In Vitro Pharmacological Screening for Potency Selectivity

In Vivo Target Directed

Broad Based In Vivo Screening

Pharmacological Screening


Disease Models




Transgenic Animals



Optimized Lead as Potential Human Therapeutic

Optimized Lead as Potential Human Therapeutic

FIGURE 3.2 Flowchart of GPCR drug discovery research.

of GPCRs. Family C shares structural similarity to the metabotropic glutamate receptor and is characterized by an extracellular ligand-binding domain. It is comprised of 11 liganded and about 5 orphan GPCRs and is represented by the metabotropic glutamate and GABAb receptors. The most recently described and less characterized Family F/S is composed of frizzled and smoothened receptors that play a role in cellular development.6 A comprehensive description of GPCR classification is provided in Chapter 10.

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