Fragment-based lead discovery
- Fragment-based lead discovery
Fragment-based lead discovery (FBLD) is a method used for finding lead compounds as part of the drug discovery process. It is based on identifying small chemical fragments, which may bind only weakly to the biological target, and then growing them or combining them to produce a lead with a higher affinity. FBLD can be compared with high-throughput screening (HTS). In HTS, libraries with up to millions of compounds, with molecular weights of around 500 Da, are screened, and nanomolar binding affinities are sought. In contrast, in the early phase of FBLD, libraries with a few thousand compounds with molecular weights of around 200 Da may be screened, and millimolar affinities can be considered useful.
References
*cite journal |journal=Chemical and Engineering News |date=July 21, 2008 |volume 86 |issue=29 |pages=15-23 |title=Piece By Piece |author=Sara Everts
Wikimedia Foundation.
2010.
Look at other dictionaries:
Drug discovery — In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are discovered and/or designed. In the past most drugs have been discovered either by identifying the active ingredient from traditional… … Wikipedia
Drug discovery hit to lead — Early drug discovery involves several phases from target identification to preclinical development. The identification of small molecule modulators of protein function and the process of transforming these into high content lead series are key… … Wikipedia
Discovery and development of renin inhibitors — Renin inhibitors are antihypertensive drugs that inhibit the first and rate limiting step of the renin angiotensin aldosterone system (RAAS). Since the 1970s scientists have been trying to develop potent inhibitors with acceptable oral… … Wikipedia
Discovery and development of small molecule c-Met inhibitors — The c Met (mesenchymal epithelial transition) tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis and angiogenesis.[1] c Met is a receptor tyrosine kinase,[2] which can cause a wide variety of different cancers, such… … Wikipedia
Astex — Infobox Company company name = Astex Therapeutics company company type = Private foundation = 1999 location = Cambridge, United Kingdom key people = Leon Bushara(CEO) Harren Jhoti (CSO) Martin Buckland (CBO) industry = Pharmaceutical products =… … Wikipedia
Drug design — Not to be confused with Designer drug. Drug design, also sometimes referred to as rational drug design or structure based drug design, is the inventive process of finding new medications based on the knowledge of the biological target.[1] The… … Wikipedia
DNA-encoded chemical library — DNA encoded chemical libraries (DEL) are a new technology for the synthesis and screening of collections of chemical compounds of unprecedented size and quality. DEL represents an advance in medicinal chemistry which bridges the fields of… … Wikipedia
Chris Abell — Christopher Abell, MA, PhD (born 11 November 1957)[1] is a British biological chemist. As of 2009, he is a professor of biological chemistry at the Department of Chemistry of the University of Cambridge and Todd Hamied Fellow of Christ s… … Wikipedia
Druggability — is a term used in drug discovery to describe the suitability of a protein or protein complex to be targeted by a drug or drug like molecule, in a way that this interaction will alter the proteins function and correct disease causing behavior. The … Wikipedia
Docking (molecular) — Docking glossary • Receptor or host or lock – The receiving molecule, most commonly a protein or other biopolymer. • Ligand or guest or key – The complementary partner molecule which binds to the receptor. Ligands are most often small molecules… … Wikipedia
