ライフサイエンスコーパス: inhibitory potency

1 ased infectivity and further reduced peptide inhibitory potency.

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

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

4 and metabolic stability without any loss of inhibitory potency.

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

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

7 titutions within these peptides increase the inhibitory potency.

8 oquinolylbenzamides, some with low nanomolar inhibitory potency.

9 ar groups in the same configuration enhances inhibitory potency.

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

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

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

13 rovided enhanced chemical stability and high inhibitory potency.

14 acids that exhibited varying degrees of HDAC inhibitory potency.

15 cells with an affinity corresponding to its inhibitory potency.

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

17 ation of these hydroxyl groups reduces their inhibitory potency.

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

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

20 ionalities results in essentially no loss of inhibitory potency.

21 nt on the aromatic ring demonstrated maximal inhibitory potency.

22 l homologues led to significant increases in inhibitory potency.

23 ydroxy substituents in order to exhibit high inhibitory potency.

24 the galloyl ester moiety were essential for inhibitory potency.

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

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

27 tional interactions with RT and thus improve inhibitory potency.

28 dity and thus substantially increasing their inhibitory potency.

29 zoic moieties were performed to maximize the inhibitory potency.

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

31 st potent inhibitors was correlated to their inhibitory potency.

32 inverse relationship between processing and inhibitory potency.

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

34 tructure-based optimization led to increased inhibitory potency.

35 he prosthetic group allows the prediction of inhibitory potency.

36 ed that the p27 variants exhibited disparate inhibitory potencies.

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

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

39 hibited a complex response with two separate inhibitory potencies.

40 ecule hLDH5 inhibitors displaying remarkable inhibitory potencies.

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

42 target for DECA analogs with increasing PKC inhibitory potencies.

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

44 acid derivatives with low to high nanomolar inhibitory potencies.

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

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

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

48 51 active site topology underlies their high inhibitory potency, a longer coordination bond between t

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

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

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

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

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

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

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

56 midine were synthesized and tested for their inhibitory potency against bovine trypsin, rat skin tryp

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

58 Compounds 1-6 showed moderate inhibitory potency against DHFR from Pneumocystis carini

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

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

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

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

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

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

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

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

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

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

69 1, compound 3 demonstrated increased growth inhibitory potency against several human tumor cell line

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

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

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

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

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

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

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

77 7-azaindenoisoquinolines can modulate their inhibitory potencies and selectivities vs Top1, Tdp1, an

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

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

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

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

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

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

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

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

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

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

88 9 leads to a substantial improvement of the inhibitory potency and metabolic stability.

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

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

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

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

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

94 Excellent inhibitory potency and selectivity for nNOS over eNOS an

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

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

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

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

99 xylamine peptidomimetics, by virtue of their inhibitory potency and stability, are superior to N-pept

100 ar relationship between the logarithm of the inhibitory potency and the stability of the correspondin

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

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

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

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

105 asing length and/or charge showed increasing inhibitory potency, and detectable heparin inhibition of

106 yl heptyl sulfide (46) was optimum for COX-2 inhibitory potency, and introduction of a triple bond in

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

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

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

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

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

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

113 ptide amides have profound influences on the inhibitory potency as well as on the isoform selectivity

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

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

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

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

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

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

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

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

122 have also demonstrated remarkably different inhibitory potency between influenza A and B neuraminida

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

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

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

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

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

128 Optimization of inhibitory potency can be facilitated by structural info

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

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

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

132 ma-Azidoanilido-2',5'-dd-3'-ATP exhibited an inhibitory potency comparable with that of 2', 5'-dd-3'-

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

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

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

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

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

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

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

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

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

142 sequently used to probe a database of growth-inhibitory potency for 123 "standard agents," which incl

143 to approximately 1246-fold reduction in the inhibitory potency for [125I]DTXk binding and a large de

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

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

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

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

148 ound (1) which was found to have significant inhibitory potency for fXa (Ki = 34 nM).

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

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

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

152 of the 3-substituted-THIQs displayed similar inhibitory potency for PNMT.

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

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

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

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

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

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

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

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

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

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

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

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

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

166 ,4-thiadiazoles and -1,2,3-triazoles with an inhibitory potency in the nanomolar range.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

181 isolated and cellular forms of PKC, the weak inhibitory potency observed against isolated PKC cannot

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

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

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

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

186 Overall, inhibitory potencies of nucleotides at sGCalpha1beta1 ve

187 Enhanced inhibitory potencies of polyvalent over monovalent forms

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

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

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

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

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

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

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

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

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

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

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

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

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

201 The inhibitory potency of both these single agents against V

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

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

204 hese ions have an antagonistic effect on the inhibitory potency of compound 4.

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

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

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

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

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

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

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

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

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

214 The iNOS inhibitory potency of KLYP956 is insensitive to changes

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

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

217 The inhibitory potency of mAChR subtype-selective antagonist

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

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

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

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

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

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

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

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

226 This may explain in part the stronger inhibitory potency of sildenafil for wild-type PDE5 comp

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

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

229 nhibition allowed comparison of the relative inhibitory potency of the compounds on the two proteins'

230 A comparison of the PNMT inhibitory potency of the enantiomers of these 3-fluorom

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

232 The inhibitory potency of the fusion peptides was even great

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

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

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

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

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

238 ccharides per molecule of protein, the molar inhibitory potency of the oligosaccharide inhibitor was

239 The inhibitory potency of the potent protease inhibitor, BIL

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

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

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

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

244 The inhibitory potency of these analogues was greater agains

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

246 The inhibitory potency of these thiol-based compounds agains

247 The inhibitory potency of this family of inhibitors is simil

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

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

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

251 ance of two hydrogen-bonding networks toward inhibitory potency: one between Asn131 and an appropriat

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

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

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

255 ace of a Cbz-leucine moiety, maintained good inhibitory potency relative to the amino acid-based inhi

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

277 AK inhibitory potency was greatest for those compounds with

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

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

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

281 Using full-length RI subunit, the inhibitory potency was reduced by replacing Ile98 with A

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

283 Their inhibitory potencies were comparable to that of casodex

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

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

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

287 Changes in inhibitory potency were generally consistent with the in

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

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

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

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

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

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

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

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

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

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

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

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

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