To search for the pharmacological agents for potential GBM therapeutics, we employed an ultra-high-throughput screen (uHTS) in a 1536-well plate format and testing funnels to screen and identify the small molecules, which differentially inhibited the growth of U87MG/EGFRvIII cells against U87MG (PTEN mutant) parental cells. The gene discussed is PTEN; the disease is glioblastoma.