GPCR Profiling Services with Off-target Panels
In the process of developing new pharmaceuticals, the benefits and drawbacks of drugs having off-target effects have come to light. In complicated in vivo systems, off-target activities are more frequently seen as harmful to the drug development process. In order to prevent those risks early in the drug discovery process, there is interest in knowing the factors influencing drug promiscuity. GPCRs are oftentimes "off-targets" for medications, exhibiting unexpected interactions that may have life-threatening or unexpected therapeutic side effects. A lot of GPCRs are profiled before compounds are tested in human clinical trials since GPCRs are often off-targets for medications that target kinases and other non-GPCR molecular targets.
Testing for activity against a panel of comparable targets from the same and closely related super families of proteins is the simplest way to obtain selectivity data on a set of hits. These studies are necessary to determine whether a compound is feasible to pursue as a lead candidate. These investigations also quickly reveal compounds with a non-selective mechanism of action, as these drugs frequently exhibit pleiotropic effects on a whole protein family. Creative Biolabs has established GPCR off-target panels with 44-targets and 90-targets to help our clients discover potential off-target risk in the lead compound optimization stage.
Advantage of Our Off-target Panels
- Functional assays
Our off-target panels make use of functional tests based on cells. They accurately depict a test compound's particular functional activity in a setting that is relevant to biology. They provide a significant phenotypic readout to supplement data from such direct binding assays between the drug and target because they clearly outperform binding assays. They may also aid in clarifying the ligand's mode of action. Acquiring these cellular mechanistic readouts in advance is extremely valuable for comprehending the possible effects of target modification in support of drug evaluation during lead generation.
- Multiple assay modes
GPCRs are a crucial target class in the search for new drugs. Targeting GPCRs for the treatment of diseases ranging from cancer, immunology, cardiovascular, neurological, and metabolic disorders, several significant medications have been produced. The majority of GPCR-based medicines are either antagonists that block the effects of natural agonists or agonists that stimulate GPCRs. Our off-target panels provide more thorough information on drug off-target effects by simultaneously detecting agonistic and inhibitory effects.
GPCR Profiling Services with Off-target Panels
Our off-target panels include a core panel with 44 targets and a complete panel with 90 targets to identify unwanted potential hazards early in the drug discovery process. Transporter, ion channel, nuclear receptor, and kinase enzyme targets are also included in this panel. Creative Biolabs' off-target panels can be used to focus on particular requirements for your drug development initiative. Please contact us for more information.
