The use of high-throughput screening for early stage drug discovery im
poses several constraints on the format of assays for therapeutic targ
ets of interest. Homogeneous cell-free assays based on energy transfer
, fluorescence polarization spectroscopy or fluorescence correlation s
pectroscopy provide the sensitivity, ease, speed and resistance to int
erference from test compounds needed to function in a high-throughput
screening mode. Similarly, novel cell-based assays are now being adapt
ed for high-throughput screening, providing for in situ analysis of a
variety of biological targets. Finally, recent advances in assay minia
turization mark a transition to ultra high-throughput screening, ensur
ing that identification of lead compounds will not be the rate-limitin
g step in finding new drugs.