Improving success rates for lead generation using affinity binding technologies.
Affinity technologies have been applied at several stages of the drug discovery process, ranging from target identification and purification to the identification of preclinical candidates. The detection of ligand-macromolecule interactions in lead discovery is the best studied and most powerful of these techniques. Although affinity methods have been in widespread use for about a decade, only recently have many reports emerged on their utility. Primary affinity screens of large libraries of small molecules or fragments have begun to produce results for challenging targets. Furthermore, in secondary assays affinity methods are opening new avenues to tackle important medicinal chemistry tasks.
Makara
Gergely M
GM
Merck Research Laboratories, Merck & Co., RY80Y-325, Rahway, New Jersey 07065, USA. gergely_makara@merck.com
Athanasopoulos
John
J
D000818:Animals; D001681:Biological Assay / Q000379:methods / Q000639:trends; D020650:Combinatorial Chemistry Techniques / Q000379:methods / Q000639:trends; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000639:trends; D006801:Humans; D008024:Ligands; D013329:Structure-Activity Relationship
D008024:Ligands