The field of structural biology is being revolutionized by the rapid advancements in both light and electron microscopies. Combined with X-ray crystallography and NMR spectroscopy, the range of biophysical measurements now extends from the atomic to the cellular level. The amount and spatiotemporal resolution of the resulting data provides an unprecedented opportunity for modeling of large systems, including the whole cell. Application of these experimental and computational advances towards the G protein-coupled receptor (GPCR) signaling field creates enormous opportunities for advancing drug discovery. In this symposium, we will combine imaging across the scales as it applies to drug discovery, from molecular to cellular to organ level, with an example focus on GPCRs. Data integration across the scales, underpinned by varied types of modeling, is one of the most challenging areas of both basic and applied science today, and the focus of many of the top labs around the world.