Tauopathies are neurodegenerative disorders associated withthe accumulation of abnormal tubulin associated unit (tau)protein in the brain. Tau pathologies include a broad spectrumof diseases, with Alzheimer’s disease (AD) being the mostcommon tauopathy. The pathophysiological mechanisms ofAD are still only partially understood. As a consequence,attempts to establish therapeutic approaches have led tonumerous clinical trial failures and, to date, no curativetreatment is available for AD despite the considerable numberof research programs. Therefore, over the past decade, theaggregation of the tau protein in AD has become a therapeutictarget of interest. In this review, we gather in silico, in vitro, andin vivo methodologies that are relevant to assess compoundstargeting tau aggregation, from early drug design to clinicaltrials.