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Bioorg Med Chem DOI:10.1016/j.bmc.2011.11.071

Unbiased binding assays for discovering small-molecule probes and drugs.

Publication TypeJournal Article
Year of Publication2012
AuthorsKemp, MM, Weïwer, M, Koehler, AN
JournalBioorg Med Chem
Date Published2012 Mar 15
KeywordsAnimals, Drug Discovery, Humans, Mass Spectrometry, Models, Molecular, Protein Binding, Proteins, Small Molecule Libraries, Surface Plasmon Resonance

2011 marks the 10-year anniversary of milestone manuscripts describing drafts of the human genome sequence. Over the past decade, a number of new proteins have been linked to disease-many of which fall into classes that have been historically considered challenging from the perspective of drug discovery. Several of these newly associated proteins lack structural information or strong annotation with regard to function, making development of conventional in vitro functional assays difficult. A recent resurgence in the popularity of simple small molecule binding assays has led to new approaches that do not require knowledge of protein structure or function in advance. Here we briefly review selected methods for executing binding assays that have been used successfully to discover small-molecule probes or drug candidates.


Alternate JournalBioorg. Med. Chem.
PubMed ID22230199