The invention provides a human KLK2 which is associated with the hematological disorders, cancer, cardiovascular diseases, inflammatory diseases, neurological disorders, reproduction disorders and urological disorders. The invention also provides assays for the identification of compounds useful in the treatment or prevention of hematological disorders, cancer, cardiovascular diseases, inflammatory diseases, neurological disorders, reproduction disorders and urological disorders. The invention also features compounds which bind to and/or activate or inhibit the activity of KLK2 as well as pharmaceutical compositions comprising such compounds.