ライフサイエンスコーパス: selective inhibitor

1 17 selective inhibitor, but not by an ADAM10 selective inhibitor.

2 he flap pocket substituent led to one Plm IV selective inhibitor.

3 hedding was, however, inhibited by an ADAM10 selective inhibitor.

4 ther, posing a challenge for the design of a selective inhibitor.

5 ha (HIF-1alpha) signaling was assessed using selective inhibitors.

6 he binding site of chroman-4-one-based SIRT2-selective inhibitors.

7 tion confirmed further by gene knockdown and selective inhibitors.

8 hobic pocket that was used to design isoform-selective inhibitors.

9 manner that is sensitive to certain Aurora-A-selective inhibitors.

10 targeting allosteric sites to obtain mutant-selective inhibitors.

11 c acid for their ability to act as substrate-selective inhibitors.

12 ucts might inform the creation of potent and selective inhibitors.

13 y to be critical for the function of mt-DHFR selective inhibitors.

14 binding surfaces for the rational design of selective inhibitors.

15 the discovery and optimization of potent and selective inhibitors.

16 city that might be exploited to develop CDK1-selective inhibitors.

17 be used to obtain highly desirable substrate-selective inhibitors.

18 ROS was attenuated by MEK-selective and JNK-selective inhibitors.

19 ould guide the development of allosteric, DM-selective inhibitors.

20 ly has been restricted by the lack of highly selective inhibitors.

21 ish parameters needed to design novel hCA IX selective inhibitors.

22 uided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metallo

23 sulted in the identification of a potent TDO selective inhibitor (11e, IC50 = 30 nM), making it a pot

24 Here we demonstrate that the DPP8/9 selective inhibitor 1G244 blocks adipogenesis in preadip

25 0 inhibitors were not evident with our Grp94-selective inhibitor, 4-Br-BnIm.

26 Blocking TAK1 kinase activity with a highly selective inhibitor (5z-7-oxozeaenol) attenuated the ind

27 ding mode enabled the design of a potent and selective inhibitor 8i (IACS-9571) with low nanomolar af

28 e pharmacological effects of PDE4B and PDE4D selective inhibitors, A-33 and D159687, in mediating neu

29 tly reported that seviteronel, a CYP17 lyase-selective inhibitor, aedemonstrated a sustained reductio

30 The FabI isoform was inactivated by the FabI selective inhibitor AFN-1252, but the FabK isoform was n

31 ogy designed to facilitate identification of selective inhibitors against RING type E3 ubiquitin liga

32 Development of potent, highly selective inhibitors against this target remains an unme

33 Imatinib, a c-Abl-selective inhibitor, also specifically blocked PKCdelta

34 Apoptosis-Inducing Ligand); is an extremely selective inhibitor, among kinases, of human RIPK1 enzym

35 s inhibited in mice treated with a p110gamma-selective inhibitor and in Pik3cg(-/-) mice after lipopo

36 OX-2-dependent 2-AG oxygenation by substrate-selective inhibitors and blocked the inhibition of AA or

37 Here, we introduce subunit-selective inhibitors and dual-color fluorescent activity

38 ch-derived labdane-type diterpenes are TRPC6-selective inhibitors and may represent a starting point

39 fference between the responses of our highly selective inhibitors and published tool compounds sugges

40 Selective inhibitors and small interfering RNAs for NOX5

41 s and identified previously unrecognized SRM selective inhibitors and synergistic interactions betwee

42 ed, for other subtypes much less is known on selective inhibitors and the consequences of their inhib

43 the clinic to treat leukemia, but tight and selective inhibitors are not available for Bcl-2 paralog

44 Our studies demonstrate that SIRT2-selective inhibitors are promising anticancer agents and

45 hts the need for brain-penetrant IDH1 mutant-selective inhibitors as an alternative therapeutic optio

46 ngly bolster the utility of developing GLUT4-selective inhibitors as anti-cancer therapeutics.

47 Here we use conformationally selective inhibitors as chemical probes for interrogatio

48 medicinal chemists seeking to develop highly selective inhibitors as pharmacological probes and as cl

49 s have been directed toward discovery of ITK-selective inhibitors as potential treatments of inflamma

50 plex with a recently developed bioactive and selective inhibitor at 2.53 A resolution.

51 besartan and losartan were largely G protein-selective inhibitors at the AT(1)R, with very low potenc

52 Treatment with the ATR-selective inhibitor AZ20 caused proliferation inhibition

53 key findings were confirmed with another ATR-selective inhibitor AZD6738.

54 ATPase H(+) pump by Cl(-) removal or via the selective inhibitor bafilomycin had only a small effect

55 oxidation and CO2 reduction are inhibited by selective inhibitor binding to the Mo(VI) horizontal lin

56 old led to development of the original Grp94-selective inhibitor, BnIm.

57 A disintegrin and metalloprotease) 10 and 17 selective inhibitor, but not by an ADAM10 selective inhi

58 amino-alcohol carbazole (N-CBZ) as a PfHsp90-selective inhibitor by virtually docking a large set of

59 argely blocked by TG4-155, TG6-10-1 or COX-2 selective inhibitor celecoxib, but not by GW627368X.

60 The CFTR-selective inhibitor, CFTRinh-172, modestly reduced MCCV-

61 isoforms, making the design of CA IX isoform selective inhibitors challenging.

62 The selective inhibitor CK-2018571 prevents strong binding t

63 is end, we previously developed a potent and selective inhibitor (compound 1) of Toxoplasma gondii ca

64 Finally, we demonstrate that a parasite-selective inhibitor could be used to attenuate parasite

65 Selective inhibitors could help unveil the mechanisms by

66 ia and lymphoma cells, suggesting that HDAC3-selective inhibitors could prove useful for the treatmen

67 Given these evidence, 4a, as MGL selective inhibitor, could represent a valuable lead for

68 demonstrate that targeting PI3Kgamma with a selective inhibitor, currently being evaluated in a phas

69 ical inhibition of SUV39H1 using a novel and selective inhibitor decreased levels of H3K9me3 in the h

70 s further suggest that the approach of using selective, inhibitor-dependent phosphoproteome analysis

71 ell conserved between family members, making selective inhibitor design challenging.

72 deacetylase through small interfering RNA or selective inhibitor Ex527 greatly enhances MK-1775-induc

73 tease classes, making the development of the selective inhibitors exceedingly challenging.

74 R11935, a brain-penetrant and JNK2/3 isoform-selective inhibitor, exerted similar anorectic effects a

75 Here, a Grp94-selective inhibitor facilitated mutant myocilin degradat

76 examined in an initial study, an exquisitely selective inhibitor for a poorly characterized serine hy

77 ALDH1/2 isoenzymes, including compound 36, a selective inhibitor for ALDH2 (Ki = 2.4 muM), and compou

78 To date, no selective inhibitor for BRD7/9 has been reported despite

79 the selective PI3Kbeta inhibitor TGX221 as a selective inhibitor for ccRCC with both VHL and SETD2 mu

80 As a result, PTM is a selective inhibitor for FabF/FabB, while PTN is a dual i

81 ment with 2-AG alone or JZL184, a potent and selective inhibitor for monoacylglycerol lipase (MAGL) t

82 XDM-CBP is a highly potent and selective inhibitor for the bromodomains of CBP and p300

83 e the utility of these leads by developing a selective inhibitor for the previously untargeted kinase

84 However, there are no commercially available selective inhibitors for ALDH1A1.

85 ly aimed at the design of novel, potent, and selective inhibitors for each of these enzymes.

86 Selective inhibitors for each serine/threonine phosphata

87 the challenges in structure-based design of selective inhibitors for either enzyme.

88 The lack of potent and selective inhibitors for endocannabinoid transport has p

89 o assays were employed to develop potent and selective inhibitors for group VIA calcium-independent P

90 However, designing selective inhibitors for hCA IX has been difficult due t

91 yl sulfamate inhibitors has shown promise as selective inhibitors for hCA IX.

92 demonstrate an effective strategy to explore selective inhibitors for helicases, and 9 could be a pro

93 nt structural insight for the design of more selective inhibitors for hGLUTs and hGLUT1 in particular

94 is the absence of chemical tools designed as selective inhibitors for IKKalpha over IKKbeta.

95 efforts to develop stable, bioavailable, and selective inhibitors for the PADs.

96 ent cancer targets; however, very few highly selective inhibitors for these are available.

97 minobenzoic acid derivatives show promise as selective inhibitors for this group of aminopeptidases.

98 ruritic effects with topical applications of selective inhibitors for TRPV4 and also for MEK, the kin

99 To date, no PAD2-selective inhibitor has been developed.

100 Selective inhibitors have been challenging to design bec

101 f mutant myocilin in vitro, to date no Grp94-selective inhibitors have been investigated in vivo.

102 While for HDACs 1-3 and 6 many potent selective inhibitors have been obtained, for other subty

103 ave low predicted druggability and so far no selective inhibitors have been published.

104 HDAC8 deficiency or inhibition using HDAC8-selective inhibitors (HDAC8i) effectively restores p53 a

105 o determine the effect of the PI3K p110delta-selective inhibitor idelalisib on allergic responses.

106 ulting in regulatory approval of one isoform-selective inhibitor (idelalisib) for treatment of certai

107 etitive glutamate antagonists AP5 and GluN2B-selective inhibitor ifenprodil reduced NMDA-activated cu

108 ition synergism with low doses of this beta2-selective inhibitor in artemisinin-sensitive and -resist

109 azole and heterocyclic ring afforded a SphK1-selective inhibitor in SLP7111228 (Ki = 48 nM), which al

110 potential of targeting the STAT/TET1 axis by selective inhibitors in AML treatment.

111 t therapeutic target, for which there are no selective inhibitors in clinical trials to date.

112 ofiles may enable the use of HSP90alpha/beta selective inhibitors in treating chronic neurodegenerati

113 he efficacy and safety of fedratinib, a JAK2-selective inhibitor, in patients with ruxolitinib-resist

114 We identified several SRM selective inhibitors including selenate, selenite, tellu

115 However, the recent finding that MDM2-selective inhibitors induce high levels of its homologue

116 er TBI, as post-TBI injection of a calpain-2 selective inhibitor inhibited c-Abl activation and tau o

117 le of the Rho GTPase proteins by injecting a selective inhibitor into the mPFC and found that activat

118 now apparent that the targeting of RTKs with selective inhibitors is only transiently effective, as t

119 ent inhibitory activity of the first CYP26A1 selective inhibitors is reported.

120 Abemaciclib, a CDK4/6-selective inhibitor, is currently in phase III studies f

121 studies demonstrate that SLP120701, a SphK2-selective inhibitor (Ki = 1 muM), decreases S1P levels i

122 stration of ACY-738, a histone deacetylase 6-selective inhibitor, led to Hsp90 hyperacetylation in br

123 The absence of any potent, selective inhibitors limits clear understanding of the t

124 Reversible, beta5i-selective inhibitors may be useful for treatment of dise

125 re, we report that inhibiting NLRP3 with the selective inhibitor MCC950, blocked release of IL-1beta

126 The discovery of this new class of EAAT1-selective inhibitors not only supplements the currently

127 The selective inhibitor of 2-AG biosynthesis O7460 abolished

128 Here, we describe Sephin1 (selective inhibitor of a holophosphatase), a small molec

129 study, we synthesized and evaluated a novel selective inhibitor of ABCB1 (TTT-28) with high efficacy

130 ed the safety and efficacy of selonsertib, a selective inhibitor of apoptosis signal-regulating kinas

131 Here we report the discovery of a selective inhibitor of Aurora A, a key regulator of cell

132 Alisertib is an investigational, oral, selective inhibitor of aurora kinase A.

133 by MAST3 kinase converts the protein into a selective inhibitor of B55alpha- and B56delta-containing

134 Venetoclax (ABT-199) is a small-molecule selective inhibitor of BCL2 currently in clinical trials

135 hibited STAT5 by treating Mo-DCs with JQ1, a selective inhibitor of BET epigenetic readers, which can

136 ontaining proteins shows that 31 is a highly selective inhibitor of BET proteins.

137 n of EZH2 and EZH1, which include UNC1999, a selective inhibitor of both enzymes, and UNC2400, an ina

138 Dabrafenib is an oral selective inhibitor of BRAF kinase.

139 We assessed whether CCX140-B, a selective inhibitor of C-C chemokine receptor type 2 (CC

140 n of, to our knowledge, the first potent and selective inhibitor of CARM1 that exhibits anti-prolifer

141 in striatal medium spiny neurons, acts as a selective inhibitor of certain forms of the serine/threo

142 similar effect was observed with Go 6976, a selective inhibitor of classical Ca(2+)-dependent PKCs (

143 covered compound 3i (666-15) as a potent and selective inhibitor of CREB-mediated gene transcription

144 f the C-terminal peptide mimetic alphaCT1, a selective inhibitor of Cx43 channels, sensitized human M

145 shown that PD 0332991 (PD), an FDA-approved selective inhibitor of cyclin-dependent kinase 4/6 (CDK4

146 Orteronel is an investigational, partially selective inhibitor of CYP 17,20-lyase in the androgen s

147 ll-molecule screen, we found that UNC0638, a selective inhibitor of EHMT1 and EHMT2 histone methyltra

148 = 0.002 muM, cellular EC50 = 0.032 muM) and selective inhibitor of EZH2.

149 t the use of compound ND-336, a novel highly selective inhibitor of gelatinases (MMP-2 and MMP-9) and

150 ain so after switching to oral eliglustat, a selective inhibitor of glucosylceramide synthase.

151 roach we systematically characterize FR as a selective inhibitor of Gq/11/14 over all other mammalian

152 ted the efficacy and safety of GSK2330672, a selective inhibitor of human ileal bile acid transporter

153 an 600 clinically approved drugs as a direct selective inhibitor of human MCU.

154 antagonist cyclopamine acts as a potent and selective inhibitor of in vitro and in vivo hRSV replica

155 have identified BMS-986126, a potent, highly selective inhibitor of IRAK4 kinase activity that demons

156 n monocytes treated with a highly potent and selective inhibitor of IRAK4, we show that IRAK4 kinase

157 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinica

158 ted the prophylactic effects of rapamycin, a selective inhibitor of mammalian target of rapamycin sig

159 elumetinib (AZD6244 or ARRY-142886), an oral selective inhibitor of MAPK kinase (MEK) 1 and 2, in chi

160 ine, suggesting that it may provide a highly selective inhibitor of MEK1/2 for use as a cancer therap

161 CFI-402257 is a novel, selective inhibitor of Mps-1 with antineoplastic activit

162 (AG-221/CC-90007) is a first-in-class, oral, selective inhibitor of mutant-IDH2 enzymes.

163 )benzyl)morpholine ((11)C-MeNER) is a highly selective inhibitor of noradrenaline transporters, and P

164 as chromosome maintenance region 1 (CRM1) by Selective Inhibitor of Nuclear Export (SINE) compounds r

165 Selinexor is the first oral selective inhibitor of nuclear export compound tested fo

166 , safety, and efficacy of selinexor, an oral selective inhibitor of nuclear export compound, in patie

167 Selinexor is a novel, first-in-class, selective inhibitor of nuclear export compound, which bl

168 The selective inhibitor of nuclear export, selinexor, is in

169 netics, and pharmacodynamics of selinexor, a selective inhibitor of nuclear export, when combined wit

170 Losmapimod is a potent and selective inhibitor of p38 MAPK.

171 n the discovery of 2, an in vitro potent and selective inhibitor of PDE10A with high striatal occupan

172 A selective inhibitor of PI3Kbeta inhibits the Akt/mTOR pa

173 he identification of 52, a potent and highly selective inhibitor of PI3Kdelta that demonstrates effic

174 is work led to the discovery of 35, a highly selective inhibitor of PI3Kdelta which displays an excel

175 Idelalisib, a selective inhibitor of PI3Kdelta, is approved for the tr

176 Conversely, a selective inhibitor of PKC, calphostin C, blocks mbGR/PK

177 Imatinib, a selective inhibitor of platelet-derived growth factor re

178 Furthermore, a selective inhibitor of PLD2, CAY10594, and a lipase-dead

179 hway of cholesterol metabolism with MK886 (a selective inhibitor of PPARalpha) in RAW264.7 macrophage

180 A selective inhibitor of reverse mode Na/Ca exchange block

181 This study reveals that the selective inhibitor of RNA polymerase I (Pol I) transcri

182 e approximately 400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation o

183 The only known selective inhibitor of SETD8 to date is nahuoic acid A,

184 Administration of XPro1595, a selective inhibitor of soluble TNFalpha, effectively pro

185 Entospletinib (GS-9973) is an oral, selective inhibitor of spleen tyrosine kinase.

186 rm of the methylthioninium moiety, acts as a selective inhibitor of tau protein aggregation both in v

187 LP99 is now reported as the first potent and selective inhibitor of the BRD7 and BRD9 bromodomains.

188 A selective inhibitor of the calcium-activated chloride ch

189 e profiling revealed 5-IT to be a potent and selective inhibitor of the dual-specificity tyrosine pho

190 Docking studies with GSK-J1, a selective inhibitor of the KDM6/KDM5 subfamilies, identi

191 RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a

192 ur data show that idelalisib is a potent and selective inhibitor of the kinase activity of PI3Kdelta.

193 Here we describe a selective inhibitor of the kinetoplastid proteasome (GNF

194 se 1 trial, idelalisib (GS-1101, CAL-101), a selective inhibitor of the lipid kinase PI3Kdelta, was e

195 ddC is a selective inhibitor of the mitochondrial DNA polymerase

196 exidine dihydrochloride, an antibiotic and a selective inhibitor of the mitochondrial phosphatase Ptp

197 ded phase 2 dose (RP2D) of oral selinexor, a selective inhibitor of the nuclear export protein XPO1.

198 study, we compared the effects of ToxB to a selective inhibitor of the Rac-specific guanine nucleoti

199 r inhibits cyclooxygenases; R-ketorolac is a selective inhibitor of the small GTPases Ras-related C3

200 y, we used a pharmacologic approach (SM16, a selective inhibitor of the type 1 TGF-beta receptor acti

201 was attributable solely to OX2 receptors; a selective inhibitor of this receptor subtype, N-ethyl-2-

202 cently, we have shown that VNI, a potent and selective inhibitor of trypanosomal CYP51 that we identi

203 Linifanib, a potent, selective inhibitor of vascular endothelial growth facto

204 ose AZD1775 is a first-in-class, potent, and selective inhibitor of WEE1 with proof of chemopotentiat

205 ered Ceapins, a class of pyrazole amides, as selective inhibitors of ATF6alpha signaling that do not

206 Several potent and selective inhibitors of ATR have been reported showing s

207 Therefore, the development of potent and selective inhibitors of BACE1 has been a focus of many d

208 Selective inhibitors of bromodomain-containing protein 9

209 ion provided potent (cellular IC50 < 10 nM), selective inhibitors of c-Met with desirable pharmacokin

210 din-2-amine derivatives as highly potent and selective inhibitors of CDK4 and CDK6.

211 (PG) production with either nonselective or selective inhibitors of cyclooxygenase-2 (COX-2) activit

212 Potent and selective inhibitors of Dyrk1B kinase were developed to

213 Using selective inhibitors of either PKG or cysteine proteases

214 , we discovered that UNC0638 and UNC0642-two selective inhibitors of euchromatic histone lysine N-met

215 afranal and its semisynthetic derivatives as selective inhibitors of five isoforms of human carbonic

216 llowing treatment of FLT3/ITD AML cells with selective inhibitors of FLT3.

217 cuted a small-molecule screen and discovered selective inhibitors of FOXO-dependent glucose productio

218 This study sought to identify selective inhibitors of GLUT4 to develop a more potent c

219 Selective inhibitors of hyaluronan (HA) binding to the c

220 A high throughput screen for selective inhibitors of IDH1 bearing the oncogenic mutat

221 he first time a series of novel, potent, and selective inhibitors of IKKalpha.

222 imidine carboxylic acids that are potent and selective inhibitors of kynurenine monooxygenase and com

223 he case of matrix metalloproteinases (MMPs), selective inhibitors of MMP-12 and MMP-13 are available

224 binders, of which 14 performed as potent and selective inhibitors of MMP-14 rather than as broad-spec

225 rs a fruitful approach to the development of selective inhibitors of mosquito ACE enzymes as novel la

226 -substituted-6-arylthiouracils as potent and selective inhibitors of MPO.

227 ation for the further development of ANPs as selective inhibitors of MtHGPRT and as antituberculosis

228 Although selective inhibitors of mutant IDH1 and IDH2 have been i

229 -activity studies, several highly potent and selective inhibitors of nNOS were discovered.

230 new class of orally available small-molecule selective inhibitors of nuclear export, specifically, th

231 emonstrated by the development of potent and selective inhibitors of PAD3, a PAD subtype implicated i

232 Veliparib and niraparib are selective inhibitors of PARP1 and PARP2; olaparib, rucap

233 Herein, we report a detailed study of novel selective inhibitors of PI4K IIIbeta, which exert antivi

234 Isoform-selective inhibitors of PKCbetaII, PKCdelta, and PKC giv

235 nyl benzo[d]isothiazol-3(2H)-ones as species-selective inhibitors of Plasmodium spp. 2-C-methyl-D-ery

236 dxG nucleoside or related prodrug analogs as selective inhibitors of Poltheta activity.

237 an be used for the structure-based design of selective inhibitors of potential medical interest.

238 Well-characterized selective inhibitors of protein arginine methyltransfera

239 Selective inhibitors of protein lysine methyltransferase

240 dings provide a detailed characterization of selective inhibitors of rat brain DAGL and demonstrate t

241 trial operations, few compounds are known as selective inhibitors of respiratory sulfate reducing mic

242 However, selective inhibitors of SETD8 are scarce.

243 ery of structures that are potent and highly selective inhibitors of SGLT2.

244 ut screening strategy to identify potent and selective inhibitors of SRM, quantitatively ranked the s

245 or and constrained tryptamine derivatives as selective inhibitors of the 5-HT6 serotonin receptor and

246 xamides has been discovered and optimized as selective inhibitors of the ataxia telangiectasia mutate

247 reports the development of highly potent and selective inhibitors of the beta5c catalytic activity of

248 To date, no potent and selective inhibitors of the bromodomain have been report

249 Selective inhibitors of the CREB binding protein (CREBBP

250 n similar to oligomycin A and apoptolidin A, selective inhibitors of the mammalian ATP synthase (comp

251 report the engineering of highly potent and selective inhibitors of the Nav1.7 channel based on tara

252 AIDs of the fenamate class are effective and selective inhibitors of the NLRP3 inflammasome via inhib

253 ence from which they are derived, and act as selective inhibitors of the p53/hDM2 interaction.

254 action in normal and pathological processes, selective inhibitors of this association have not been w

255 Selective inhibitors of this enzyme are potential broad-

256 ance of NSD2 to cancer, there are no potent, selective inhibitors of this enzyme reported.

257 S, and the use of this information to design selective inhibitors of this enzyme.

258 Development of potent and subtype-selective inhibitors of this ion channel is crucial for

259 d provide a rationale for the development of selective inhibitors of this state.

260 Here we report the development of selective inhibitors of three deltaPKC substrates (in vi

261 but its function there is unclear and potent selective inhibitors of TRAP are required to assess func

262 Given the analgesic potential of subtype-selective inhibitors of voltage-gated sodium (NaV) chann

263 of a series of triazolopyridazines that are selective inhibitors of wild-type (WT) MET kinase and se

264 onitor by NMR the effect of conformationally selective inhibitors on kinase backbone dynamics.

265 reviously, we discovered two classes of GRK2-selective inhibitors, one stemming from GSK180736A, a Rh

266 of Akt was abolished in the presence of a Gq-selective inhibitor or in Gq-deficient murine platelets,

267 LRRK2's kinase activity, with the potent and selective inhibitor PF-06447475, rescues the observed de

268 tified a novel, state-dependent human Nav1.7 selective inhibitor (PF-05089771, IC50 = 11 nM) that int

269 revented by pretreatment of GCs with the PKA-selective inhibitor PKA inhibitor (PKI), the MEK inhibit

270 b, an orally bioavailable clinical stage CDK-selective inhibitor, potently blocks CDK9, the transcrip

271 Fedratinib, a JAK2-selective inhibitor, previously demonstrated clinically

272 In contrast, IDH1 mutant-selective inhibitors provided considerable survival bene

273 dependent phospholipase A2gamma (iPLA2gamma)-selective inhibitor (R)-BEL suggested that iPLA2gamma is

274 profiling studies demonstrate that the ROS1-selective inhibitors retain efficacy against the recentl

275 ce to direct inhibition of ERK by the ERK1/2-selective inhibitor SCH772984.

276 ently discovered group II PAK (PAK4, -5, -6) selective inhibitor series based on a benzimidazole core

277 retreatment of airway secretions with a KLK5-selective inhibitor significantly reduced the activation

278 ted in numerous companies identifying potent selective inhibitors, some of which progressed to early

279 ors such as 1 (NG25) and 2 as well as MAP4K2 selective inhibitors such as 16 and 17.

280 ays resulted in identification of potent and selective inhibitors such as compounds 9 and 45.

281 Accordingly, application of CK2-selective inhibitors suppressed KCNQ2 current.

282 The goal of our program was to find a PARP-1 selective inhibitor that would potentially mitigate toxi

283 prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more a

284 amic acid, and tolfenamic acid are substrate-selective inhibitors that bind rapidly to COX-2, quench

285 tion led to the identification of potent and selective inhibitors that demonstrated favorable pharmac

286 ly, HDAC6 is a target for the development of selective inhibitors that might be useful in new therape

287 s, culminating in the creation of potent and selective inhibitors that were used to understand the fu

288 ach coupled with treatment using PDE isozyme-selective inhibitors to characterize the phosphoproteome

289 herapeutic interest in developing potent and selective inhibitors to control LMW-PTP activity.

290 They were also used as selective inhibitors to effectively compete with focal a

291 ar on target activity of the most potent and selective inhibitor TPOP146, which showed 134 nM affinit

292 olubility-driven optimization of our isoform-selective inhibitors using a scorpion shaped lead.

293 A series of nonazole CYP26A1 selective inhibitors was identified with low nM potency.

294 Potent, selective inhibitors were efficacious in both chemical a

295 Selective inhibitors were used to disentangle the roles

296 ing schedules requires a well-characterized, selective inhibitor with pharmacokinetic properties, fle

297 ffold would allow access to a series of PAD2-selective inhibitors with enhanced cellular efficacy.

298 COX inhibition potency and were found to be selective inhibitors with high affinity to COX-2 (IC50 r

299 ers (Jak1, Jak2, Jak3, and Tyk2), developing selective inhibitors within this family is challenging.

300 and can aid in the design of more potent and selective inhibitors without agonistic function.