Technologies
term index
Related glossaries include Assays & screening
Chemistry
Drug discovery & development Drug
discovery & development informatics Drug targets
Molecular Imaging
array synthesis:
Form of parallel synthesis in which the reaction
vessels are maintained in a specified spatial distribution, e.g.
the wells of a 96-well plate or pins held in a rack IUPAC COMBINATORIAL
CHEMISTRY Related term spatially addressable.
asymmetric
catalysis: See catalytic asymmetric synthesis
bead:
(Normally spherical) particle of solid support. IUPAC Combinatorial
Chemistry Related term: microspheres; bead arrays Microarrays
biased libraries:
Libraries of compounds (putative drug leads)
that exclude compounds unlikely to interact with particular protein family
structures; these libraries are, therefore, “informed” by structure data. Broader term: combinatorial libraries.
binning:
Approach to classifying the diversity of a set of compounds
by grouping related members in "bins" on the basis of common physical or
structural features. Commonly applied to the analysis of a set for the
completeness of coverage of the desired property space. IUPAC COMBINATORIAL
CHEMISTRY
biomimetic synthesis:
[Clayton
Healthcock's] research has been
concerned with developing strategies for streamlining the synthesis of complex,
naturally occurring compounds. "A particularly powerful strategy," he
said, "is 'biomimetic synthesis,' in which we guess how nature might
assemble a particular molecule and then try to mimic this hypothetical route in
the laboratory." Heathcock's work in the total synthesis of natural
products and the development of new synthetic methodology has been of major
interest to the pharmaceutical industry as well as to the international academic
community. Univ. of California- Berkeley news release "Organic
chemist Clayton H. Heathcock named Dean of College of Chemistry at the
University of California, Berkeley" 8/12/99 http://www.berkeley.edu/news/media/releases/99legacy/8-12-1999.html
building block:
One of a number of interchangeable reagents
which can be used in combinatorial library synthesis, part of the structure of which becomes
incorporated into the final product, i.e. its residue. See also diversity
reagent, monomer. IUPAC Combinatorial Chemistry Related terms: combinatorial chemistry, combinatorial synthesis, diversity, directed library, fully combinatorial, in situ scaffold
formation, monomer, pool/ split, residue, sub- library, unbiased library
catalytic
asymmetric synthesis: The 2001
Nobel Prize in Chemistry will be shared by three scientists who devised
techniques for catalytic asymmetric synthesis -- the use of chiral catalysts to
accelerate the production of single- enantiomer compounds for pharmaceutical use
and a wide range of other applications. Stu Borman, Asymmetric Catalysis Wins,
Chemical & Engineering News 79 (42): Oct. 15, 2001 http://pubs.acs.org/cen/topstory/7942/7942notw1.html
chemical ligand studies:
Drug targets
cleavage:
Process of releasing compound from solid support, thereby
permitting assay or analysis of the compound by solution- phase methods.
Dissolution of the compound following , rather than the cleavage
step itself, may be rate- limiting. IUPAC COMBINATORIAL CHEMISTRY Related term: solid support
click chemistry: Organic chemistry methodology that mimics the modular nature
of various biosynthetic processes. It uses highly reliable and selective
reactions designed to "click" i.e., rapidly join small modular units
together in high yield, without offensive byproducts. In combination with COMBINATORIAL
CHEMISTRY TECHNIQUES, it is used for the synthesis of new compounds
and combinatorial libraries. MeSH 2011
cluster:
Group of compounds which are related by structural or
behavioral properties. Organizing a set of compounds into clusters is often
used in assessing the diversity of those compounds, or in developing SAR
models. See also binning; and principal components analysis,
recursive partitioning (Algorithms).
IUPAC Combinatorial Chemistry
combichem: See combinatorial chemistry
combinatorial biosynthesis:
Of focused libraries of natural products holds great promise for capitalising on hardwon natural product leads. Miniaturisation of screens is required to reduce the cost of screening
combinatorial libraries. Developments in the processes preceding and following synthesis are required to enable the flow of increased numbers of compounds without new bottlenecks developing. The impact of combinatorial chemistry will be greatly enhanced by synergy with ongoing parallel developments in genetic technologies, screening technologies and bioinformatics.
D. Brown "Future pathways for combinatorial chemistry" Molecular Diversity
2 (4): 217- 222 April 1997
combinatorial biology: Bioengineering
& Biomaterials
combinatorial chemistry:
Using a
combinatorial process to prepare sets of compounds from sets of building
blocks. IUPAC Combinatorial Chemistry
In the early 1990's it was believed that combinatorial chemistry would revolutionize the drug discovery industry. Ten years later the route from design and synthesis of compound libraries to identification of lead structures is still long and costly. Synthesis of an almost unlimited number of organic compounds covering as much of chemistry space as possible is no longer the most cost effective and time saving approach to hit identification. Creating libraries, using biological
target structure to inform chemical design, facilitated by quantum advances in structural genomics and computational capabilities, is a smarter, more efficient way to produce good initial
leads. Considering solubility, permeability and other
drug- like properties early in library design and introducing both target and lead structural constraints in
lead development are further ways to ensure more compounds make it to trial. Note that there is not enough matter in the universe to prepare all
possible combinatorial variations. Related terms: combinatorial libraries, diversity,
dynamic combinatorial, chemistry, microtiter plates, molecular diversity, fully combinatorial,
pool/ split Equivalent term?: diversity oriented
synthesis
combinatorial chemistry techniques:
A chemistry- based technology in
which sets of reactions, for solution or solid- phase synthesis, are used
to create molecular libraries for analysis of compounds on a large scale. MeSH,
2000
combinatorial library:
A set of compounds prepared by combinatorial
chemistry. May consist of a collection of pools, or sub- libraries. Its
composition may be described by the chemset notation. IUPAC Combinatorial
Chemistry See
combinatorial library definition in IUPAC Biomolecular Screening Narrower terms: combinatorial library SAR, combinatorial peptide libraries, combinatorial protein
libraries, compound library, hit optimization library, lead discovery library,
biased libraries, combinatorial
antibody libraries, directed libraries, focused
libraries, pool, pool/ split libraries, sub- library, random libraries, unbiased
libraries;
Broader term: library; Related terms: combinatorial synthesis, fully combinatorial, scaffold.
combinatorial organic synthesis:
A key feature of combinatorial
techniques is that compound synthesis can be designed such that a range of
structures can be produced simultaneously as mixtures in the same reaction
vessel or individually in parallel using semi- automated synthesis. The
repetitive nature of the synthetic processes involved in most combinatorial
applications lends itself to automation or semi- automation. This key feature
means that the bench chemist can single- handedly prepare tens, hundreds, or
thousands of compounds of known structures in the time that it would take to
prepare only a few pure entities by orthodox methodology. NCI, CANCER
DRUG DISCOVERY: DIVERSITY GENERATION AND SMART ASSAYS, RFA: CA-97-006, May 9,
1997 http://grants.nih.gov/grants/guide/rfa-files/RFA-CA-97-006.html
combinatorial synthesis:
A process
to prepare large sets of organic compounds by combining sets of building
blocks. IUPAC Medicinal Chemistry
compound
collection: compound
library, compound deck. Set of chemicals that has been assembled and annotated
for easy storage and retrieval and that is available for screening. Note:
Generally consists of compounds synthesized by combinatorial or standard
synthetic methods or purchased from commercial sources, or of natural products
as pure samples. Compounds may be stored in dry powder form, or dissolved at a
fixed concentration in a solvent, such as dimethylsulfoxide. IUPAC Biomolecular
Screening recommendations 2011 Chemical library, compound library, compound
collection: (1) Collection of samples (e.g., chemical compounds, natural
products, over-expression library of a microbe) available for biological
screening. (2) Set of compounds produced through combinatorial chemistry or
other means, which expands around a single core structure or scaffold. IUPAC
Mec Chem 2013
DNA Library Gene
categories See related gene library, genome library
These are different types of libraries.
deconvolute:
To render less complex; Process of optimizing an
activity of interest by fractionating (normally by resynthesis, or by elaborating
a partial library) a pool with some level of the desired activity to give
a set of smaller pools. Repeating this strategy leads to single members
with (ideally) a high level of activity and is termed iterative deconvolution.
IUPAC COMBINATORIAL CHEMISTRY
deconvolution:
Wikipedia http://en.wikipedia.org/wiki/Deconvolution Narrower term: iterative deconvolution
Related term: unbiased library.
discrete sub- structural analysis DSA: See under
privileged substructures
diversity:
The "unrelatedness" of a set of, for example, building
blocks or members of a combinatorial
library, as measured by their properties such as atom connectivity,
physical properties, computational measurements, or bioactivity. IUPAC
Combinatorial Chemistry
The general
understanding of this term is that diversity describes the degree of
dissimilarity within a set of chemical structures. This Opinion article proposes
that this understanding is superficial at best and irrelevant at worst. It is
argued that relevant diversity can only be measured by the application of
external criteria (such as a biological assay), which can discriminate the
different structures by their different behaviour within this external context.
According to this understanding, the diversity of a collection is highly
dependent on the applied criteria. Therefore, a relevant diversity of chemical
structures, per se, does not exist. HJ Roth, "There is no such thing as
'diversity'!" Curr Opin Chem Biol. 9 (3): 293- 295, June 2005
diversity- oriented synthesis:
Commonly referred to as combinatorial
chemical synthesis. is a process by which multiple compounds (chemical
libraries) are generated simultaneously, in a predictable fashion, by using
techniques that involve parallel chemical transformations. Diversity- oriented
synthesis may use solid- or solution- phase reaction techniques. A library
may be small (e.g., a few compounds) or large (e.g., thousands or even millions
of compounds), and it may focus on a narrow or wide range of “diversity
space.” When subjected to high- throughput biological screening.
... Leaders in the pharmaceutical industry (where diversity oriented synthesis
is used extensively) view the limitations of current methodology as a problem of
considerable urgency and see this as a significant impediment to the
identification of drug candidates in new classes and with new mechanisms of
action. NIGMS, Centers of Excellence in Chemical Methodologies and Library
Development, RFA-GM-01-006, June 18, 2001 http://grants.nih.gov/grants/guide/rfa-files/RFA-GM-01-006.html
Related term: combinatorial chemistry
diversity space: The underlying philosophies that need to be
contemplated before embarking on combinatorial studies have strong analogies in computational
chemistry and molecular simulation. This parallel has been explored by Peter
Coveney, until recently at Schlumberger Cambridge Research and now at Queen Mary
and Westfield College, London. The whole idea of searching 'diversity space' is
mirrored by the idea of searching for energy minima within conformational space
in molecular systems. It is therefore clear that there are strong parallels
between stochastic algorithms
and parallel combinatorial search methods. Equivalents to the random search
methods, such as Metropolis Monte Carlo, simulated annealing and genetic
algorithms will all have their part to play in combinatorial problems,
especially those that are particularly complex in nature or
'multivariate' as Coveney likes to call them. Andy Whiting, Discovery and
Diversity, Chembytes E-zine, Royal Society of Chemistry, UK, 1999 http://www.chemsoc.org/chembytes/ezine/1999/whiting.htm
See also under chemical diversity libraries Related term: Assays
diversity screening
diversomers:
Solid- phase chemistry, organic synthesis, and an apparatus for multiple,
simultaneous synthesis have been combined to generate libraries of organic
compounds. Arrays of compounds were synthesized over two to three steps
incorporating chemically diverse building blocks on a polystyrene- based solid
support in a multiple, simultaneous manner. SH Dewitt et. al, Diversomers: an
approach to nonpeptide, nonoligomeric chemical diversity. PNAS Proc Natl Acad
Sci U S A; 90(15): 6909- 6913, Aug. 1, 1993
dynamic combinatorial chemistry:
Is based on the reversible
combination of initial building blocks to form dynamic combinatorial libraries.
It has recently emerged as an efficient strategy to detect and to evaluate
affinity between the library products and a target molecule. Ivan Huc and Régis
Nguyen "Dynamic Combinatorial Chemistry" Combinatorial Chemistry
& High Throughput Screening 4 (1): 53-74, 2001
fragment libraries:
The
synthesis and screening of fragment libraries is at the leading edge of this
trend toward more design-conscious compound library synthesis. Fragment-based
approaches emerged from the understanding that a molecular weight >500
Daltons
typically correlates with poorer oral bioavailability. Furthermore, drug
compounds tend to be even larger than the leads from which they were derived as
a result of lead optimization efforts. Vicki Glaser, When smaller is better 2008
http://www.bio-itworld.com/BioIT_Content.aspx?id=69996&terms=glaser+smaller+is+better
Related term: Assays fragment based screening
Free Wilson model: See under combinatorial
library SAR
fully combinatorial:
Containing, or designed to contain, all
possible combinations of building blocks. Pool/ Split libraries are
generally fully combinatorial while parallel synthesis libraries may not
be. See also reagent efficiency. IUPAC COMBINATORIAL CHEMISTRY gel phase:
Description applied to certain 'solid' supports
which display properties intermediate between solid and liquid phases,
e.g. in the apparent mobility of the support as determined by NMR
spectroscopy. IUPAC COMBINATORIAL CHEMISTRY
gene library,
genomic library: Gene categories
These are different types of libraries.
high throughput
chemistry: Some years ago, combinatorial chemistry
began emerging as a highly efficient means of generating as many compounds as
desired, feeding the demand for compounds as a result of increasingly high
throughput screening. Now there is growing recognition of the need for
greater quality and diversity over sheer numbers, and greater experience is
making it possible to more intelligently design better libraries.
high throughput organic synthesis: It
appears that the real difficulties in drug discovery chemistry continue to be
from high-throughput organic synthesis through purification. New tools, improved
strategies, enhanced techniques, and new methods are beginning to revolutionize
these segments of the drug discovery industry.
I.R. Thermography Infrared thermography:
Screening technique
where the heat of reaction of a multitude of samples is simultaneously
measured. Has been applied in particular to the screening of libraries
of potential catalysts. IUPAC Combinatorial Chemistry in situ
scaffold formation:
Process whereby a scaffold
is formed during library production which contains residues of at least
two building blocks; compare preformed scaffold. IUPAC COMBINATORIAL
CHEMISTRY
iterative deconvolution:
Multi- step application of deconvolution
where successively smaller sub- libraries are prepared and tested to identify
individual active members of a combinatorial library. IUPAC COMBINATORIAL
CHEMISTRY Broader term
deconvolution.
lead, lead likeness:
Assays
& screening
library: An unordered collection of clones (i.e., cloned DNA
from a particular organism), whose relationship to each other can be established
by physical mapping. [DOE] Narrower terms: cDNA libraries, chemical libraries, combinatorial library,
compound libraries, hit optimization library, lead discovery library, biased libraries, combinatorial
antibody libraries, directed libraries, focused
libraries, pool, pool/ split libraries, sub- library, random libraries, unbiased
libraries;
Related terms:
Cell biology; gene
library, genomic library; Sequencing: DNA library
linker:
Bifunctional chemical moiety attaching compound to solid
support or soluble support which can be cleaved to release compounds from
the support. Careful choice of linker allows cleavage to be performed under
appropriate conditions compatible with the stability of the compound and
assay method. IUPAC COMBINATORIAL CHEMISTRY
MPS multiple parallel synthesis: See parallel synthesis
member:
a) specific compound which is included in a library;
b) the uncharacterized physical product of a library synthesis. IUPAC
COMBINATORIAL CHEMISTRY
microwave
chemistry:
Emerging as a popular tool for manipulating chemical synthesis.
molecular diversity:
Covers combinatorial chemistry, combinatorial
libraries, solid- phase synthesis, robotics, molecular graphics: The
visualization and manipulation of three- dimensional representations of
molecules on a graphical display device. IUPAC Medicinal Chemistry Related terms combinatorial chemistry, drug design, high
throughput organic synthesis; Drug discovery
informatics Broader term diversity
monomer:
Member of a building block set which can be repeatedly
incorporated into a library to give a set of compounds of repeating structure;
e.g. amino acids in a peptide library. IUPAC COMBINATORIAL CHEMISTRY
orthogonality:
(a) Property of protecting groups or linkers allowing
removal, modification, or cleavage of one such without affecting others;
(b) pooling strategy whereby library members are incorporated in more than
one pool, and are mixed with a different set of other members in each pool.
Thus a hit results in two or more active pools with only one member in
common. IUPAC COMBINATORIAL CHEMISTRY
One meaning of orthogonal is independent of disjoint, with
no overlap.
parallel synthesis:
Strategy whereby sets of discrete compounds
are prepared simultaneously in arrays of physically separate reaction vessels
or microcompartments without interchange of intermediates during the assembly
process. Contrast pool/ split. IUPAC COMBINATORIAL CHEMISTRY
peptide library:
A collection of cloned peptides, or chemically
synthesized peptides, frequently consisting of all possible combinations of
amino acids making up an n-amino acid peptide. MeSH, 1997
Used by Mario Geysen (1985 +) to map peptide
epitopes or antigenic sites on proteins. Numerous strategies have
developed over the past 20 years to synthesize mixtures of thousands to
millions of peptides and allow selection of those with the desired activities.
Related term: combinatorial peptide libraries
pool:
(a) A sub-library; (b) process of combining and mixing
library components or sub- libraries. See pool/ split. IUPAC COMBINATORIAL
CHEMISTRY pool/split:
Also split/ pool; split & mix; divide, couple,
recombine; portion/ mix. Strategy for assembly of a combinatorial library.
The solid support is divided into portions, each of which is subjected
to reaction with a single building block. Pooling of these portions results
in a single batch of solid support bearing a mixture of components. Repetition
of the divide, couple, recombine processes results in a library where each
discrete particle of solid support carries a single library member, and
the number of members is equal to the product of the number of building
blocks incorporated at each step (i.e. fully combinatorial) IUPAC COMBINATORIAL
CHEMISTRY preformed scaffold:
A scaffold which is incorporated into the
library as a unit. Compare in situ scaffold. IUPAC COMBINATORIAL
CHEMISTRY
Broader term: scaffold.
privileged structure:
Substructural feature which confers desirable
(often drug- like) properties on compounds containing that feature. Often
consists of a semi- rigid scaffold which is able to present multiple hydrophobic
residues without undergoing hydrophobic collapse. IUPAC COMBINATORIAL
CHEMISTRY property space:
Multidimensional representation of a set of compounds
in which the axes represent quantifiable properties such as molecular weight, CLogP, molar refractivity, etc., and individual compounds are represented
by a vector or set of coordinates. IUPAC COMBINATORIAL CHEMISTRY
random library: See unbiased library.
IUPAC Combinatorial Chemistry residue:
(a) Portion of a chemical structure which can be identified
as being derived from a particular building block, such as the alanine
residue in the peptide (b) portion of a building block which is incorporated
into the final product but is not part of the scaffold. IUPAC Combinatorial
Chemistry Compare residue
Proteins resin: Insoluble polymeric material which allows ready separation from
liquid-phase materials by filtration; can be used to carry library members (i.e.
solid
support) or reagents, or to trap excess reagents or reaction by-products
(see scavenger
resin) IUPAC Combinatorial
retrosynthetic analysis:
A synthesis is planned in reverse, beginning
with the final product. The investigator identifies a reaction that could afford
a particular product and then deduces the structure of the required starting
material. This process is repeated until a set of easily- procured starting
materials is identified that can be converted, by using an appropriate sequence
of reactions, to a complex target structure. NIGMS, Centers of Excellence
in Chemical Methodologies and Library Development, RFA-GM-01-006, June 18, 2001 http://grants.nih.gov/grants/guide/rfa-files/RFA-GM-01-006.html
Compare: chemical diversity libraries
ring-closing metathesis RCM; ring- opening metathesis polymerizaton
ROMP: See under metathesis strategies
SAR Cheminformatics
structure activity relationship SAR
scaffold:
Core portion of a molecule common to all members of
a combinatorial library. IUPAC Combinatorial Chemistry This is
different from the scaffold defined in the Sequencing
Narrower terms:
in situ scaffold, preformed scaffold. Chemistry molecular
scaffold
small
molecule libraries:
Large collections of small
molecules (molecular weight about 600 or less),
of similar or diverse nature which are used for high-throughput screening
analysis of the gene function, protein interaction, cellular processing,
biochemical pathways, or other chemical interactions. MeSH 2008
SPE: See solid phase extraction.
solid-phase extraction:
Method for sample purification whereby
either the desired or undesired components of a mixture have preferential
affinity for a solid material. Adding the mixture to the solid material
then allows facile separation of the desired material by filtration. Related
terms sequestration- enabling reagent and scavenger resin.
IUPAC Combinatorial Chemistry
solid phase synthesis:
In solid- phase approaches, pin or bead
techniques permit the synthesis of different molecules on each pin (i.e.,
"one molecule- one bead"). The products of solid- phase synthesis can
be cleaved from the backbone matrix for solution screening (which is essential
when the screening target is a cell), or the most active molecules displayed on
the polymer surface may be detected using molecular targets
(receptor, enzyme, antibody) pre- tagged with a means of detection (visible color, fluorescence,
radioactivity, chromophore, etc.) and then isolated and identified. NCI, CANCER
DRUG DISCOVERY: DIVERSITY GENERATION AND SMART ASSAYS, RFA: CA-97-006, May 9,
1997 http://grants.nih.gov/grants/guide/rfa-files/RFA-CA-97-006.html
Related term: high throughput
purification Narrower term: solid phase- traceless
solid support: Insoluble, functionalized, polymeric material
to which library members or reagents may be attached (often via a linker)
allowing them to be readily separated (by filtration, centrifugation, etc.)
from excess reagents, soluble reaction by- products, or solvents. IUPAC
Combinatorial chemistry Related terms: bead, high throughput organic synthesis, cleavage,
gel phase, linker, pool/ split, resin, sort and combine
soluble support:
An attachment, common to all library members,
which renders the library components soluble under conditions for library
synthesis, but which can be readily separated from most other soluble components
when desired by some simple physical process. This process has been termed
liquid- phase chemistry. Examples of soluble supports include linear polymers
such as poly(ethylene glycol), dendrimers, or fluorinated compounds
which selectively partition into fluorine- rich solvents (see fluorous synthesis).
IUPAC COMBINATORIAL CHEMISTRY
solution phase synthesis:
Solution techniques utilize methods
essentially similar to standard methods for the synthesis of single compounds,
except that instead of utilizing one well- defined reaction partner of each type
per reaction, mixtures of several known reaction partners are utilized as building
blocks, thus resulting in mixtures of analogs. The type of the chosen
chemical reaction and the number of reactants depend on the nature of the
desired structures. These mixtures may not be purified elaborately but are
directly subjected to screening against the desired target (e.g., receptor,
enzyme, antibody, cell). The chemistry is then
repeated a few times in batches using different but well defined mixtures of
reaction partners, and the products isolated and screened. In order to identify
the leads, the chemistry is repeated several times using fewer reaction partners
in each run, and the products are screened. This deconvolution process is
repeated until the most potent lead is identified. NCI, CANCER DRUG
DISCOVERY: DIVERSITY GENERATION AND SMART ASSAYS, RFA: CA-97-006, May 9, 1997 http://grants.nih.gov/grants/guide/rfa-files/RFA-CA-97-006.html
Related term: high throughput purification
sort and combine:
Use of directed sorting to facilitate library
assembly. Related to pool/ split protocol but more commonly applied to macroscopic
solid supports (such as pins and related carriers) where each library member
is found on only one, or a small number of carriers. IUPAC COMBINATORIAL
CHEMISTRY
space: Narrower terms: chemical space, diversity space, property
space. Related term: spatially addressable
spatially addressable:
Having the ability to identify at least
part of the structure of a library component or pool by noting its physical
location in an array. IUPAC COMBINATORIAL CHEMISTRY
split/pool: See pool/split
split samples: See under aliquot.
sub-library: See also pool. A subset of a combinatorial
library, physically separate from the rest of the library, generally with
one or more fixed building block. IUPAC COMBINATORIAL CHEMISTRY synthesis:
Narrower terms: biomimetic synthesis, combinatorial biosynthesis,
combinatorial synthesis, high throughput organic synthesis,
multi- component reactions, organic
synthesis, parallel synthesis, solid phase synthesis, solution phase synthesis,
thematic libraries- synthesis; array synthesis Related term: retrosynthetic
analysis
target-oriented synthesis TOS:
Modern drug discovery often involves screening
small molecules for their ability to bind to a preselected protein target.
Target- oriented syntheses of these small molecules, individually or as
collections (focused libraries), can be planned effectively with retrosynthetic
analysis. Drug discovery can also involve screening small molecules for their
ability to modulate a biological pathway in cells or organisms, without regard
for any particular protein target. This process is likely to benefit in the
future from an evolving forward analysis of synthetic pathways, used in
diversity- oriented synthesis, that leads to structurally complex and diverse
small molecules. One goal of diversity- oriented syntheses is to synthesize
efficiently a collection of small molecules capable of perturbing any
disease-related biological pathway, leading eventually to the identification of
therapeutic protein targets capable of being modulated by small molecules.
Stuart l. Schreiber, Target- oriented and diversity- oriented organic synthesis
in drug discovery, Science 287(5460): 1964- 1969, Mar 17, 2000
tether: See linker.
unbiased library:
Library prepared from building blocks and scaffold
chosen without bias towards a particular target. IUPAC COMBINATORIAL CHEMISTRY
Libraries & Synthesis resources
ChemDiv Glossary , 2018
http://www.chemdiv.com/resources/chemistry-glossary/
Combichem Glossary, Combinatorial Chemistry Review,
Professor Oleg Larin, 2004-2016 http://www.combichemistry.com/medical-chemistry-glossary.html
IUPAC
Glossary of terms in Biomolecular Screening 2011 http://iupac.org/publications/pac/83/5/1129/
IUPAC
Combinatorial International Union of Pure and Applied Chemistry, Glossary of Terms Used in Combinatorial Chemistry, D.
Maclean, J. J. Baldwin, V.T. Ivanov, Y. Kato, A. Shaw, P. Schneider, and E. M.. Gordon, Pure
Appl. Chem., Vol. 71, No. 12, pp.
2349- 2365, 1999. 100+ definitions. http://www.iupac.org/reports/1999/7112maclean/
IUPAC
Glossary of terms in combinatorial chemistry, revision of the 1999 Technical
Report,
https://www.degruyter.com/view/j/pac.1999.71.issue-12/pac199971122349/pac199971122349.xml
How
to look for other unfamiliar terms
IUPAC definitions are reprinted with the permission of
the International Union of Pure and Applied Chemistry.
It is easy to lose sight of
the numbers involved in combinatorial chemistry and useful to recall the
old story of the inventor of chess and his patron, the emperor of China.
The emperor had so fallen in love with his new game that he offered the
inventor a reward of anything he wanted in the kingdom. "Just one grain
of rice on the first square of the chessboard, and two on the next."
"That's all?" "Yes, and four
grains of rice on the third square, and so on." This seemingly modest request
was quickly granted. But the grains of rice required for each square ultimately required more rice fields than would cover twice
the surface of the Earth, oceans included.
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