A new (and freely available) original research article published ahead-of-print at SLAS Discovery Online describes a new methodology that enables the investigation of a large number of structurally conserved enzymes belonging to the Fe(II)/2-oxoglutarate-dependent dioxygenase superfamily. This superfamily comprises approximately 60 enzymes that are responsible for regulating a wide number of biological processes including epigenetic regulation, DNA/RNA repair and oxygen sensing. Of these, JumonjiC histone lysine demethylases (JMJCs) and prolyl hydroxylases are potential drug targets because of their relevance to human diseases.