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Pre-equilibrated combinatorial libraries based on multivalent peptide acyl hydrazones were used to find potent inhibitors of β-tryptase. The best inhibitors bind to the protein surface, and inhibit β-tryptase with nanomolar affinity ( K  i  ca.  10 nM) and high selectivity in a reversible and non-competitive way.

Discovery of potent inhibitors of human β-tryptase from pre-equilibrated dynamic combinatorial libraries