Ribbon drawings of exemplar structures from each of the four classes of membrane‐bound proteins of pharmacologic interest, viewed parallel to the lipid bilayer (shaded grey rectangle). (a) GPCR (PDB 5vai)36: GLP1‐R (glucagon‐like peptide‐1 receptor, active conformation in green) bound to GLP1 (red) and heterotrimeric G‐protein (blue, yellow, and magenta). (b) VGIC (PDB 6j8i)106: Nav1.7 (green), beta1 and beta2 (blue), bound to inhibitor tetrodotoxin (yellow). Voltage‐sensing helices are shown in red. (c) LGIC (PDB 5uow)72: NMDA receptor (blue, green, and red) bound to channel blocker MK‐801 (magenta). An antibody Fab (grey) was used in the structure determination. (d) Transporter (PDB 6o2p)85: CFTR (cystic fibrosis transmembrane conductance regulator (blue) bound to ivacaftor (yellow), which interacts with a long transmembrane helix involved in gating (red)