Although rapidly developing genome sequencing technology has helped to reveal potential disease-causing proteins, for chemists it does not mean that an effective drug will be designed. Approved drugs currently cover only 10% of the human therapeutic proteome, probably because a classic chemical inhibitor requires a well-defined hydrophobic binding site on the surface of target protein, like growth factor receptors and protein kinase. Transcription factors and other proteins lacking a defined active site are still hardly druggable.