The ability of organisms, or individual cells, to react to external chemica
l signals, which are detected and transduced by cell-surface receptors, is
crucial for their survival. These receptors are the targets of the majority
of clinically used medicines. Combinatorial genetics can provide almost un
limited numbers of mutant receptor proteins and combinatorial chemistry can
produce large libraries of potential therapeutic compounds that act on the
se membrane receptors. What is missing for the fundamental understanding of
receptor function and for the discovery of new medicines are efficient pro
cedures to screen both ligand-receptor interactions and the subsequent func
tional consequences. Ultrasensitive fluorescence spectroscopic approaches,
in combination with efficient labelling protocols, offer enormous possibili
ties for highly parallel functional bioanalytics at the micro- and nanomete
r level.