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Markossian S, Grossman A, Arkin M, et al., editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.

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Assay Guidance Manual [Internet].

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Figure 9. . Characteristic patterns of agonist concentration curves in a dose-shift assay in the presence of different pharmacological agents.

Figure 9.

Characteristic patterns of agonist concentration curves in a dose-shift assay in the presence of different pharmacological agents. Figure 9A–C: (9A) competitive antagonist under equilibrium condition, (9B) competitive antagonist in hemi-equilibrium, and (9C) non-competitive antagonists/modulators. Figures 9D–F: Allosteric modulator that decreases affinity which does not affect agonist efficacy (9D), reduces agonist efficacy (9E), or enhances efficacy (9F). Figures 9G–I: Allosteric modulator that increases affinity which does not affect agonist efficacy (9G), reduces agonist efficacy (9H), or enhance efficacy (9I).

From: Pharmacological Characterization of GPCR Agonists, Antagonists, Allosteric Modulators and Biased Ligands from HTS Hits to Lead Optimization

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