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Inhibiting the activity of these efflux pumps has been a well\u2010known strategy of drug design studies in this regard. In this manuscript, our earlier published machine learning models and homology structures of P\u2010gp and NorA were utilized to screen a chemolibrary of 95 in\u2010house chalcone derivatives, identifying two hit compounds, namely, F88 and F90, as potential modulators of both transporters, whose activity on <jats:italic>Staphylococcus aureus<\/jats:italic> strains overexpressing NorA and resistant to ciprofloxacin was subsequently confirmed. 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