Results 271 to 280 of about 417,281 (310)

An Examination of IC50 and IC50-Shift Experiments in Assessing Time-Dependent Inhibition of CYP3A4, CYP2D6 and CYP2C9 in Human Liver Microsomes

Drug Metabolism Letters, 2008
The relationship between time-dependent inactivation (TDI) and IC50 is examined using a consolidated method for evaluating CYP450 inhibition during drug discovery. An IC50 fold-shift of >1.5 indicated significant TDI potency. Further, the "shifted IC50" could be used to estimate, the K(I) and TDI potency ratio k(inact)/K(I) to within 2-fold in most ...
Loren M, Berry, Zhiyang, Zhao
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Relationships between Inhibition Constants, Types of Inhibition and IC50: Calculation and Comparison on IC50 of Two Model Tyrosinase Inhibitors

2010 4th International Conference on Bioinformatics and Biomedical Engineering, 2010
Calculating methods for inhibitor concentration (IC50) leading to 50% activity lost (for diphenolase activity) of a novel parabolic competitive inhibitor (the trifluoromethyl-containing 1,2,3-triazole, TF-TA) and a novel mixed inhibitor ([E]-4-(1-imidazoylmethyl) cinnamic acid (ozagrel) were derived on the basis of kinetics of tyrosinase inhibition ...
Hairong Mao, Jiangang Xie, Qimeng Zhang, Xinyu Lu, Shubai Li   +4 more
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Impact of Impurities on IC50 Values of P450 Inhibitors

Drug Metabolism Letters, 2011
During 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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The IC50 Concept Revisited

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, Zhengyin, Yan, Wensheng, Lang, John A, Masucci   +3 more
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Measuring Bioactivity: KI, IC50 and EC50

2011
Which 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, 2014
Calculating 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, Qing Sheng Chen, Men Yi Xu   +2 more
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Bacterial survival rate data of MIC and IC50 tests

2023
plumbagin ...
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Effect of Altered Serum Lipid Concentrations on the IC50 of Halofantrine against Plasmodium Falciparum

Journal of Pharmaceutical Sciences, 1998
Halofantrine (Hf) is a highly lipophilic antimalarial which significantly associates with triglyceride (TG) rich plasma lipoproteins, and this is likely manifest as a decrease in the free fraction of drug. This study assessed the effect of using growth media containing 10% serum containing different concentrations of TG (i.e.
A J, Humberstone, A F, Cowman, J, Horton, W N, Charman   +3 more
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Generation of Dose–Response Curves and Improved IC50s for PARP Inhibitor Nanoformulations

2017
Poly(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, Shifalika, Tangutoori, Srinivas, Sridhar   +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, 2015
To 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, Shifu, Wu, Li, Hou, Xin, Wang, Luanluan, Wang, Yanping, Shi   +5 more
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