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ligand binding affinity. The interaction of most ligands with their
binding sites can be characterized in terms of a
binding affinity. In general, high-affinity
ligand binding results from greater intermolecular force between the
ligand and its receptor while low-affinity
ligand binding involves less intermolecular force between the
ligand and its receptor.
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binding affinity calculated by recent scoring functions, the protein-
ligand interaction and compound 3D structure information are used for analysis. Kwok et al. (1994) used fluorescence anisotropy measurements to define the equilibrium
binding parameters of the phosphoCREB:CBP interaction and reported that CBP can activate transcription through a region in its C terminus. The activation domain of CBP interacts directly with the basal transcription factor TFIIB ().As TFIIB interacts with the TATA-box-
binding protein TBP1 (), a …
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receptor ligand binding assay allows for the study and simple imaging of cell surface receptors for research and diagnostic applications.
Receptor ligand binding is used in drug development applications to identify blocking antibodies or inhibitors that can modulate downstream signaling events, and is often used to screen for drugs that target hormone and neurotransmitter activity.
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binding affinity datapoints (pK i) plotted against the maximal pK i for a set of 442 protein targets from BindingDB plotted as green circles. The correlation is weak (R 2 = 0.11) reinforcing the concept of differential ligandability.For example, dihydrofolate reductase protease has high maximal pK i for small effort (red circle) whereas carbonic anhydrase I has ...
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