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Humans have relied on nature throughout their ages to cater for their basic needs including medicines to cure a wide spectrum of diseases. Plants have formed the basis for sophisticated systems of traditional medicines. For therapeutic agents many of the presently known lead compounds are natural products or their derivatives. Ethnomedicinal studies play a vital role to discover new drugs from indigenous medicinal plants. Green pharmaceuticals are getting popularity and extraordinary importance because vast opportunities for new drug discoveries are provided by the unmatched availability of chemical diversity and natural products either as pure compounds or as homogenous plant extracts. Therefore, in recent years the demand for herbal medicines and several natural products from a variety of plant species is consistently increasing. In spite of being an agricultural country and having different ecological regions, the medicinal plants of Pakistan have not been explored for their secondary metabolites which are responsible for treating different diseases. Although, huge importance of different extracts of medicinal plants from Pakistan have been reported for their different activities such as antimicrobial, anti-cancerouse, antiviral and antioxidant but complete biochemical profiling of these medicinal plants is lacking. LC-MS and GC-MS techniques have been applied in the field of drug discovery from medicinal plants but in Pakistan its success rate is very low in the subject of biochemical profiling. Therefore, such techniques should be used in Pakistan to explore active constituents from medicinal plants which could be used as medicines in future.