Small molecule drug discovery combinatorial chemistry

The identification of compounds with a desired property is a central pursuit in science. In the field of drug discovery combinatorial chemistry has played an increasingly important role for identification and optimization of drug leads which target therapeutically important biomolecules. For the successful implementation of combinatorial methods, new and innovative synthesis methods have been developed. Additionally, novel conceptual approaches to the design of compounds have been pursued to more efficiently generate libraries of small molecules. 

Hermkens, P.H.H. and Muller, G., The impact of combinatorial chemistry on drug discovery, in Ernst Schering Research Foundation Workshop Small Molecule-Protein Interactions, Vol. 42, 2003, pp. 201-220. 

In chemogenomics and drug discovery, the most challenging task is to find small molecule modulators of protein function that specifically modulate the protein function of interest. Combinatorial chemistry has emerged as a powerful tool to address this problem by generation of large compound... 

---