhibitors in this series contained a five-member

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

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

49 The most potent inhibitors induced demethylation of CDKN2A promot

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

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

54 For example, we identified a potent inhibitor missed by differential scanning fluorim

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

56 Gleevec is a potent inhibitor of Abl tyrosine kinase but not of the h

57 of ChK1 inhibitors, was found to be a highly potent inhibitor of acetylcholine esterase (AChE) and un

58 2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation amo

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

60 2,5-dihydroxybenzoic acid was found to be a potent inhibitor of alpha-amylase with an IC50 value of

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

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

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

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

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

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

67 Ileal Fgf15 is a potent inhibitor of BA synthesis.

68 n) onset of agglutination but was an equally potent inhibitor of bacterial motility.

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

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

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

72 re very similar to that of Gleevec, G6G is a potent inhibitor of both Abl and c-Src kinases.

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

74 Crizotinib is a potent inhibitor of both ROS1 and ALK kinase domains.

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

76 Ibrutinib is a potent inhibitor of Bruton's tyrosine kinase (BTK).

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

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

79 oxin-interacting protein (TXNIP), which is a potent inhibitor of cellular glucose uptake and aerobic

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

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

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

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

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

85 Dasotraline is a novel compound that is a potent inhibitor of dopamine and norepinephrine transpor

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

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

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

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

90 sponding to hBVR's SH2-binding domain, was a potent inhibitor of glucose uptake and IRK.

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

92 ependent transcription in TZM-bl cells and a potent inhibitor of GSK-3beta kinase in vitro.

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

94 We demonstrate that L-MU-P is a more potent inhibitor of HA synthesis than oral MU in the 4T1

95 Entecavir (ETV) is a potent inhibitor of hepatitis B viral replication, but l

96 We show here that pyrvinium is a potent inhibitor of HH signaling, which acts by reducing

97 22 is facilitated where it functions as a bi-potent inhibitor of HIF-1alpha and TGF-beta activities,

98 ERINC5, and to a lesser extent SERINC3, as a potent inhibitor of HIV-1 particle infectivity that is c

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

100 t, we demonstrate that p18 protein is a more potent inhibitor of HSC self-renewal than p27 in mouse m

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

102 Compound NVP-BEZ235 (1) is a potent inhibitor of human phospoinositide-3-kinases and

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

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

105 thrombocytopenia syndrome virus (SFTSV) is a potent inhibitor of IFN responses.

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

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

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

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

110 These results reveal SNX-482 as the most potent inhibitor of Kv4.3 channels yet identified.

111 ng these enzymes, APOBEC3A (A3A) is the most potent inhibitor of L1 retrotransposition in cultured ce

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

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

114 oth neutral and acidic pH and proved to be a potent inhibitor of LRP1 function both in vitro and in v

115 The increased avidity for IgE made HBI a potent inhibitor of mast cell degranulation in the rat b

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

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

118 parahaemolyticus effector protein VopQ is a potent inhibitor of membrane fusion based on an in vitro

119 We identified Serpinb6b as a potent inhibitor of mGzmA.

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

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

122 Our findings demonstrated that 2 is a potent inhibitor of MRSA and fosfomycin-resistant MurA,

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

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

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

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

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

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

129 The p57kip2 gene encodes one such potent inhibitor of oligodendroglial differentiation and

130 ollectively, our data indicate that JQ1 is a potent inhibitor of osteoblast and osteoclast differenti

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

132 d identified gossypol acetic acid (GAA) as a potent inhibitor of oxidative stress-induced RPE cell de

133 Taken together, we have identified GAA as a potent inhibitor of oxidative stress-induced RPE necrosi

134 d an antibody that later emerged as the most potent inhibitor of pancreatic cancer cells grown as tum

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

136 9 is a promiscuous tankyrase inhibitor and a potent inhibitor of PARP1 in vitro and in cells, whereas

137 that it mediated collagen degradation, and a potent inhibitor of peptidase activity was identified.

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

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

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

141 Bortezomib is a potent inhibitor of proteasomes currently used to elimin

142 that the antibiotic amicoumacin A (AMI) is a potent inhibitor of protein synthesis.

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 zol-1-yl)-2,4 diaminoquinazoline, which is a potent inhibitor of S. aureus DHFR (Ki = 0.002 nM) with

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

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

148 id pharmacophore, with the goal of finding a potent inhibitor of serine carbapenemase enzymes that ar

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

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

151 MFP remains a potent inhibitor of SRM growing by fermentation, and MFP

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

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

154 Nitrite is a potent inhibitor of sulfate reducers, and it has been su

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

156 KE-driven breast cancer cells with CYT387, a potent inhibitor of TBK1/IKBKE and JAK signaling, impair

157 tified pyrazole sulfonamide, DDD85646 (1), a potent inhibitor of TbNMT.

158 zation experiments indicate that PRN694 is a potent inhibitor of Th1 and Th17 differentiation and cyt

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

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

161 ibition by 6-fluoromevalonate diphosphate (a potent inhibitor of the classical mevalonate pathway), r

162 agenesis and identification of bestatin as a potent inhibitor of the enzyme.

163 -2'-spirooxetane uridine triphosphate (8), a potent inhibitor of the HCV NS5B polymerase.

164 Cyclopamine (CPA), a potent inhibitor of the Hedgehog pathway, has produced p

165 Previously, we identified ISRIB as a potent inhibitor of the integrated stress response (ISR)

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

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

168 rgillomarasmine A (AMA), that is a rapid and potent inhibitor of the NDM-1 enzyme and another clinica

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

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

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

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

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

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

175 hemichannel antagonist lanthanum alone was a potent inhibitor of the spontaneous activity.

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

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

178 The xenobiotic rapamycin is a potent inhibitor of the yeast complex.

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

180 We show that HPV1 E4 is a potent inhibitor of this host cell kinase.

181 The most potent inhibitor of this series exhibits two-digit nanom

182 2][PF6] (AubipyOMe) was found to be the most potent inhibitor of TRAP5a and 5b activity reported to d

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

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

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

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

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

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

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

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 Potent inhibitors of bacterial IMPDHs have been identifi

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 tuted [1,2,4]triazolo[4,3-a]phthalazines are potent inhibitors of both the BET bromodomains such as B

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

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

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

202 (DM2), and are transformed into oligomeric, potent inhibitors of DM2 RNA dysfunction by a Huisgen 1,

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

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

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

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

207 nding or neuraminidase (NA) activity but are potent inhibitors of fusion.

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

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

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

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

212 Compounds 7 and 11 were potent inhibitors of glycinamide ribonucleotide formyltr

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

214 Novel potent inhibitors of h-15-LOX-1 are required to explore

215 CypA antagonists, such as cyclosporines, are potent inhibitors of HCV replication.

216 Insulin is one of the most potent inhibitors of hIAPP fibril formation, but its inh

217 rinergic antagonists, we found that the most potent inhibitors of HIV-1 fusion were those that target

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

219 These hybrids are potent inhibitors of human acetylcholinesterase and buty

220 rine derivative 6b were found to be the most potent inhibitors of human AChE (hAChE), demonstrating I

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

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

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

224 Their D-gluco-counterparts are also potent inhibitors of intestinal glycosidases, and becaus

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

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

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

228 count for the fact that two of them are very potent inhibitors of microtubules assembly and are cytot

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

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

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

232 compounds, among which several compounds are potent inhibitors of mutant IDH1 with Ki as low as 420 n

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

234 lycosides, including ouabain and digoxin, as potent inhibitors of NMD.

235 all tested compounds were evaluated as more potent inhibitors of NMDA-induced currents (IC50 values

236 ation of new 6-aminoquinolone derivatives as potent inhibitors of NS5B polymerase, an attractive and

237 Boronic acids have been shown to be potent inhibitors of numerous hydrolytic enzymes due to

238 closporin A, and most other cyclosporins are potent inhibitors of OATP1B1, MRP2, MDR1, and other impo

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

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

241 anti-inflammatory drugs (NSAIDs), which are potent inhibitors of phospholipase A2 and play a role in

242 Here, we developed highly specific and potent inhibitors of PI4KA and conditional knock-out mic

243 om an herbicide optimization program, highly potent inhibitors of Plasmodium falciparum (Pf) and Plas

244 acterium smegmatis, they proved to be highly potent inhibitors of Plasmodium falciparum in vitro grow

245 and cellular evidence that artemisinins are potent inhibitors of Plasmodium falciparum phosphatidyli

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

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

248 Nelfinavir and its analogs are more potent inhibitors of S2P cleavage activity than 1,10-phe

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

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

251 FR901464 (1) and spliceostatin A (2) are potent inhibitors of spliceosomes.

252 immature monocytes and granulocytes that are potent inhibitors of T cell activation.

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

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

255 Interestingly, microtubules are potent inhibitors of the actin nucleation activity of Ca

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

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

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

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

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

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

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

263 gene products PARP7, PARP10, and PARP12L are potent inhibitors of the replication of Venezuelan equin

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

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

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

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

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

269 of PfCRT, which could be exploited to design potent inhibitors of this key mediator of drug resistanc

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

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

272 All compounds were found to be potent inhibitors of various glycosidase enzymes with Ki

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

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

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

276 One of the most potent inhibitors reported in their work was demonstrate

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

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

279 The most potent inhibitor shows an IC50 value in the low micromol

280 27 was a weak DNA ligand, analog 5, the most potent inhibitor, strongly interacted with DNA.

281 24 and 25 muM respectively (similar range as potent inhibitors such as diclofenac and indomethacin in

282 pment and preclinical evaluation of a novel, potent inhibitor targeting CBP/p300 bromodomains that im

283 Methlut is also a more potent inhibitor than luteolin of de novo-synthesized TN

284 Methlut is a more potent inhibitor than luteolin or cromolyn for beta-hexo

285 nd why neutral phosphonate diesters are more potent inhibitors than monoanionic phosphonates.

286 Consequently, different potent inhibitors that target bacterial topoisomerases h

287 2,4-pyridinedicarboxylic acid (2,4-PDCA) are potent inhibitors, they exhibit limited selectivity.

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

289 s, but these compounds were not sufficiently potent inhibitors to validate our stabilization hypothes

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

291 The most potent inhibitor was further characterized for Gtf bindi

292 Most of these potent inhibitors were devoid of cytotoxicity toward hea

293 The most potent inhibitors were N(6)-(4-chlorobenzyl)- (10l, PSB-

294 7 or PF-367) has been identified as a highly potent inhibitor, which is among the most selective anta

295 ndeed, we identified compound 38 as a highly potent inhibitor with an IC50 value of 0.02 muM in a PDG

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

297 From these, AM-6761 (4) emerged as a potent inhibitor with remarkable biochemical (HTRF IC50

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

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

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