Plants are the source of different drugs belonging to various therapeutic categories like antidiabetics, antispasmodics, antihypertensive, anticancer, antidepressants, antimicrobials, etc. Plants are used to treat various ailments and these plants have been used by different individuals and tribals worldwide. Use of plants to treat various ailments have also been mentioned in Ayurveda. Along these lines, various researchers are involved in isolating and assessing different bioactive molecules, to be isolated from various plant sources. Isolation of bioactive molecules is not an easy task for researchers. This review gives a focus on extraction and phytochemical screening methods along with their merits and demerits.