Understanding how the binding of a single ligand influences the behaviour of a membrane protein target is a fundamental concept of both molecular pharmacology and drug discovery. My research examines this question in detail using a multitude of approaches from ligand docking and Molecular Dynamics simulations in computational biology for drug discovery, through to using microfluidics and building ‘organs on a chip’ to define the actions of drugs on cells in a realistic setting. This multifaceted approach is well suited to study this rich and complex topic and will aid the future development of new drugs and novel treatments for disease.