Exorbitant expenses, lengthy development periods, and a high incidence of drug candidate attrition plague the conventional pharmaceutical R&D pipeline---a problem sometimes referred to as ``Eroom's Law.'' By radically reorganizing the discovery process, generative artificial intelligence (AI), which has emerged as a transformational force, promises to buck this tendency. Through data synthesis on key performance metrics, this review offers a thorough analysis of the effects of AI-enhanced methodologies. We explore how a new set of tools is changing the paradigm from experimental screening to in silico design. These tools include graph neural networks (GNNs)—a class of neural architectures... More >