Determination of Thermodynamic Parameters ΔG and ΔH of a Small Molecule Binding to p38 using MST

Determination of Thermodynamic Parameters ΔG and ΔH of a Small Molecule Binding to p38 using MST

25 Feb 2016

In current drug discovery efforts, hits are discovered by conventional high-throughput or fragment screening campaigns. The only established technology that is capable of measuring the enthalpy of an interaction ΔH directly is ITC. The use of ITC early on in the drug discovery process is frequently hampered by its vast consumption of sample materials. This application note demonstrates that it is possible to gather this thermodynamic information by the use of MicroScale Thermophoresis (MST), taking full advantage of its unique benefits such as tiny sample consumption, and a temperature controlled sample mount.

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High-Throughput ScreeningHigh-throughput screening (HTS) is an automated drug discovery technique for identification of active compounds against a compound library. Use HTS readers and integrated assay preparation / analysis workstations to screen your compounds. Identify active compounds against various HTS libraries, including membranes, proteins and peptides and HTS cell lines. Find the best high-throughput screening products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.High-Content ScreeningHigh-content screening (HCS), also known as high-content analysis (HCA), is a high-throughput technique used in drug discovery to identify substances that alter the phenotype of cells. HCS uses fluorescent microscopic imaging and automated image analysis to investigate cellular events such as apoptosis, cell viability, GPCR activation, oxide production, neurite outgrowth, and cell signaling. Find the best fluorescent labeling reagents, cellular assays, and high-content imaging systems in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Thermal ProcessesHigh ThroughputHigh throughput experiments allow the simultaneous processing of several samples. This parallelization reduces the cost per experiment and increases reproducibility and output volume of data.PharmaceuticalsPharmaceuticals are medicinal drugs used in healthcare to diagnose, prevent, cure and treat illnesses. Pharmaceuticals that are excreted after use appear in wastewater and can have detrimental effects on the environment.Compound ScreeningCompound screening is a method used to discover specific compounds that could be promising candidates for pharmaceutical use. This potential is identified when compounds interact with the target protein during screening and could therefore be carried forward in the drug development process.Small Molecules