Abstract: More attention has been paid to the pioneering drug innovation since the new millennium, while the creation space of fast-followed drugs is shrinking due to the serious risks observed in the clinical phases fo llowing marketing. Innovative drug discovery aiming at the brand new target is dependent on the breakthrough in basic biology, followed by chemical biology, and medicinal chemistry. This roadmap requires harmonious environment and free exploration atmosphere, while mandatory planning unlikely accelerates drug discovery. This article concisely analyzes several critical aspects of current status of drug discovery.