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From a database of 10\u2009369\u2009180 compounds, we identified 85\u2009021 natural product\u2010derived phenolic fragments, which were virtually O\u2010phosphorylated and screened for in silico binding to the STAT3 SH2 domain. Nine screening hits were then synthesized, eight of which showed a degree of in vitro inhibition of STAT3. After analysis of its selectivity profile, the most potent inhibitor was then developed to Stafia\u20101, the first small molecule shown to preferentially inhibit the STAT family member STAT5a over the close homologue STAT5b. 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