CB1R Allosteric modulator 1,25

Determining Allosteric Modulator Mechanism of Action: Integration of Radioligand Binding and Functional Assay Data

binding and functional assay datasets in concert to elucidate allosteric modulator mechanism of action.

Quantifying Allosteric Modulation of G Protein-Coupled Receptors

-receptor complex. If the concentration-response curve of the agonist is measured in the absence and presence of a range of concentrations of the allosteric modulator, then it is always possible to estimate the affinity constant

Quantification of Allosteric Interactions at G Protein–Coupled Receptors Using Radioligand Binding Assays

interactions involve the simultaneous binding of two ligands to the same receptor. An allosteric modulator causes a conformational change in the receptor protein that yields a change in the binding or signaling of an orthosteric agent, i.e., an agonist