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Compound Screening Methods

Many types of assay are available to be used in HTS protocols to identify inhibitors of PPIs, but a competition assay, in which inhibition of complex formation is measured, is most common. Fluorescence polarization (FPA), fluorescence resonance energy transfer (FRET), enzyme-linked immunosorbent assays (ELISA), and other assay formats have been used. The interacting proteins can be used in their full-length forms though, more frequently only the interacting domains are employed, and if possible the excised interacting peptide is usually preferred. [Pg.9]


Order Material Group of Compound Screening Method Sample Preparation Method... [Pg.314]

Passive controls, process controls, 97-98 Paterson, New Jersey incident, 160-161 Peroxide formers, screening methods, 46-48 Physical processing chemical reactivity hazard, 8-10,11 screening methods, 36, 41—42 worked examples, 128,129 Polymerizing compounds, screening methods, 55... [Pg.198]

As the availability of crystal structures increased in the early 1990s, a number of experimental and computational methods were developed to use the structure of the protein target as a route to discover novel hit compounds. The methods include de novo design, virtual screening, and fragment-based discovery. These developments are covered in more detail in the later chapters of this book, but their main features can be summarized as follows. [Pg.284]

A multi-residue method for 25 selected pesticides including propanil using an SPE disk has also been developed as a rapid screening method for organic contaminants in river, lake and seawater samples. Cig SPE disks are conditioned with 10 mL of acetone for 3 h. Water samples (1L) are allowed to percolate through the disks in order to trap the residues at a fiow rate of 50 mL min under vacuum. Residues trapped in the disks are extracted twice by eluting with 5 mL of dichloromethane-ethyl acetate (1 1, v/v). The more hydrophobic compounds (log/fow>3) seem to show no... [Pg.340]

The most X-ray intensive screening method was described by Card et al. [8] on the design of phosphodiesterase (PDE) inhibitors (Figure 1.7). The authors initially biochemically screened a 20,000 member library of small molecular weight (120-350 MW) core scaffold compounds against 5-PDE isoforms at 200 pM. Multiple isoforms of PDE were used in order to eliminate the number of false positives obtained from the screen. There were 316... [Pg.13]

Test a substantial number of compounds. VS methods generally offer enrichment, but most ranked hit lists contain a significant proportion of false positives. Hitlists should be scaled to 1-5% of the compounds in the virtual library screened. In many real world situations, the computational chemist is being asked to choose lists of compounds representing 0.1% or less of the compounds screened (e.g., the best 100 of 100,000 compounds). Typically, VS methods have been validated considering 1%, 5%, or 10% of the total number of compounds in the VS collection. By following up on more compounds, one increases the probability of impact from VS. [Pg.117]

Li, W., Josephs, J.L., Skiles, G. and Humphreys, W.G. (2008) Metabolite generation via microbial biotransformation with actinomycetes rapid screening methods and synthesis of important human metabolites of two development stage compounds, BMS-587101 and dasatinib. Drug Metabolism and Disposition The Biological Fate of Chemicals, 36, 721-730. [Pg.225]

Due to the availability of chemical libraries, plant and microbial extracts and rapid screening methods lead compounds are rapidly identified. When the structures of PTKs are known optimization by organic synthesis and computer modeling follows. Compounds that successfully pass all the screening tests are ready to be evaluated for clinical trials. [Pg.10]


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Screening-Methode

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