GPCRProfiler Allosteric Services
Allosteric compounds are an emerging class of exciting GPCR therapeutics. Compared to traditional orthosteric compounds, allosteric compounds interact at novel sites on a receptor and have a wider range of possible activities, including the ability to modulate the activity of a receptor’s native ligand. As such, allosteric modulators, including both positive allosteric modulators (PAMs) and negative allosteric modulators (NAMs) have a promising benefit of allowing the body to retain physiologic regulation of receptor activation.
Many properties of allosteric modulators make them challenging molecules to screen and profile. For example, traditional equilibrium binding assays often fail to identify allosteric modulators because allosteric compounds don’t directly compete for the radiolabeled orthosteric compound. Millipore’s functional based service, however, does not rely on competition between molecules. It instead measures the functional interaction of compound with the receptor. Therefore, functional based assays can readily detecting allosteric modulators as well as traditional orthosteric compounds.
Download the data sheet: GPCRProfiler Allosteric Services |
AllostericProfiler Services
Millipore’s allosteric selectivity-profiling service, AllostericProfiler, was developed to identify a wide range of off-target activities for allosteric compounds.
Why Profile Allosteric compounds?
- Allosteric compounds are hoped to be more selective compounds as they interact at non-traditional binding sites. However, beyond limited analysis within distinct GPCR ligand families, the general selectivity for allosteric compounds remains unknown.
- Identifying off-targets interactions is an important step in drug discovery as many GPCRs have been found to be liability targets in addition to therapeutic targets.
About AllostericProfiler
Extending the capabilities of our GPCRProfiler services, the first service to offer standard cell-based functional assays, AllostericProfiler service was developed to address the challenges of allosteric modulator detection. By monitoring 3 different activities (agonist, PAM or antagonists/NAM), AllostericProfiler captures any off-target activates of allosteric compounds – whether the off-target activity is the same or different than the compound’s activity at the primary GPCR target.
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AllostericScreen Service
AllostericScreener service was developed to screen compound libraries to identify new compounds having positive allosteric modulator (PAM) activity for a target of interest. AllostericScreener service employs an assay design that is similar, but slightly modified, to our standard GPCRProfiler services. This assay design can identify both agonist and PAM activities. Therefore, you can discriminate hits that either activate the receptor directly, modulate the receptor’s activity or those that have a mixture of these activities.
Receptor List
A complete list of the targets is available: GPCRProfiler Services.
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