Therapeutics in any modality to combat Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infections are in urgent demand across the entire world as the Coronavirus Disease 2019 (COVID-19) pandemic continues to interrupt the well-being of human life. Without clinical therapeutics available for any of the human coronaviruses, a key starting point is to focus on target-based high-throughput screening (HTS) to reveal potent anti-SARS-CoV-2 hit-to-leads that are safe to human cells.