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functional in vitro assays for drug discovery

directory of Chem Help ASAP videos: https://www.chemhelpasap.com/youtube/ Biochemical assays are often relatively simple to perform compared to the other in vitro assay types. The classic example an in vitro assay is an enzyme inhibition assay. The assay can be performed in a small volume and would include the enzyme, substrate for the reaction, the inhibitor (which is your potential drug), co-factors required for the reaction, a solution buffer, and perhaps a cosolvent to maintain solubility of the inhibitor. Biochemical assays are only relevant for target-based drug discovery programs as the target protein must be isolated and purified in order to be tested in these assays. These assays are functional assays. In the case of the enzyme inhibition assays, the function is reducing enzymatic activity, which would be reported as an IC50 value. Cellular assays involve living cells. The drug target could be a receptor found on the surface of the cell or perhaps some protein or other molecule within the cell. Examples of observed activity can include ion transport across the cell membrane, cell viability, cell proliferation (as with cancer cell growth), gene expression, antibacterial activity, and metabolic stability. Cellular assays are appropriate for both target-based and phenotypic programs. For example, when developing a new antibiotic, one does not need to know the drug target. You can simply culture bacteria and see whether the molecule kills the bacteria. This would be a functional assay (killing bacteria), and you do not need to know how the molecule works to measure its activity. Activity values in cellular assays are normally reported as EC50 or IC50 values. Tissue-based assays observe the action of a molecule on a tissue. The tissue is generally taken from a living organism, in which case the assay may be called an ex vivo study. Examples of tissue-based assays could include an assay for vasoconstriction (likely performed on arterial tissue), bronchodilation (using lung airway tissue), or psoriasis (using a skin sample). Tissue-based assays are appropriate for target-based or phenotypic programs. The readout may be in the form of EC50 or IC50. In this video we have mostly focused on in vitro assays that measure the efficacy of a compound, primarily on-target efficacy. In vitro assay results are also vital for gaining an early glimpse into the safety properties of a molecule – cellular toxicity or mutagenicity. In vitro assays can also give early information on how a molecule is absorbed and metabolized in the body, which can affect how often or in what manner the drug will be dosed into patients. Therefore, in vitro assays are truly the backbone for an early drug discovery program and guide the discovery team as to which compounds are the most promising and should be advanced into in vivo studies.