Isothermal Titration Calorimetry (ITC)
At Sygnature Discovery we are experts in applying multiple techniques to characterize ligand binding, including the use of Isothermal Titration Calorimetry (ITC). ITC is considered to be the gold standard quantitative Biophysical Technique for characterizing the binding interaction between two or more molecules in solution.
ITC is unique amongst biophysical techniques in that it fully characterises the thermodynamics of ligand-target binding, enabling the determination of: KD, reaction stoichiometry, enthalpy (∆H) and entropy (ΔS). This information can be used to characterise the ligand-target interaction, as both hit confirmation and to guide the progression of a Hit-to-Lead for your program with Sygnature Discovery.
Figure A: ITC thermograms generated for the injection of A) tool compound JQ1 and B) Sygnature Discovery fragment into a sample of BRD3 and the corresponding fitted curves used to determine KD values for the interactions.