Figure 5. [Effect of changing receptor density...]. - Assay Guidance Manual

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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-.

Assay Guidance Manual [Internet].

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Figure 5.

Effect of changing receptor density on response of (A) a high efficacy agonist with comparatively low affinity (K_A = 10 nM) and (B) a lower efficacy agonist with high affinity (K_A = 0.1 nM). (R)_t % = relative receptor density. Simulations are carried out in accordance to the Operational Model (35).

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

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Sum CS, Murphy BJ, Li Z, et al. Pharmacological Characterization of GPCR Agonists, Antagonists, Allosteric Modulators and Biased Ligands from HTS Hits to Lead Optimization. 2019 Nov 1. In: 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-. Figure 5. [Effect of changing receptor density...].
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