Related Experiment Video
Updated: Oct 17, 2026

Autoradiography as a Simple and Powerful Method for Visualization and Characterization of Pharmacological Targets
Published on: March 12, 2019
Displacement analysis of binding inhomogeneities in crude extracts of receptors
Abstract:
Guidelines are given to distinguish different kinds of binding inhomogeneities of non-radiolabeled ligands in crude extracts of receptors if an appropriate 'binding analogue' of the displacers is available in radiolabeled form. Three minimal models for the simplest types of binding inhomogeneities are analysed theoretically. These models include a cooperative system (with two interacting sites on the same receptor molecule) and two non-cooperative systems (one of them with a single-site receptor having two conformational states in equilibrium and the other with two single-site receptors independent of each other). In certain cases one can distinguish these systems experimentally. Furthermore, if a group of displacers is already classified according to the above models, then dissociation constants can be determined. The quantitative comparison of these displacers on the basis of their dissociation constants is more appropriate (e.g. in Quantitative Structure Activity Relationship studies) than on the basis of their ID50 and Ki values or Hill coefficients, which is often done.
More Related Videos
10:17Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library
Published on: January 14, 2020
09:09Removal and Replacement of Endogenous Ligands from Lipid-Bound Proteins and Allergens
Published on: February 24, 2021
Related Concept Videos
Conserved Binding Sites
Binding sites are often located in large pockets, and if their location on a protein’s surface is unknown, it can be predicted using various approaches. The energetic method computationally analyses the...
The Equilibrium Binding Constant and Binding Strength
Drug-Receptor Interactions
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Quantitative Aspects of Drug-Receptor Interaction
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
Factors Affecting Protein-Drug Binding: Drug Interactions
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...