96-well drug plate setup diagram for functional binding assays. The functional binding plate is designed to contain two buffer controls (Column 1 and 11), one agonist control (Column 2), one antagonist control (Column 12) and 2 compounds (Columns 2 - 10). Agonists are subjected to full concentration-response (eight serial drug dilutions are made in quadruplicate) to determine their efficacy and potency. Antagonists are subjected to full concentration-response (eight serial drug dilutions are made in quadruplicate) studies to determine IC50 values against EC50 to EC80 concentrations of a reference agonist. Results are normalized and transformed to percentage values. For agonists, the reference agonist activity at 10 μM is set as 100% and basal activity with buffer as 0%. For antagonists, the basal activity with buffer only is set as 100% inhibition and the activity of the EC80 of the reference agonist as 0% inhibition. For allosteric potentiators, the activity of the EC20 of a reference agonist is set as 0% potentiation.