Binding kinetics (BK), an often overlooked key aspect of the broader concept of drug mechanism of action (MOA), is increasingly recognized as a springboard from pharmacokinetics (PK) to pharmacodynamics, and as a critical differentiator and predictor for drug efficacy and safety. Just as greater attention to PK issues has helped reduce the attrition of drugs tested in clinical trials, the emerging paradigm shift from primarily affinity/potency-emphasized to a more holistic BK-perceptive and MOA-informed approach is expected to further enhance the success of drug discovery and development. This perspective attempts to envision what this new approach looks like when proper emphasis is placed on BK and MOA in designing better and best in class drugs.