Traditional drug screening relies on monolayer cell culture, which is not always predictive of natural physiological state, where the complex microenvironment consists of various cell types that interact in 3-dimensional structures. As the cost of drug development rises, there is increasing pressure for more predictive in vitro models for functional analysis and compound characterization. Cambridge Healthtech Institute’s Inaugural Physiologically-Relevant Cellular Models for Drug Discovery meeting will focus on the latest advances in 3-D cellular models, complex co-culture systems, and simple model organisms for functional analysis studies and compound screening/characterization.