NAAA-IN-1 (Compound 1) is a potent and selective inhibitor of NAAA with an IC 50 of 7 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-1 has the potential for the research of inflammation and pain.