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1 ent values for Km that depend on the product inhibition constant.
2 o inhibit the kinase activity with a similar inhibition constant.
3 r normally depends on prior knowledge of the inhibition constant.
4 polypeptides resulted in a decrease in each inhibition constant.
5 I(1)=0 and I(2)=E+K, where K is the apparent inhibition constant.
6 of inhibition by compounds with subnanomolar inhibition constants.
7 while inhibiting thrombin at low micromolar inhibition constants.
8 ro binding to the enzyme active site and for inhibition constants.
9 R2 = 0.89) between computed and experimental inhibition constants.
10 V, I47T, and S94A, have little impact on the inhibition constants.
11 ugh free energy simulations and experimental inhibition constants.
12 lysis of the temperature dependence of their inhibition constants.
13 bitors featuring label-free determination of inhibition constants.
14 at least one hCA isozyme with low nanomolar inhibition constants.
15 , enzyme specificity constants, and apparent inhibition constants.
16 ons between SL3 RNA and NCp7 with micromolar inhibition constants.
17 he compounds possessed subnanomolar apparent inhibition constants.
18 inhibitor to ATP and OSB with low micromolar inhibition constants.
19 -ADAM displayed high affinity to SERT sites (inhibition constant = 0.081 nmol/L, using membrane prepa
23 ed subnanomolar binding affinities for SERT (inhibition constants, 0.51 and 0.76 nM, respectively), h
26 e.g. XK216, the least potent inhibitor (Ki (inhibition constant) = 4.70 nM), possesses the smallest
27 ase and phosphatase activities with the same inhibition constant; a point mutation that weakens phosp
30 nfluence the accurate calculation of ISO-1's inhibition constant, an MIF inhibitor that is broadly us
33 erivatives display subnanomolar or picomolar inhibition constants and high selectivity for the tumor-
34 on of a known inhibitor of shikimate kinase; inhibition constants and mode of inhibition were accurat
35 ytes, a clear correlation between the enzyme inhibition constants and P. falciparum inhibition concen
37 s curves and yields estimates of the in vivo inhibition constants and the rate constants for eliminat
39 ("true") values of the uninhibited velocity, inhibition constant, and total enzyme concentration were
40 num inhibit blood coagulation with picomolar inhibition constants, and have been targeted as novel ph
41 ic properties (steady and pre-steady state), inhibition constants, and thermodynamic properties of E:
42 rresponds to the rate of inhibition, and the inhibition constants are in the micromolar range but var
43 is disrupted, enzyme kinetic parameters and inhibition constants are similar to those obtained for s
46 thod with respect to the detectable range of inhibition constants (both classical and tight-binding)
47 both human and mouse FAP with low nanomolar inhibition constants but does not inhibit close FAP homo
48 lass, CM026 and CM037, exhibit submicromolar inhibition constants but have different mechanisms of in
53 ive site concentration and the tight-binding inhibition constant can be determined simultaneously fro
54 ) and of (55)Fe(2+) transport by Mn(2+) gave inhibition constants comparable to each cation's K(a) fo
55 correlate with their Michaelis constants or inhibition constants, consistent with their exerting an
56 omplexation was very similar to the relative inhibition constant derived from solution phase kinetics
57 rocedure for the estimation of tight-binding inhibition constants directly from dose-response data.
62 inhibitor (TFPI) that critically reduces the inhibition constant for FXa to below the plasma concentr
65 sm correctly predicts the observed change in inhibition constant for the complex of A77003 and the re
66 o disrupt enzyme-inhibitor interactions, and inhibition constants for 13 inhibitors were determined t
69 pable of easily measuring kinetic values and inhibition constants for a range of natural and nonnatur
70 ared to CA II (6.2 vs 6.9), as well as lower inhibition constants for a variety of anions, including
73 say, we examined the correlation between the inhibition constants for enzyme activity (Ki values) and
74 most potent compounds display sub-nanomolar inhibition constants for factor Xa and show greater than
76 most potent compounds (33, 35, and 37) have inhibition constants for human FXa of 3.9, 2.3, and 0.83
78 s of thioxolone yielded similar estimates of inhibition constants for most compounds, although two co
82 nication so that the apparent activation and inhibition constants for regulators depended upon each o
84 uring the SKIE on the noncompetitive (mixed) inhibition constants for the C-terminal reaction product
85 re, and we suggest that the magnitude of the inhibition constants for the dead-end inhibitors may pro
90 onship between these two enzymes and similar inhibition constants for these two enzymes with several
91 tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the
93 This method was also used to determine the inhibition constant (IC50 value) for the competitive inh
94 200 microM NMDA-evoked responses with a 50% inhibition constant (IC50) of approximately 1 microM at
95 e from Arabidopsis thaliana (GST-rAtKS) with inhibition constants (IC50 = 1 x 10-7 and 1 x 10-6 M) si
97 e DELI tended to produce higher half-maximal inhibition constants (IC50s) than FCM, with an overall b
98 e, produced an 8-fold increase in the enzyme inhibition constant in contrast with the abolition of ca
99 PEP and OAA in order to achieve a micromolar inhibition constant in the absence of direct coordinatio
101 of hits by rapid and accurate measurement of inhibition constants in continuous assays, and pre-stead
102 utants resemble those of PR(WT) with similar inhibition constants in good agreement with the antivira
103 three of the phosphate inhibitors displayed inhibition constants in the 4-5 nM range, indicating tha
105 osaccharomyces pombe lumazine synthase, with inhibition constants in the low nanomolar to subnanomola
106 ncompetitive or linear mixed inhibitors with inhibition constants in the millimolar concentration ran
108 o the development of potent antibiotics with inhibition constants in the single-digit picomolar range
109 ymes (I, II, IX, and XII) with submicromolar inhibition constants, including perfluorooctanoic acid,
111 d sensitive to adefovir diphosphate with the inhibition constants increasing by 1.3-fold and 2.2-fold
112 alogues were further analyzed for their P-gp inhibition constant, intrinsic toxicity, and potency to
114 he hydration constant for AcLF-13CHO and its inhibition constant, its K(d) is 16 microM, 8000-fold la
116 ashed PSII (1.5-5 mM), whereas values of the inhibition constant K(I) in intact PSII (9-17 mM) were l
117 enzyme in a fast equilibrium, defined by the inhibition constant K(i), to form an initial reversible
118 olecular tongs to date were obtained with an inhibition constant K(id) of 50 nM for PR and 80 nM for
119 protocol for the rapid determination of the inhibition constant ( K (i)) for competitive inhibitors
122 itor in this series (72, SE170) has a potent inhibition constant (K(i) = 0.3 nM), is 350-fold selecti
124 a series of quinuclidine derivatives with an inhibition constant (K(i)) < 6 nmol/L (33 pmol/L for 4)
125 icated that orforglipron is a high-affinity [inhibition constant (K(i)) = 1 nM], selective ligand of
126 g activity on G4 DNA but not duplex DNA: the inhibition constant (K(i)) for NMM inhibition of G4 DNA
128 d into the PAP active site with a calculated inhibition constant (K(i)) more favorable than that of t
129 phthaloyl-L- ornithine] was found to have an inhibition constant (K(i)) of 0.35 +/- 0.10 pM against h
130 lyses were active and inhibited YprA with an inhibition constant (K(i)) of 1.7 nM, and the addition o
131 is a slow-binding inhibitor with an overall inhibition constant (K(i)) of 2 nM and a dissociation ra
132 ] cluster to an apo-acceptor protein with an inhibition constant (K(i)) of 200 mum, which reflects th
137 ivity was Na(+) sensitive with a significant inhibition constant (K(i)) shift observed following K(+)
138 dinium iodide (11), which had an equilibrium inhibition constant (K(i)) value of 219 nM at human A(3)
140 ficient inhibitor of all three kinases, with inhibition constant (K(i)) values similar to or lower th
143 alf-maximal inhibitory concentration (IC50), inhibition constant (K(i)), and the inhibition mechanism
144 g competitive component [i.e., a competitive inhibition constant (K(ic)) of 0.12 +/- 0.02 mM and an u
146 binding MMP-3 compared with WT TIMP-1, with inhibition constants (K(i) ) in the low picomolar range.
147 xhibited strong inhibition, with equilibrium inhibition constants (K(i) values) from 0.38 to 1.7 micr
149 inhibition by triclosan, with uncompetitive inhibition constants (K(i)') of 0.18+/-0.01 and 0.12+/-
151 -1) protease (enzyme, E) that values for the inhibition constants (K(i)) could not be determined by c
152 fy the mechanism of inhibition and determine inhibition constants (K(i)) for a weak competitive inhib
154 riments with [(3)H]adenosine, P2 transporter inhibition constants (K(i)) have been determined for a d
155 cosine and dansyl-L-asparagine from HSA with inhibition constants (K(i)) of 85 +/- 3 microM and 1500
157 c resistance to famciclovir, we compared the inhibition constants (K(i)) of penciclovir triphosphate
158 inases (TIMPs), we have assessed equilibrium inhibition constants (K(i)) of putative physiological in
162 noesterase activity of lambdaPP, albeit with inhibition constants (K(i)) that range over 5 orders of
163 that association rate constants (k(on)) and inhibition constants (K(i)) were similar to those for ot
169 icin tetraloop gave slow-onset tight-binding inhibition constants (K(i)*) of 2.3-8.7 nM under physiol
171 trated picomolar affinity at D(2)RHigh (mean inhibition constant [K(i)] = 85 pM) and excellent select
173 n acceptors, although the value of the slope inhibition constant, K(is), was 25-30-fold greater with
175 r solution over the range 0-9% increases the inhibition constants, K(i), by up to an order of magnitu
176 mbinant delta-dendrotoxin has a half-maximal inhibition constant (Kd) of 150 nM when applied to ROMK1
180 dard error of the mean (SEM), n = 16) and an inhibition constant Ki of 0.59 mM +/- 0.07 (mean +/- SEM
181 e well correlated with literature values for inhibition constants Ki and kcat/Km for the correspondin
182 tations in its interface, that has an MMP-14 inhibition constant (Ki ) of 0.9 pm, the strongest MMP-1
184 For the viral enzyme the logarithm of the inhibition constant (Ki) correlated with neither the log
185 he enzymatic activity of scuPA/suPAR with an inhibition constant (Ki) equal to 1.9 microM, increased
186 ), k(cat), and k(cat)/K(m)) and the apparent inhibition constant (Ki) for adenosine 5'-diphosphate (A
187 e second-order rate constant (ki/Ki) and the inhibition constant (Ki) for inhibition of human alpha-t
189 functional assays in rabbit vas deferens and inhibition constant (Ki) of 0.02 nM measured in radiolig
191 -350 nM, in good agreement with the in vitro inhibition constant (Ki) of 6.3 nM and regional Bmax in
192 fected cells is inhibited by lipoate with an inhibition constant (Ki) of approximately 5 microM.
195 efficiency were used in conjunction with the inhibition constant (Ki) to evaluate the advantage of th
196 atechuate is a competitive inhibitor and the inhibition constant (Ki) was obtained as 0.23 muM but do
198 In this manner, the value of the microtubule inhibition constant (Ki), which is the binding constant
199 he previously noted correlations between the inhibition constants (Ki 170-1.2 microM) and the chemica
200 valid for the calculation of the competitive inhibition constants (Ki values) for inhibitors in the F
203 to change Asp-49 and Phe-142 to alanine, and inhibition constants (Ki) for both mutants were determin
204 en constant (Km) for 3beta-HSD substrate and inhibition constants (Ki) for epostane and trilostane to
206 ent monoglutamate against DHFR (7.0 nM), the inhibition constants (Ki) for the parent monoglutamate a
207 d resistance to lamivudine triphosphate with inhibition constants (Ki) increased by 8.0-fold, 19.6-fo
208 al/mol and - 12.1 kcal/mol and corresponding inhibition constants (Ki) of 1.13 nM and 1.33 nM, respec
209 amin K-dependent proteins by determining the inhibition constants (Ki) toward a factor IX propeptide/
211 idylprolyl isomerase activity of FKBP12 with inhibition constants (Ki,app) approaching 0.10 microM.
212 , we identified 30 potential lead compounds (inhibition constant, Ki= 1-32 microM) representing nine
216 rmed experimentally by measuring competitive inhibition constants KI2 for propidium and tacrine, inhi
217 howing how the variation in apparent product inhibition constants (Kii) can be used to predict the ra
218 tion by thioacetyl-lysine peptide yielded an inhibition constant (Kis) of 0.017 microM, 280-fold lowe
219 with acetyl-lysine substrate and yielded an inhibition constant (Kis) of 4.8 microM, similar to its
222 nversely, the determination of tight-binding inhibition constants normally requires prior knowledge o
223 potent inhibitor 8 binds to plasmin with an inhibition constant of 0.2 nM, whereas K(i) values >1 mu
224 was NFLP, which had a competitive (with P5C) inhibition constant of 100 mum The structure of PYCR1 co
225 ting divalent inhibitor exhibits an in vitro inhibition constant of 165 pM against the BoNT/A catalyt
226 binding affinity of nifrolidine exhibited an inhibition constant of 2.89 nmol/L for the alpha(4)beta(
228 catalytic/disintegrin domain with an overall inhibition constant of 280 +/- 34 nM and high specificit
229 bited by a recombinant Kunitz domain with an inhibition constant of 344 +/- 37 pM versus 422 +/- 33 p
230 a-1-fucose (GDP-2F-Fuc) was observed with an inhibition constant of 4.2 microM which represents the m
231 Ia is inhibited by protease nexin II with an inhibition constant of 437 +/- 62 pM, compared to 229 +/
233 xed-type inhibitor of Gsp synthetase with an inhibition constant of 6 microM for the inhibitor bindin
235 n kinetic analysis shows that RAY1216 has an inhibition constant of 8.4 nM and suggests that it disso
241 petitive inhibition versus cysteine, with an inhibition constant of approximately 306 nM versus ATP.
242 everely impaired carboxylase binding with an inhibition constant of at least 200,000-fold weaker than
243 These findings were corroborated when the inhibition constant of binding to Bcl-XL was determined
247 s (IC(50) = 2.4 nM) correlated well with the inhibition constant of MII[H9A;L15A] for [(125)I]alpha-c
248 a two-carbon linker led to a decrease of the inhibition constant of the resulting compound by 3 order
249 und to be competitive inhibitors of AAP with inhibition constants of 0.24 and 4.6 mM, respectively.
251 hibition of transport on mOat3 in cells with inhibition constants of 198 +/- 39, 558 +/- 75, 745 +/-
252 variable substrate with apparent competitive inhibition constants of 2.1, 36, and 29 microM, respecti
254 For o1R binding, OF-NB1 and MF-NB1 exhibited inhibition constants of 410 and 2,700 nM, respectively.
255 sigma1R binding, OF-NB1 and MF-NB1 exhibited inhibition constants of 410 and 2,700 nM, respectively.
256 0 A, respectively, and measured the apparent inhibition constants of 5G9 on a panel of TF mutants.
257 udine-resistant hepatitis B virus (HBV), the inhibition constants of adefovir diphosphate and lamivud
258 two descriptors explained 90% of variance in inhibition constants of all 28 inhibitors, ranging from
259 as used for measuring binding affinities and inhibition constants of BACH1 peptides and small molecul
260 moa assay was successfully used to determine inhibition constants of both bosutinib and dasatinib.
262 a DDAH-1 selective inhibitor, as seen in the inhibition constants of N5-(1-iminoethyl)-, N5-(1-iminop
263 device was used for the MS determination of inhibition constants of several inhibitors of HIV-1 prot
265 comparison with the nucleoside derivatives, inhibition constants of their corresponding 5'-phosphory
267 avir, and reduced dimer stability, while the inhibition constants of two peptide analog inhibitors we
269 using equilibrium dialysis and to the K(i) (inhibition constant) of 6.7 microm for CoA obtained from
270 ncubation interval significantly affects the inhibition constants on a structurally dependent basis.
271 rgets, pairs that have binding affinities or inhibition constants ranging from subnanomolar to low mi
274 presence of Ca(2+) with a stoichiometry and inhibition constant similar to those for the binding to
275 luco- and galacto-configured inhibitors, the inhibition constants suggested preferred recognition of
276 Furthermore, the similarity of amiloride inhibition constants suggested that the channel in neona
277 , normal SKIE values were observed for these inhibition constants, suggesting that both kinetic and t
278 s to members of the RNase A superfamily with inhibition constants that span 10 orders of magnitude.
279 losed conformer seen with DEER and enzymatic inhibition constants, thermodynamic dissociation constan
280 sing clustering of experimentally determined inhibition constants (to define specificity classes of k
281 In contrast to studies with AAC(6')-Ii, the inhibition constants toward AAC(6')-Iy are essentially i
283 racer with high affinity for aggregated tau (inhibition constant value, 8 nM) and high (>/=500x) in v
284 ts with a relatively wide range of estimated inhibition constant values (K(i) values = 169-1147 micro
287 The most potent, compound 3, had a picomolar inhibition constant versus BChE due to strong cation-pi
289 P,4-P), having the most favorable calculated inhibition constant, was synthesized and characterized.
292 ed by tert-butyl hydroperoxide, and apparent inhibition constants were determined to be between 33 an
294 s were used in preparing (86)Y- 4: - 6: PSMA inhibition constants were evaluated by competitive bindi
300 was examined in more detail by measuring the inhibition constants with Torpedo AChE, fetal bovine ser