The ability to rapidly survey and compare gene expression levels between re
ference and test samples is moving the drug discovery process towards a mor
e genomic orientation. The success of the Human Genome Project and related
private genomics initiatives, combined with new technologies to probe, imag
e and access expression data, are responsible for this transformation. This
article reviews the history, status and future direction of high-throughpu
t gene expression analysis. It describes classical approaches, explains the
development of methods such as differential display for discovering novel
genes, and discusses how microarray technology is exploiting collections of
known sequences to pinpoint drug targets.