West Nile virus (WNV) is a mosquito-borne virus member of the Flavivirus genus that includes also dengue virus (DENV), Japanese encephalitis virus (JEV), tick-borne encephalitis virus (TBEV), yellow fever virus (YFV), and Zika virus (ZIKV); it is a relevant zoonotic pathogen that has overcome geographical barriers and is one of the most important causative agents of human viral encephalitis. WNV is a small, enveloped, spherical particle of 40–50 nm diameter with single-stranded, positive-sense RNA genomes. Although no licensed vaccine or approved therapeutic options are available and WNV inhibitors still have not been developed into approved drugs, recent progress has led to the identification of several small molecules with inhibitory activity at low micromolar or even nanomolar concentrations. These compounds can be classified based on the specific targets they act upon, from entry of the virus into the host cell to its translation and replication, and also as allosteric and non-allosteric inhibitors. In addition, the nonstructural proteins play a crucial role in the viral replication cycle, which is why a number of inhibitors are designed to target these proteins. Overall, however, it is important to note that for many WNV inhibitors, the exact mechanism of action is not yet fully understood. In this review, we summarize recent developments in the field including the identification of molecules tested in in vivo models and potential broad-spectrum anti-flavivirus inhibitors.