ライフサイエンスコーパス: pharmacophore

1 ter forms an essential part of the inhibitor pharmacophore.

2 presented here agree well with the proposed pharmacophore.

3 e that contains the hypothesized Arg-Phe-Phe pharmacophore.

4 domimetic HIV-1 inactivators based on the PT pharmacophore.

5 ulfoquinoline lead compound with the minimal pharmacophore.

6 propyl]piperazi ne (1, PB28) was used as the pharmacophore.

7 AR study using sumanirole (1) as the primary pharmacophore.

8 has furnished a previously unknown antitumor pharmacophore.

9 lic moiety, imidazolidine-4,5-dione, a known pharmacophore.

10 ation of a 1,8-diazaspiro[4.5]dec-3-en-2-one pharmacophore.

11 hitherto unreported mode of action for this pharmacophore.

12 hich contains a Trp-based type II' beta-turn pharmacophore.

13 t binds the cationic moiety of the nicotinic pharmacophore.

14 analogue of moenomycin based on the minimal pharmacophore.

15 naturally occurring FabF-specific antibiotic pharmacophore.

16 he spacer and the point of attachment to the pharmacophore.

17 st with a sulfonium isostere of the ammonium pharmacophore.

18 ere truncated in order to identify a minimum pharmacophore.

19 ore as well as in the amine part outside the pharmacophore.

20 ther antimalarial drugs with the artemisinin pharmacophore.

21 agment-binding sites and their corresponding pharmacophores.

22 ived from canonical or atypical dopaminergic pharmacophores.

23 in the synthesis of diversely functionalized pharmacophores.

24 gned as a combination of quinone/cannabinoid pharmacophores.

25 natural products and a number of established pharmacophores.

26 exhibited a perfect match with known sigma1R pharmacophores.

27 ographic studies and automatically generated pharmacophores.

28 acetylenic moiety that connects the terminal pharmacophores.

29 c ligands would be composed of two identical pharmacophores.

30 ll molecules and definition of corresponding pharmacophores.

31 or the regioselective synthesis of potential pharmacophores.

32 e pyridone and pyridine amides and their key pharmacophores.

33 accessible chiral compounds, containing the pharmacophore 1,3,4-thiadiazoline nucleus joined by a sp

34 y showing that the GSTP1- and MDR-inhibiting pharmacophore 4-chloro-7-nitro-benzoxadiazole was also a

35 The other part of the pharmacophore, a hydrogen bond acceptor, has recently be

36 Queries are specified in terms of a pharmacophore, a spatial arrangement of the essential fe

37 nthesized, based upon a lead neuroprotective pharmacophore acting in part by GABA(A) receptor potenti

38 The coupling of two different pharmacophores afforded compounds 1-12, whose biological

39 em located outside the ethylenediamine kappa pharmacophore allows the fine-tuning of the pharmacodyna

40 eloped in our group, to select 437 shape and pharmacophore analogs of reference kinase inhibitors.

41 unds that conjugate a sigma (sigma) receptor pharmacophore and a nitric oxide (NO) photodonor.

42 ain models, but the lack of knowledge of its pharmacophore and binding site on ASIC3 has impeded deve

43 igned to (a) disrupt the promiscuous binding pharmacophore and diminish off-target interactions and (

44 e/bromodomain inhibitors and generate ad hoc pharmacophore and docking models.

45 A pharmacophore and docking-based virtual screening of com

46 We determined a pharmacophore and generated 1,4-DHPs with IC(50)s for TG

47 that [des-Arg(7)]Dyn A(1-9)-NH2 is a minimum pharmacophore and its modification at the N-terminus lea

48 rather than the pyrazole moiety of the MP-10 pharmacophore and performed in vivo evaluation.

49 oup to interrupt the lipophilic, promiscuous pharmacophore and promote interaction with human nNOS-sp

50 Finally, we developed a pharmacophore and proposed a mechanistic model for how t

51 e ene reaction easily assembles the asmarine pharmacophore and transmits remote stereochemistry to th

52 es of dynamic processes inherent to the OPAC pharmacophores and can help augment our understanding of

53 ing a trans-cyclopropylmethyl linker between pharmacophores and manipulating linker length resulted i

54 e. a combination of static three-dimensional pharmacophores and molecular dynamics-based conformation

55 Merging known pharmacophores and systematic exploration of the structu

56 ar stress and cell viability demonstrate key pharmacophores and their physicochemical properties requ

57 ns are extremely useful in providing protein pharmacophores and to characterize function and structur

58 ere determined to fit a merged sEH/PPARgamma pharmacophore, and structure-activity relationship studi

59 he 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione pharmacophore appears metabolically resistant to O-glucu

60 Through a convergent pharmacophore approach, we synthesized alpha-ketothioami

61 es and to identify which enzyme(s) and which pharmacophores are critical for plasma stability.

62 These independently active pharmacophores are liberated during metabolism, resultin

63 h ASP and AGRP, the hypothesized Arg-Phe-Phe pharmacophores are on exposed beta-hairpin loops.

64 ipids embedding two terminal alkynylcarbinol pharmacophores are reported.

65 nyl pharmacophore, but not the 7-hydroxy Tic pharmacophore, are better tolerated at kappa and mu rece

66 ide, to establish the tetrahydroisoquinoline pharmacophore as an attractive starting point for lead o

67 s in the arylacetamide and amine part of the pharmacophore as well as in the amine part outside the p

68 their utilization in applications such as in pharmacophores, as scaffolds in molecular construction,

69 tion of the N-hydroxyimide two-metal binding pharmacophore at position 4 by carboxamido side chains w

70 eries maintained the potency of the original pharmacophores at both receptors (adenosine A2A and dopa

71 To discover novel RNAP inhibitors, a pharmacophore based on the alignment of described inhibi

72 We generated computational 3D pharmacophores based on data derived by both acoustic an

73 points that can be seamlessly exported to a pharmacophore-based drug discovery workflow.

74 jugating fluorescent dyes to a non-peptidic, pharmacophore-based ligand, based on a molecular modelin

75 class of inhibitors of hQC, resulting from a pharmacophore-based screen.

76 A pharmacophore-based search led to the identification of

77 We present CSD-CrossMiner, a novel tool for pharmacophore-based searches in crystal structure databa

78 The combination of pharmacophore-based virtual screening methods with radio

79 Iterative pharmacophore-based virtual screening was performed to i

80 nformation whereas TAK-779 (with a different pharmacophore) binds to a different high-energy conforma

81 unrelated to the classic phenylethanolamine pharmacophore, binds at the same GluN1/GluN2B dimer inte

82 of types 1-3 consist of three different D2R pharmacophores bound to an affinity-generating lipophili

83 r hand, modifications of the 3-hydroxyphenyl pharmacophore, but not the 7-hydroxy Tic pharmacophore,

84 er demonstrates that bicyclic salicylic acid pharmacophores can be used to deliver PTP inhibitors wit

85 f those substituents, and secondary aromatic pharmacophores can enhance agonist efficacy for the cAMP

86 ity (9- and 5-fold) relative to the original pharmacophore, clozapine.

87 Our work identifies Ile105 as a new pharmacophore component for developing better hCB1R anta

88 This pharmacophore comprises a 6 + 5 fused ring heterocycle l

89 This pharmacophore comprises a central aromatic ring o-substi

90 mate-urea-glutamate or glutamate-urea-lysine pharmacophores conjugated to CIM or TIM chelators were r

91 hesis and modification of novel oligopeptide-pharmacophore conjugates by C-H functionalization.

92 ut inferior to Glide for most systems unless pharmacophore constraints are used; in that case rDock a

93 Our exhaustive analysis includes a pharmacophore contact analysis for over 1900 protein-lig

94 Data from acoustic dispensing generates a pharmacophore containing two hydrophobic features, one h

95 antagonist and identification of the minimum pharmacophore converted the mechanism of inhibition from

96 The acoustic dispensing-derived pharmacophore correctly identified active compounds in a

97 arbonic anhydrase (CA, EC 4.2.1.1) inhibitor pharmacophores, coupled with either ethylene glycol olig

98 -phenylacetamide) was discovered by using 3D pharmacophore database searches and was biologically con

99 y, this method can be applied to both single-pharmacophore DECLs and self-assembled dual-pharmacophor

100 -pharmacophore DECLs and self-assembled dual-pharmacophore DECLs.

101 12 bearing a P3(sp)-tethered tricyclic P3-P1 pharmacophore derived from 3 is described.

102 ein interactions and automatically generated pharmacophores derived from this structural data.

103 A pharmacophore describes the spatial arrangement of the e

104 Using structure-guided pharmacophore design followed by docking, we found two a

105 The computed pharmacophores differ significantly depending upon dispe

106 udy, based on co-crystallization studies and pharmacophore-docking-based virtual screening, we discov

107 esized that focused upon modification in the pharmacophore domain.

108 gamma-turn secondary structure in the ligand pharmacophore domain.

109 rhaps reflecting a lesser importance of this pharmacophore element for alpha7 binding.

110 unds containing redox-directed electrophilic pharmacophores employing the Stress & Toxicity PathwayFi

111 cture, which displayed a possible overlay of pharmacophore features supportive for further design of

112 tic scaffold exploration to design a general pharmacophore for AC inhibition.

113 de the first view of an allosteric inhibitor pharmacophore for alpha(1)-adrenoceptors and mechanistic

114 vide information on the structure and on the pharmacophore for ASIC channel inhibition by mambalgins

115 structure similarities revealed a potential pharmacophore for cartilage targeting.

116 chemokine antagonist and represents a novel pharmacophore for CXCR1/2 antagonism.

117 ronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild

118 hat N-phenylanthranilic acid was the minimal pharmacophore for fenamate activation of Slo2.1 channels

119 amine-based side chain were selected as the pharmacophore for further modification, resulting in met

120 The biotin 1,2,3-triazole provides a novel pharmacophore for future medicinal chemistry programs to

121 g the position of the carboxylic acid, a key pharmacophore for GPR40.

122 ethylsulfonylpyrrole core structure is a new pharmacophore for hGSTA1-1, whereas its derivative 9 may

123 ments that modulate the activity of the core pharmacophore for MC4R and provide a rationale for caref

124 Here, we aimed to generate a new pharmacophore for negative-gating modulation of KCa2/3 c

125 ne and that the structures revealed a common pharmacophore for the three ligands.

126 -based C-ring, which possessed the requisite pharmacophores for binding to protein kinase C (PKC) tog

127 type-specific allosteric modulators, few ECS pharmacophores for class A receptors have been identifie

128 ications about the structural requirement of pharmacophores for further increasing potency and state-

129 ignificant role in providing novel leads and pharmacophores for medicinal chemistry.

130 MenA inhibitors reported here are useful new pharmacophores for the development of selective antimyco

131 Neutron Capture Therapy agents, but also as pharmacophores for the targeting of biologically importa

132 t contain both mu agonist and CB1 antagonist pharmacophores for use as tools to study the functional

133 Herein, the opioid pharmacophore H-Dmt-d-Arg-Aba-beta-Ala-NH2 (7) was linke

134 Endogenous MC4R agonists possess a critical pharmacophore (HFRW), and cyclization of peptide agonist

135 We used a pharmacophore hybridization strategy to combine key stru

136 macophore module to generate natural product-pharmacophore hybrids endowed with unknown biological (p

137 provides tools for constructing and refining pharmacophore hypotheses directly from molecular structu

138 mpound collection based on a minimal binding pharmacophore hypothesis and high-throughput screening.

139 ken together, these results substantiate our pharmacophore hypothesis and validate our ligand-based a

140 xample of how to systematically reengineer a pharmacophore in order to overcome toxicological problem

141 onstrated the importance of the di-2-pyridyl pharmacophore in their activity.

142 cyclopropyldihydrocinnamates to be important pharmacophores in one of our drug discovery programs and

143 With one of those pharmacophores in place at C24, morpholines or carbamate

144 Enamides represent bioactive pharmacophores in various natural products, and have bec

145 ed preliminary SAR for the new AR antagonist pharmacophore, including the finding that the Michael ac

146 roximately 4 A resolution in the presence of pharmacophores, including a potent antagonist.

147 t DEEP-STD NMR can be used to readily obtain pharmacophore information on the protein.

148 Replacement with an optimized P3-P1 pharmacophore interacting to the nonsubstrate S3(sp) cav

149 positive functional evidence linking tropane pharmacophore interaction with the core substrate-bindin

150 ains (chi-space) that constitute the peptide pharmacophore is equally important.

151 The aryl sulfamate pharmacophore is highly versatile, operating via three d

152 This pharmacophore is inconsistent with the X-ray crystallogr

153 Benzoxazolone pharmacophore is present in clinical pharmaceuticals, dr

154 stage infection revealed that the tetraoxane pharmacophore itself is also an excellent liver stage P.

155 on the three-dimensional binding interfaces pharmacophore-like features that act as "selectivity fil

156 ontain mu opioid agonist and CCR5 antagonist pharmacophores linked through homologous spacers (14-24

157 tain mu opioid agonist and mGluR5 antagonist pharmacophores linked through spacers of varying length

158 The three ligands with a similar pharmacophore (Maraviroc, PF-232798, and Aplaviroc) bind

159 ad compounds identified from a metal-binding pharmacophore (MBP) library screen.

160 The binding of a series of metal-binding pharmacophores (MBPs) related to the ligand 1-hydroxypyr

161 Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ

162 Herein, we describe a pharmacophore merging strategy combining the JAK2/FLT3 i

163 Despite the conceptual prevalence of pharmacophore methods for scaffold hopping, a variety of

164 Computational studies resulted in a pharmacophore model and confirmed the SAR results.

165 We developed a pharmacophore model and used the putative bioactive conf

166 ty, compound 34 showed a high fit value to a pharmacophore model derived from the PT-1.

167 The main features of the pharmacophore model developed for this class of sigma(1)

168 ranslating essential binding features into a pharmacophore model followed by in silico screening of t

169 ivator and pharmacoenhancer, we have built a pharmacophore model for a CYP3A4-specific inhibitor.

170 ata formed the basis for a three-dimensional pharmacophore model for GHB ligands, which identified mo

171 data was used to build a CYP2C19 inhibition pharmacophore model for the series.

172 rmone aldosterone, and were used to obtain a pharmacophore model for this enzyme.

173 We developed a pharmacophore model for type II inhibitors that was used

174 entify such a selective binder, we derived a pharmacophore model from the peptide EAVSLKPT, a fragmen

175 This new conorphine KOR agonist class and pharmacophore model provide opportunities for future rat

176 electivity, and stability assays generated a pharmacophore model supporting rational design of highly

177 ed in this study, we developed a preliminary pharmacophore model that confirmed the experimental data

178 othesized binding modes and alignment with a pharmacophore model that we have developed.

179 Specifically, we derived a pharmacophore model to describe inhibitors capable of pr

180 We report a pharmacophore model trained on approximately 200 antagon

181 With these data, a six-feature pharmacophore model was constructed for future drug desi

182 A pharmacophore model was developed and employed to better

183 The pharmacophore model was supported by computational docki

184 from the GSK collection were used to build a pharmacophore model which could be used in the virtual s

185 4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir bi

186 ructural features and formed part of the one pharmacophore model.

187 r further evaluation and optimization of the pharmacophore model.

188 These results provided the basis to use pharmacophore modeling and molecular docking analyses to

189 Pharmacophore modeling and subsequent in vitro screening

190 reening procedure, depending on ligand-based pharmacophore modeling followed by structure-based virtu

191 atives was designed by means of ligand-based pharmacophore modeling in an attempt to identify improve

192 ors (EPIs) library was used for ligand-based pharmacophore modeling studies.

193 Our results, combined with pharmacophore modeling, suggest a molecular basis for si

194 g a combination of druggability simulations, pharmacophore modeling, virtual screening, and in vitro

195 enhanced the original method by including a pharmacophore modelling and information of nucleic acid

196 tor classes in light of recent insights from pharmacophore models and cocrystallization studies.

197 The results were in line with the available pharmacophore models and highlighted that the 1,4-dioxan

198 QSAR models and ligand- and structure-based pharmacophore models and to select the most appropriate

199 In this study, ligand-based pharmacophore models for 17beta-HSD2 inhibitors were con

200 bserved SAR is in agreement with established pharmacophore models for 5-HT(3) ligands and is used for

201 Phe-Tic-(pNO2)DPhe-NH2, revealing new ligand pharmacophore models for melanocortin receptor drug desi

202 Pharmacophore models were developed based on known C3d-l

203 Pharmacophore models were generated and used to perform

204 pes of ligands were prepared on the basis of pharmacophore models.

205 o the fuzziness and overlap of protein-based pharmacophore models.

206 transformations: e.g., the installation of a pharmacophore module to generate natural product-pharmac

207 ems would enable access to a series of known pharmacophores (molecular features responsible for a dru

208 screening of large compound databases using pharmacophores, molecular shape and energy minimization.

209 We show that proteins have evolved diverse pharmacophore motifs for binding the adenine moiety, few

210 S234 by incorporating generally accepted H3R pharmacophore motifs.

211 tified by exploiting an understanding of the pharmacophore of a high throughput screening (HTS)-deriv

212 KPV and KdPT, both of which lack the central pharmacophore of alpha-MSH.

213 rial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of clotrimazole-b

214 as an alkyltriphenylphosphonium moiety to a pharmacophore of interest.

215 s of 35 chemical derivatives, we defined the pharmacophore of LD7, and identified a more potent deriv

216 Collectively, our study identifies a pharmacophore of N-end rule inhibitors, which provides a

217 We have analyzed the protein-binding pharmacophore of NAD and its close analogues in all prot

218 molecule docking indicated that the tropane pharmacophore of RTI 82 was positioned in the central DA

219 istry effort, we optimized the benzothiazole pharmacophore of SKA-31 toward KCa3.1 selectivity and id

220 with the aim of optimizing the benzothiazole pharmacophore of SKA-31 toward KCa3.1 selectivity.

221 of stereo preference and revealing a common pharmacophore of structurally distinct inhibitors of int

222 We identified compounds that match the pharmacophore of the key actin residues of Pfn1-actin in

223 n protocol allows direct access to medicinal pharmacophores of broad utility using feedstock substrat

224 ible to design small peptides based on known pharmacophores of mu-conotoxins without losing their pot

225 eful approach for rapid investigation of the pharmacophores of small inhibitory binding proteins.

226 After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-

227 The structures indicate a critical pharmacophore on the compounds that leads to the distinc

228 These findings provide insight into a pharmacophore on VSDIV through which modulation of inact

229 Structure-guided addition of a metal-binding pharmacophore onto LE retrofragment scaffolds produced l

230 troduce a broad range of carbonyl-containing pharmacophores onto oligopeptides, thus providing a chem

231 a variety of chemical products such as drug pharmacophores or assembling macromolecular structures.

232 ic screening of compound libraries, specific pharmacophores or chemical clusters, and natural product

233 leading to displacement of CB7 from included pharmacophores (or from drug loaded porous particles).

234 y their structures to identify the essential pharmacophore, or make functional group changes to impro

235 Many topological pharmacophore patterns are common between natural produc

236 nist hydrogen bond acceptor of the nicotinic pharmacophore, perhaps reflecting a lesser importance of

237 Quinolines are common pharmacophores present in numerous FDA-approved pharmace

238 and the natural product piperlongumine as a pharmacophore probe.

239 S) hit followed by truncation to its minimal pharmacophore provided an indazole acid lead compound.

240 Intuitive pharmacophore queries describing, among others, protein-

241 dge Structural Database (CSD) using the same pharmacophore query further emphasizes the flexibility o

242 metal-binding motif of these inhibitors as a pharmacophore rather than a "chelator".

243 urbance, could, in principle, allow for easy pharmacophore recognition when the compounds are aligned

244 n network of interactions that stabilize the pharmacophore region of this class of venom peptides.

245 that resemble the critical two-metal binding pharmacophore required for HIV integrase strand transfer

246 The key structural features of the APN pharmacophore required for substrate recognition were el

247 the results provide further insight into the pharmacophore requirements for allosteric inhibition.

248 l approach to define the optimal and minimum pharmacophore responsible for the neuroprotective effect

249 ium, suggesting that the combination of both pharmacophores results in synergistic cardioprotective a

250 king docked hits with our library-derived 3D-pharmacophore revealed two distinct asymmetric binding m

251 corresponding sulfones and sulfonamides, two pharmacophores routinely encountered in drug discovery.

252 we characterized the effects of the minimal pharmacophore RWRWRW-NH2.

253 Hits from the pharmacophore screens were docked to C3d and ranked base

254 Hit expansion by two in silico approaches, pharmacophore search followed by docking, and substructu

255 ounds of the ZINC database using the Pharmer pharmacophore search technology.

256 nt-based screening, reporter gene assay, and pharmacophore search were utilized for the small molecul

257 tified from in silico three-dimensional (3D) pharmacophore searches based on known X-ray structures o

258 Compounds that match a well-defined pharmacophore serve as potential lead compounds for drug

259 Optimization of this pharmacophore should yield FabF-specific antibiotics wit

260 at other nitrogen nucleophiles (e.g., common pharmacophores such as indoles, benzimidazoles, and imid

261 roups to optimize weakly active antimalarial pharmacophores, such as the quinolone scaffold, to yield

262 igned mechanisms of action to identify novel pharmacophores supporting Tnks inhibition.

263 Coupling of two distinct pharmacophores, tacrine and trolox, endowed with differe

264 gning known active compounds onto identified pharmacophore template.

265 ning procedure, which identified a potential pharmacophore that abrogated HBx RNAi suppression activi

266 This discovery defines a new pharmacophore that displayed selective activity toward a

267 f singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clin

268 P inhibitors based upon a cyclic polysulfide pharmacophore that forms a reversible covalent bond with

269 itiated to develop the core aryl O-sulfamate pharmacophore that, over some 20 years, have led to ster

270 Heterobiaryls are important pharmacophores that are challenging to prepare by tradit

271 melanocortin (MSH) and cholecystokinin (CCK) pharmacophores that are connected via a fluorescent labe

272 back-to-back manuscripts describe the first pharmacophores that favorably and selectively interact w

273 d to generate three-dimensional quantitative pharmacophores that identified hydrophobic regions, H-bo

274 ine heterocycle has been found as the active pharmacophore, the results discussed in this work may pr

275 re of the previously reported sulfonyl ester pharmacophore to confer Tdp1 inhibition in this indenois

276 fied a sulfonamide scaffold that served as a pharmacophore to generate inhibitors of Mycobacterium tu

277 e appears that Evasin-1 and -4 use different pharmacophores to bind CC chemokines, with the principal

278 ple, that is, molecular probes, carrying two pharmacophores to simultaneously adopt orthosteric and a

279 ships consistent with a previously published pharmacophore/topological model of ligand-TSPO interacti

280 The structure shows that potent pharmacophore trans-Ned-19 acts allosterically by clampi

281 Conjugation of two 9-aminoacridine pharmacophores, using linkers of varying length, increas

282 ing a flexible linker and a potential second pharmacophore via Ru-catalyzed cross-metathesis and a nu

283 The design through energy-based pharmacophore virtual screening has led to aminocyanopyr

284 To expand the scope of this atypical pharmacophore, we tested the activity profiles of the li

285 aining a pyrrole acidic headgroup and a urea pharmacophore were designed, synthesized, and evaluated

286 er-Tyr-Ser) not considered to be part of the pharmacophore were found to have an influence on the MC4

287 the recently uncovered (S)-dialkynylcarbinol pharmacophore were secured using Carreira's procedure ad

288 e-based fragment growing approach, essential pharmacophores were added.

289 molecules in which the primary and secondary pharmacophores were derived from the D3R-selective antag

290 Pharmacophores were developed that served as a cornersto

291 t and the linker moiety between chelator and pharmacophore, which influence the overall pharmacokinet

292 Compound 1 contains a hydronaphthoquinone pharmacophore with a thioglycolic acid side chain at pos

293 proach, we demonstrate utility of a bivalent pharmacophore with dual activity as a mu/delta opioid ag

294 /3-negative-gating modulator, RA-2, as a new pharmacophore with nanomolar potency.

295 tomers of the pyrazolone ring are the active pharmacophore with the arylazanylpyrazolone analogues.

296 In contrast, the tip-based data suggest a pharmacophore with two hydrogen bond acceptors, one hydr

297 enylacetic acid lactones represent important pharmacophores with heat shock response and immune syste

298 e inhibitors, they are considered to be poor pharmacophores with reduced activity in vivo.

299 ctamase inhibitors containing a boronic acid pharmacophore, with the goal of finding a potent inhibit

300 e destabilizer that seems to occupy a unique pharmacophore within the colchicine site of tubulin.