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Impact of Impurities on IC50 Values of P450 Inhibitors
Drug Metabolism Letters, 2011During early drug discovery, the synthetic pathways for test compounds are not well defined and impurities in the test compounds are inevitable. Compounds undergo serial screening tests at this stage to assess their biological activities and drug-like properties.
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Bioorganic & Medicinal Chemistry, 2021
Recent years have seen a resurgence in drug discovery efforts aimed at the identification of covalent inhibitors which has led to an explosion of literature reports in this area and most importantly new approved therapies. These reports and breakthroughs highlight the significant investments made across the industry in SAR campaigns to optimize ...
Atli Thorarensen +8 more
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Recent years have seen a resurgence in drug discovery efforts aimed at the identification of covalent inhibitors which has led to an explosion of literature reports in this area and most importantly new approved therapies. These reports and breakthroughs highlight the significant investments made across the industry in SAR campaigns to optimize ...
Atli Thorarensen +8 more
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Current Topics in Medicinal Chemistry, 2012
A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds.
Gary W, Caldwell +3 more
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A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds.
Gary W, Caldwell +3 more
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Measuring Bioactivity: KI, IC50 and EC50
2011Which quantity permits a characterisation of the performance of a bioactive molecule? How can a test be created so as to detect the effect of a molecule on a given target? Are there any general rules to respect? The design of a test is a complex problem dealt with in chapter 3; here we emphasise that, above all, the target must be a limiting factor in ...
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Computing Method and Test on IC50 Value of Tyrosinase Inhibition
Advanced Materials Research, 2014Calculating methods of inhibitor concentration leading to yield 50% inhibition (IC50) of competitive inhibitor, noncompetitive inhibitor and mixed inhibitor were proposed on the basis of kinetics of enzyme inhibition, and were applied to calculate IC50 value of concerned compounds, such as cinnamic acid, cinnamaldehyde, benzoic acid and et al.
Sheng Zhao Gong +2 more
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Generation of Dose–Response Curves and Improved IC50s for PARP Inhibitor Nanoformulations
2017Poly(ADP-ribose) polymerase (PARP) inhibitors that target DNA damage repair pathways in cancer cells are increasingly attractive for treating several cancers. Determining the half maximal inhibitory concentration (IC50) of these molecular inhibitors in cell lines is crucial for further dosing for in vivo experiments. Typically these in vitro assays are
Paige, Baldwin +2 more
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[Study on cytotoxicity tests of medical devices based on IC50].
Zhongguo yi liao qi xie za zhi = Chinese journal of medical instrumentation, 2015To discuss IC50 application in cytotoxicity tests of medical devices, we firstly investigated the vibrating condition and endpoint of MTT method specified in ISO 10993-5: 2009. Furthermore, we demonstrated the application of IC50 in the result evaluation of MTT method.
Chenghu, Liu +5 more
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IC50 evaluation is critically dependent on the protocol used for measurement
Journal of Pharmacological and Toxicological Methods, 2020Julio Gomis-Tena Dolz +7 more
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