ライフサイエンスコーパス: inhibitory potency

1 tructure-based optimization led to increased inhibitory potency.

2 ased infectivity and further reduced peptide inhibitory potency.

3 th the AM2 channel, thus leading to stronger inhibitory potency.

4 nd chain-length factors provide the greatest inhibitory potency.

5 and metabolic stability without any loss of inhibitory potency.

6 n bonding potential at this site for optimal inhibitory potency.

7 orphinan ring leads to a strong reduction of inhibitory potency.

8 itution of N-adenine atoms with MANT reduces inhibitory potency.

9 titutions within these peptides increase the inhibitory potency.

10 oquinolylbenzamides, some with low nanomolar inhibitory potency.

11 he cargo/C-peptide linker partially restores inhibitory potency.

12 inase C, producing a >1,000-fold increase in inhibitory potency.

13 razole ring (17b, 23b, 26b-I) enhanced COX-2 inhibitory potency.

14 rovided enhanced chemical stability and high inhibitory potency.

15 acids that exhibited varying degrees of HDAC inhibitory potency.

16 cells with an affinity corresponding to its inhibitory potency.

17 the effects of ANG active site mutations on inhibitory potency.

18 ation of these hydroxyl groups reduces their inhibitory potency.

19 less PXR binding while maintaining the P2X4 inhibitory potency.

20 t side aryl ring with maintenance of good ST inhibitory potency.

21 ionalities results in essentially no loss of inhibitory potency.

22 the galloyl ester moiety were essential for inhibitory potency.

23 ope, consequently leading to a low-nanomolar inhibitory potency.

24 he prosthetic group allows the prediction of inhibitory potency.

25 ar groups in the same configuration enhances inhibitory potency.

26 d resulting in a dramatic enhancement of the inhibitory potency.

27 ophore significantly improved peptidomimetic inhibitory potency.

28 rivatives, which possess nanomolar USP1/UAF1 inhibitory potency.

29 inity of truncated PLB for SERCA and loss of inhibitory potency.

30 tional interactions with RT and thus improve inhibitory potency.

31 dity and thus substantially increasing their inhibitory potency.

32 zoic moieties were performed to maximize the inhibitory potency.

33 st potent inhibitors was correlated to their inhibitory potency.

34 inverse relationship between processing and inhibitory potency.

35 acemic mixture, were assayed for their EcDXR inhibitory potency.

36 acid derivatives with low to high nanomolar inhibitory potencies.

37 ed that the p27 variants exhibited disparate inhibitory potencies.

38 hat appear to correlate with measured growth-inhibitory potencies.

39 ted (Ile or Val) phosphopeptides showed high inhibitory potencies.

40 hibited a complex response with two separate inhibitory potencies.

41 phosphate analogues, and compared their CD73 inhibitory potencies.

42 order to examine effects on HIV-1 integrase inhibitory potencies.

43 target for DECA analogs with increasing PKC inhibitory potencies.

44 in compounds with 10-100-fold improved AMPDA inhibitory potencies.

45 ecule hLDH5 inhibitors displaying remarkable inhibitory potencies.

46 hosphorylated at Thr-38, which increases its inhibitory potency 1000-fold.

47 e the same hydrophobic pocket to gain strong inhibitory potency (13), as well as high isoform selecti

48 with an (S)-3-phenylpiperidine increased the inhibitory potency 3-fold.

49 Ser and one a Thr; phosphorylation enhanced inhibitory potency 50-fold.

50 51 active site topology underlies their high inhibitory potency, a longer coordination bond between t

51 n the left side aryl ring, while having good inhibitory potencies against IN in extracellular assays,

52 dicate that resveratrol has a broad range of inhibitory potencies against purified PKC that depend on

53 enidate (MP), was synthesized and tested for inhibitory potency against [(3)H]WIN35,428, [3H]citalopr

54 Both compounds exhibited higher inhibitory potency against a COX-2 R120A variant than ag

55 ve, and mixed), with sub- and low micromolar inhibitory potency against a fluorogenic substrate.

56 g conformational constraints, to improve the inhibitory potency against active Src kinase.

57 hydroxynorendoxifen (10), displayed elevated inhibitory potency against aromatase and enhanced affini

58 the pro domain variant C184A showed the same inhibitory potency against both TACE forms as wild type

59 employed to design additional analogues with inhibitory potency against CYP2C19.

60 osition of 5-deaza methotrexate (MTX) on the inhibitory potency against dihydrofolate reductase (DHFR

61 ine counterpart, but also displayed improved inhibitory potency against DNA methyltransferase 1, impr

62 r biological profile is explored in terms of inhibitory potency against enzymes of the PfFAS-II pathw

63 Compound 5 g shows low nanomolar inhibitory potency against HDAC6 and a selectivity of ap

64 Compound 2 had inhibitory potency against human DHFR similar to N-[4-[2

65 unds containing only a salicylic acid showed inhibitory potency against IN, none of the compounds con

66 danine) group (e.g. 5-13) showed significant inhibitory potency against IN, while the presence of eit

67 This analogue exhibited moderate inhibitory potency against Mycobacterium tuberculosis th

68 chemical synthesis of LCL204, with enhanced inhibitory potency against NMT1.

69 tested compounds, 7 and 8 showed the highest inhibitory potency against Pf enoyl-ACP-reductase (PfFab

70 hat enantiomeric D-chicoric acid (4) retains inhibitory potency against purified integrase equal to i

71 C8-C9 bridge region (analogue 3) doubled the inhibitory potency against recombinant human (rh) DHFR (

72 1, compound 3 demonstrated increased growth inhibitory potency against several human tumor cell line

73 n the identification of novel compounds with inhibitory potency against TGK.

74 Therefore, the retained and improved inhibitory potency against the drug-resistant variants A

75 of some of these compounds show low to high inhibitory potency against the human CYP17 enzyme.

76 itative rationale to the drastic decrease in inhibitory potency against the V27A variant.

77 et of rapamycin (mTOR) that also showed high inhibitory potency against Trypanosoma brucei cultures.

78 se they are not cleaved by furin and possess inhibitory potency almost equal to L-polyarginines.

79 We observed substantial differences in the inhibitory potency among structurally highly similar mor

80 in new anticancer agents with improved Top1 inhibitory potencies and cancer cell cytotoxicities.

81 played excellent acetylcholinesterase (AChE) inhibitory potencies and interesting capabilities to blo

82 7-azaindenoisoquinolines can modulate their inhibitory potencies and selectivities vs Top1, Tdp1, an

83 These were characterized in terms of their inhibitory potencies and structure-activity relationship

84 of Suprastat demonstrates subnanomolar HDAC6 inhibitory potency and a hundred- to a thousand-fold HDA

85 d favorable properties with respect to their inhibitory potency and a selective mode of action.

86 henylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the alpha(2)-adrenoc

87 ere synthesized and evaluated for their PNMT inhibitory potency and affinity for the alpha2-adrenocep

88 , V94A, E97A) in a single mutant reduced the inhibitory potency and binding to levels similar to thos

89 ies of its derivatives generated to increase inhibitory potency and drug bioavailability were tested.

90 e best inhibitor, 7, exhibited low nanomolar inhibitory potency and good isoform selectivities (nNOS

91 entification of compound 4 with desired FXIa inhibitory potency and good oral bioavailability but hig

92 ine groups have significantly increased PI3K inhibitory potency and greater efficacy in nude mouse xe

93 timized compounds that display low nanomolar inhibitory potency and high selectivity against the rela

94 ed to inhibitors (16-21) that have high PNMT inhibitory potency and high selectivity, and most of the

95 This study shows that not only greater inhibitory potency and isozyme selectivity but more drug

96 9 leads to a substantial improvement of the inhibitory potency and metabolic stability.

97 re was designed, which showed nanomolar nNOS inhibitory potency and more than 1000-fold nNOS selectiv

98 s onto the left side aryl ring enhanced 3'-P inhibitory potency and reduced selectivity toward ST rea

99 ever, the most active compounds had moderate inhibitory potency and relatively high cytotoxicity, res

100 rary (8, 14, 17, and 18) have excellent PNMT inhibitory potency and selectivity and are predicted, on

101 mides was identified with significant enzyme inhibitory potency and selectivity for HIV RNase H.

102 Excellent inhibitory potency and selectivity for nNOS over eNOS an

103 d synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B.

104 genase inhibitory activity but retain AKR1C3 inhibitory potency and selectivity.

105 es were synthesized and evaluated for AKR1C3 inhibitory potency and selectivity.

106 se compounds approached that of antimycin in inhibitory potency and some showed growth reduction of S

107 of high-affinity antibodies with the desired inhibitory potency and specificity.

108 ly unfavorable and was found to decrease the inhibitory potency and to confer high pH sensitivity, de

109 nalogues 4s and 4t, respectively, had higher inhibitory potency and/or absolute selectivity than (2S,

110 M7a of GLAST have detrimental effects on the inhibitory potency and/or efficacy of UCPH-101 while not

111 tive beta-catenin/Tcf interactions, quantify inhibitory potency, and are complementary with each othe

112 Herein we describe the design, synthesis, inhibitory potency, and pharmacokinetic properties of a

113 ropyl-thiazole (IPT) moiety affect affinity, inhibitory potency, and the ligand binding mode.

114 rination also results in a reduction in PNMT inhibitory potency, apparently due to steric and electro

115 nalogues with improved AMP deaminase (AMPDA) inhibitory potency are described.

116 omeric carbinol mixture which showed reduced inhibitory potency, arguing against tetrahedral analogue

117 nd V94A) were found that clearly reduced the inhibitory potency as measured by the activity of a reco

118 dentified that had widely varied cathepsin K inhibitory potency as well as pharmacokinetic properties

119 uted-2-pyridylquinazolines in terms of their inhibitory potency as well as selectivity toward ABCG2.

120 ult in analogues with substantially improved inhibitory potencies at EAAT1 compared to that displayed

121 Among them, compound 20 displayed high inhibitory potency at CDK1 (IC(50) = 0.021 microM), CDK2

122 maleimides) were found to have submicromolar inhibitory potency at GSK-3beta with various degrees of

123 To gain the inhibitory potency at GSK-3beta, the ring sizes of these

124 strong binding interaction with IDO1, to the inhibitory potency at the low nanomolar level in several

125 All inhibitors tested exhibited similar inhibitory potencies between mTORC1 and truncated mTOR c

126 ffered an explanation for the differences in inhibitory potency between glucosyl and glucosaminyl der

127 rimary amines like farnesylamine also showed inhibitory potency but a short duration of action, proba

128 is useful not only for the determination of inhibitory potency but also for the differentiation of t

129 We not only increased TRPV4-inhibitory potency, but surprisingly also generated two

130 By lectin conjugation, we improved CFTR inhibitory potency by approximately 100-fold (to 50 nmol

131 We were able to increase inhibitory potency by synthesizing compounds with a nitr

132 This study shows that high CD73 inhibitory potency can be achieved by simply introducing

133 Optimization of inhibitory potency can be facilitated by structural info

134 This inhibitory potency can be traced to the corresponding C-

135 er produced geometric isomers with different inhibitory potencies: cis IC(50) = 52 +/- 12 microM and

136 Of the 45 compounds, we found 11 to have inhibitory potency comparable or significantly improved

137 in higher affinity, metabolic stability, and inhibitory potency compared with aptamers with single mo

138 Although additional gains in intrinsic ECE-1 inhibitory potency could occasionally be achieved by add

139 In contrast, this inhibitory potency decreased over 30-fold against a TACE

140 Results showed that polarizability and inhibitory potency directly correlated within all four s

141 ne core and several inhibitors with improved inhibitory potency down to Ki = 0.11 muM were identified

142 couplers differed from their in vitro kinase-inhibitory potencies due to different molecular requirem

143 bstituent at the 4-pyridyl position improved inhibitory potency due to a favorable lipophilic interac

144 ghest GABA content (10.42 mg/g extract), ACE-inhibitory potency (expressed as IC(50)) of 0.18 mg prot

145 he intrinsically disordered region makes its inhibitory potency exquisitely sensitive and responsive

146 S-enantiomers of BEL would possess different inhibitory potencies for iPLA(2)beta and iPLA(2)gamma.

147 Rank order of variant inhibitory potency for all four nicotinic processes was

148 drophobic alkane-based moieties improves the inhibitory potency for both hemagglutinin-neuraminidase

149 r have comparable submicromolar affinity and inhibitory potency for CYP3A4 and, thus, could serve as

150 ion not only drastically lowers affinity and inhibitory potency for CYP3A4 but also leads to multiple

151 ws the development of INH-ODNs with superior inhibitory potency for inflammatory diseases with high m

152 howed a dramatic 800-fold improvement in the inhibitory potency for JBalphaMan, which is outstanding

153 In contrast, inhibitory potency for other P450s was increased, and th

154 The rank order of inhibitory potency for the remaining 11 compounds tested

155 nd to the identification of derivatives with inhibitory potency higher than that of the standard inhi

156 5a, 5o, and 8i have STAT3-inhibitory potencies (IC(50)) of 0.55, 0.38, and 0.34 mu

157 in 5, increased recombinant human (rh) DHFR inhibitory potency (IC(50) = 0.42 microM) as well as the

158 lamine derivative, 49, displayed good enzyme inhibitory potency (IC(50) = 1.3 microM) and the most po

159 f-life (t1/2 >> 120 min), but also sustained inhibitory potency (IC50 = 4.2 nM) and selectivity over

160 adjacent alpha-helix, whose contribution to inhibitory potency illustrates the feasibility of exploi

161 The three peptides show greater inhibitory potencies in cellular and mucosal tissue pre-

162 ead optimization, we prepared compounds with inhibitory potencies in the low-double-digit nanomolar r

163 e derivatives was synthesized and tested for inhibitory potency in [3H]WIN 35,428 binding and [3H]dop

164 responding nucleosides exhibited significant inhibitory potency in a cell-based replicon assay.

165 h these enantiomers correlated well with the inhibitory potency in a GCP II assay.

166 eneration of EphB4 inhibitors that show high inhibitory potency in both enzymatic and cell-based assa

167 unds reach low micromolar to upper nanomolar inhibitory potency in cell-based assays, are selective a

168 Ala to m-Cl-Phe led to an 8000-fold shift in inhibitory potency in favor of the Mtb proteasome, resul

169 found that bis-aroylhydrazides could acquire inhibitory potency in Mg2+ using dihydroxybenzoyl substi

170 The ability to accurately determine inhibitory potency in reactions with low picomolar conce

171 ,4-thiadiazoles and -1,2,3-triazoles with an inhibitory potency in the nanomolar range.

172 the autoinhibited conformation, retain full inhibitory potency in the presence of physiological conc

173 by beta-adrenergic blockers and the order of inhibitory potency is (s)(-)-propranolol>betaxolol>>timo

174 As a consequence, inhibitory potency is determined by the association rate

175 ynamics simulation studies revealed that the inhibitory potency is favored by promoting interactions

176 abain's rhamnose moiety had little effect on inhibitory potency, it caused a dramatic decline in liga

177 c acid itself was examined at neutral pH for inhibitory potency, it was found to have K(i) = 31 +/- 7

178 anamide (13d, delmorphan-A) showed picomolar inhibitory potency (Ke = 0.1 nM) in the [35S]GTPgammaS f

179 wo inhibitors, 13 and 14, show low nanomolar inhibitory potency (Ki = 5 nM for nNOS) and good isoform

180 d imidazo[4,5-b]pyridine analogues with high inhibitory potency (Ki values of 5.00 nM and 29.6 nM, re

181 Inhibitor 5d has shown low nanomolar enzyme inhibitory potency (Ki=1.1 nM) and very good cellular in

182 ich were found to possess human PNMT (hPNMT) inhibitory potency <5 nM versus AdoMet.

183 New compounds display telomerase-inhibitory potency (<1 microM) in the TRAP assay.

184 ly inhibit HDAC6 while maintaining nanomolar inhibitory potency: N-hydroxy-4-[(N(2-hydroxyethyl)-2-ph

185 (9) residue (5) increased the rat GH release inhibitory potency nearly 4-fold to 0.73 nM but resulted

186 ed drugs for OATP2B1 inhibition and quantify inhibitory potencies necessary for extrapolation of clin

187 lues ranging from 23 to 51 nm, comparable to inhibitory potencies observed in intact cells.

188 We conclude that the decreased inhibitory potency observed for glyphosate is a result o

189 domain of BoNT A, we determined the relative inhibitory potencies of a family of structurally related

190 perimentally both the binding affinities and inhibitory potencies of a series of 37 cardiac glycoside

191 iciency of binding to mannan and changed the inhibitory potencies of competing saccharides to more cl

192 Overall, inhibitory potencies of nucleotides at sGCalpha1beta1 ve

193 The inhibitory potencies of the C8-modified-nucleotides on t

194 ion does not affect nucleation but decreases inhibitory potency of 1-548 by 20,000-fold.

195 fficiency while maintaining or exceeding the inhibitory potency of 1.

196 The distinct binding features and superior inhibitory potency of 10a, together with its excellent e

197 A-II is responsible for the diminished CA-II inhibitory potency of 2.

198 Here we show that the nanomolar inhibitory potency of 5-Helix (IC50 approximately 6 nm)

199 escribed previously and correctly ranked the inhibitory potency of a further four verapamil metabolit

200 uld be useful for evaluating state-dependent inhibitory potency of a large number of samples.

201 al of the NTT results in the decrease of the inhibitory potency of AcCYS1 against fruit bromelain dur

202 Examination of the PTP1B inhibitory potency of an extensive series of phosphotyro

203 ompatibility, and significantly enhanced the inhibitory potency of ATRA on HCC cell growth, improving

204 ide sequence that still retained the calpain-inhibitory potency of B27-WT was found to be MSSTYIEELGK

205 ults of this work were an enhancement of the inhibitory potency of beta-lactone carbamate derivatives

206 s allosteric state-dependent modulators, the inhibitory potency of both compounds is highly dependent

207 The inhibitory potency of both these single agents against V

208 r, conflicting data has been reported on the inhibitory potency of CDKi's and a systematic characteri

209 and V170A, did not considerably diminish the inhibitory potency of certain novel inhibitor scaffolds

210 Regarding inhibitory potency of ciproxifan on rat brain MAO, these

211 The inhibitory potency of dantrolene on ECCE found in wild-t

212 Our results suggest that increased inhibitory potency of Ehp relative to Efb-C is derived f

213 The inhibitory potency of gammaT and gamma-CEHC was diminish

214 ormat enables efficient determination of the inhibitory potency of GAT1 inhibitors, is capable of ide

215 ssion shows negative correlation with growth inhibitory potency of geldanamycin but not with its anal

216 ometry-based infection assays to measure the inhibitory potency of HIV-1-neutralizing monoclonal anti

217 observation, together with the screen of the inhibitory potency of human PDE inhibitors against TcrPD

218 nciles existing contradictory values for the inhibitory potency of INH-NAD for InhA.

219 The growth-inhibitory potency of JNK2 antisense ((JNK)2 IC(50) = 0.

220 The iNOS inhibitory potency of KLYP956 is insensitive to changes

221 ants for [(3)H]MTX influx; (b) similarity of inhibitory potency of known RFC substrates; (c) lack of

222 Since the enhanced binding or inhibitory potency of L2 is diminished (to the level of

223 The inhibitory potency of mAChR subtype-selective antagonist

224 AICAr increases growth inhibitory potency of MTX and aminopterin against CCRF-C

225 binding Plasmodium FKBP has no effect on the inhibitory potency of MTXSLF in vivo.

226 either single or in combination, reduced the inhibitory potency of NaKtide on Src.

227 and 5) resulted in dramatic decreases in the inhibitory potency of nNOS.

228 This finding and the similar inhibitory potency of P10-P4' Stat(Val) for ProBACE460 a

229 ation-relieving mutations enhance the kinase inhibitory potency of R without compromising its specifi

230 s principally responsible for the changes in inhibitory potency of rapid, reversible inhibitors, wher

231 To improve the inhibitory potency of short C-peptides that target the h

232 Here, we have investigated the inhibitory potency of stable fluorinated or phosphonate-

233 and composition cumulatively account for the inhibitory potency of the aminoglycoside-arginine conjug

234 domains retains the PKR binding affinity or inhibitory potency of the full-length RNA.

235 The inhibitory potency of the fusion peptides was even great

236 Efforts to enhance the inhibitory potency of the initial purine series of fruct

237 Interestingly, the inhibitory potency of the isatin compounds was related t

238 t efficacy and specificity; for example, the inhibitory potency of the kinase was glutathione disulfi

239 terminal acetylation was found to reduce the inhibitory potency of the l-hexapeptide LLRVKR against f

240 ) to 17-normanoyl oxide (20a) and the higher inhibitory potency of the norpimarenylamine 26a (K(i) =

241 The inhibitory potency of the potent protease inhibitor, BIL

242 ycine derivative and still maintain the high inhibitory potency of the series if accompanied with a s

243 likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfon

244 A synergistic effect in increasing the PNMT-inhibitory potency of the THIQ nucleus and reducing the

245 Inhibitory potency of the unsubstituted aza-5[H]-phenant

246 ypsin complexes of inhibitors, and factor Xa inhibitory potency of these compounds, we conclude that

247 The inhibitory potency of these thiol-based compounds agains

248 The inhibitory potency of this family of inhibitors is simil

249 Despite demonstrating nearly the lowest PSMA inhibitory potency of this series, [(99m)Tc(CO)3( L1)] (

250 ivatives 11, 13, 14, 21, and 22 exhibited an inhibitory potency on aromatase comparable to that of le

251 owed that N-methylation reduces flecainide's inhibitory potency on RyR2 channels incorporated into ar

252 Compound 15 also displayed high inhibitory potency on VEGF-stimulated human umbilical ve

253 ecificity for fluoxetine determined by their inhibitory potencies or binding affinities suggests diff

254 Consequently, we were able to improve inhibitory potency or to convert inhibitors into strong

255 o ritonavir in terms of binding affinity and inhibitory potency owing to greater flexibility and the

256 , or the site of binding, but does lower the inhibitory potency, possibly due to an unfavorable inter

257 c acid), displays a >120-fold enhancement in inhibitory potency relative to the simple monovalent act

258 A comparison of inhibitory potencies shows that the diacid analogues wit

259 exylmethyl, led to increased gamma-secretase inhibitory potency, suggesting a large S1 pocket to acco

260 ls in the concentration range of its maximal inhibitory potency, suggesting that 37 will be an invalu

261 at concentrations relevant to the enzymatic inhibitory potency, suggesting that killing the parasite

262 ism of action of JS230 cumulated into growth inhibitory potency superior to that of classical two- or

263 nd inhibited AR function, exhibiting greater inhibitory potency than the approved AR antagonists.

264 In addition to inhibitory potency, this compound has the permeability,

265 lides caused binding affinity to decline but inhibitory potency to increase.

266 for compounds with similar in vitro hemozoin inhibitory potency to preconcentrate within the parasite

267 tivity-dependent manner, thus increasing the inhibitory potency to suppress the excitation through th

268 ion complex inhibitors that demonstrate high inhibitory potency toward a panel of clinically relevant

269 c amino acids led to analogues with improved inhibitory potency toward both enzymes, whereas negative

270 d excellent activity profiles with nanomolar inhibitory potency toward hMAO-B, high hMAO-B over hMAO-

271 FRET groups are important for securing high inhibitory potency toward PR3.

272 It is proposed that the loss of inhibitory potency upon Ser-16 phosphorylation or R9C mu

273 culated using ab initio quantum methods with inhibitory potency values determined in the presence of

274 e effect of this affinity enhancement on T20 inhibitory potency varied among different viral strains.

275 methyl-7-substituted-THIQs and enhanced PNMT inhibitory potency versus the corresponding 3-trifluorom

276 High inhibitory potency was also associated with 3-ether moie

277 A 35-fold decrease in inhibitory potency was also observed using a S461E mutan

278 s a correlation between binding affinity and inhibitory potency was found, some notable exceptions we

279 AK inhibitory potency was greatest for those compounds with

280 BACE-1 inhibitory potency was increased (0.9 microM to 11 nM K(

281 The contribution of TCR clonotype to inhibitory potency was investigated by delineating the r

282 luence of 4-anilino substitution on pan-erbB inhibitory potency was investigated.

283 nsistent with this finding, as the factor Xa inhibitory potencies were about 60-fold greater (DeltaDe

284 Their inhibitory potencies were comparable to that of casodex

285 and 4 were used to covalently modify wt RFC, inhibitory potencies were in the order 2 > 1 > 4; inhibi

286 For wt and K411A RFCs, inhibitory potencies were in the order 4 > 5 > 1 > 3 > 2

287 DE5(Q817A), vardenafil, sildenafil, and IBMX inhibitory potencies were weakened 610-, 48-, and 60-fol

288 Changes in inhibitory potency were generally consistent with the in

289 -amide previously led to the finding of high inhibitory potency when Xxx = 4-(phosphonodifluoromethyl

290 ctions established at the Phe-1 site improve inhibitory potency, whereas contacts provided by IPT mig

291 (C(12), C(14), or C(16)) exhibited enhanced inhibitory potencies which reached a plateau with the C(

292 phate groups with O-acyl greatly reduced the inhibitory potency, which tended to increase upon replac

293 onsubstrate) in these peptides increases the inhibitory potency while mutating the sites to aspartic

294 ated derivatives exhibited slightly improved inhibitory potencies with IC50 values up to 2.6 nM (casp

295 e aryl moieties (2c, 2j-l) demonstrated high inhibitory potencies with Kis in the low nanomolar range

296 Macrocycle 26 showed excellent enzyme inhibitory potency with a K(i) value of 0.7 nM and an an

297 tide CRVI exhibited the strongest tyrosinase-inhibitory potency (with an IC50 of 2.7 +/- 0.5 muM), wh

298 tion of compounds with excellent mTOR kinase inhibitory potency, with exquisite kinase selectivity ov

299 ree PALs showed dramatic rightward shifts in inhibitory potency, with Ki values ranging from 3.8 to 9

300 sents a 10- to 250-fold enhancement in AMPDA inhibitory potency without loss in the enzyme specificit

301 r hypothesis, because any improvement of the inhibitory potency would be readily recorded.