WebApr 13, 2024 · Inhibitor design followed a scaffold-hopping and structure-based strategy of a previously known standard NLRP3 inhibitor MCC950. In an ELISA-based assay, the IL-β inhibitory rate (%), at a dose of 1 µM was found to be 65.2%. This compound was also observed to induce the suppression of caspase-1 activation and IL-β secretion (in THP-1 … WebStructure-based drug design (SBDD) is the design and optimisation of a hit or lead compound using structural information obtained from either X-ray crystallography, cryo-EM or NMR. In any drug research programme, optimisation involves the design of compounds with the right balance of potency, selectivity and ADME properties, but structural …
Fluorescence polarization assays in high-throughput screening …
WebCrystallography can reliably provide the answer to structure related questions, from global folds to atomic details of bonding and the information from X-ray diffraction … WebThrough the combination of the CrystalDirect technology and the CRIMS software, the HTX lab has developed the concept of Online Crystallography: fully automated, remote controlled crystallography … phone on fire 10
High-throughput crystallisation and ligand screening
WebApr 12, 2016 · Design Type(s) macromolecular structure generation objective Measurement Type(s) 3D structure determination assay Technology Type(s) X-ray crystallography assay Factor Type(s) Sample ... X-ray crystallography is the experimental science determining the atomic and molecular structure of a crystal, in which the crystalline structure causes a beam of incident X-rays to diffract into many specific directions. By measuring the angles and intensities of these diffracted beams, a crystallographer can produce a three-dimensional picture of the density of electrons within the crystal. From this elect… WebJan 1, 2015 · The high protein content of the crystallization drop usually requires ligand concentrations in the range of 0.5–5.0 mM. A typical soaking protocol involves the … phone on finger