Antibody drug conjugation is a promising approach to improve the clinical outcomes of cancer therapy. Antibody Drug Conjugates (ADCs) allow for targeted delivery of the cytotoxic agents to the tumor cells and can diminish dose limiting toxicity that is mostly associated with unwanted effects of cancer therapeutics on normal cells. Conjugation of monoclonal antibodies (mAbs) with small cytotoxic molecules can improve the pharmacokinetic profile of the small molecule and minimize its off-target toxicity, and as a result improve therapeutic outcomes. Antibody, payload and the linker form the three major components of an ADC, and each have been extensively studied to improve the ADCs properties. Conjugation chemistry strategy is a major aspect when designing ADCs, and can have a profound impact on the potency and safety of the developed agent. Linker technology and choice of payload are other important critical attributes. The current book chapter covers an extensive evaluation of chemistry adapted for conjugation practice and various linkers that are commonly used for ADC development, in addition to a brief discussion about the payloads that have been subjected to antibody drug conjugation.