Contact Points
Statement of Need and Purpose: We need to assess the global selectivity of our lead D3 dopamine receptor negative allosteric modulator candidates. Modifying the parent compound to improve certain pharmacological characteristics could potentially also decrease selectivity. We need to know if our new lead candidates are still extremely selective for the D3 dopamine receptor which would reduce potential off-target effects when using the compounds in vitro or in vivo.
Background Information and Objective: We are developing a new D3R-selective negative allosteric modulator scaffold for use as an in vitro or in vivo probe, or as a potential clinical lead compound. To accomplish this, we have set out to design highly selective D3 dopamine receptor negative allosteric modulators that do not have off target activity at other closely related or unrelated GPCRs. We used this screen from Eurofins DiscoverX when we first began developing this chemical scaffold. Since then, we have optimized the compound into higher potency lead compounds. We need to screen our lead candidates for off-target activity to ensure that any modification to the drug did not alter its selectivity. We would like to have Eurofins DiscoverX run their gpcrMAX panel in agonist and antagonist modalities. They are the only source for this assay and will run 168 G protein-coupled receptors at one concentration in duplicate. This will provide us with information on the selectivity of our leads at a broad array of receptors and predict if there will be off-target side effects. We will use this data to compare back to the parent compound which was run in the gpcrMAX panel many years ago. To run this assay ourselves is prohibitively expensive due to the need to buy 168 cell lines and would require months of work.
Purchase Description: gpcrMAX panel, gpcrMAX GPCR Functional Panel, DiscoverX, Eurofins DiscoverX, 86-0115.
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