Panel Assay

GPCR Panel Assay

We provide reliable and comprehensive human/mouse GPCR panel assay services on our proprietary functional assay platform (Patent Publication Number WO/2020/026979).
Our panel services include

• FlexPanel48, focused panels with 48 GPCRs.
• therapeutic area panels
• safety panels to screen off-target potencies
• large-scale comprehensive panels covering a maximum of 294 human GPCRs and 250 mouse GPCRs.

The receptors eligible for our panel assays are listed at the bottom. If you have any questions, feel free to ask us.

FlexPanel48

FlexPanel48 is a series of focused panels with 48 receptors consisting of custom panels and therapeutic area panels.

Custom Panels

• One can choose 48 receptors from the >550 human/mouse GPCRs on our list.
• Two assay modes, the agonist and antagonist modes, are available. Orphan GPCRs are assayed in the agonist mode only.
• The two assay modes may coexist in a single panel.
• One can replace receptors in a panel with other human receptors or mouse orthologs.

FlexPanel48 Therapeutic Area Panels

• Assorted are the 48 GPCRs with high disease-gene association scores according to the DisGeNET database.
• The receptors in each panel are listed below.
• Two assay modes, the agonist and antagonist modes, are available.
• The two assay modes may coexist in a single panel.

Panel Assay Examples

FlexPanel48 Endocrinology/Metabolism Panel

Figure 1. TAK-875 screened in the endocrinology/metabolism panel

Figure 2. Concentration-response curve for TAK-875

TAK-875, a Phase 3 antidiabetic, was screened in the agonist mode in the FlexPanel48 Endocrinology/Metabolism Panel (Figure 1). TAK-875 selectively activated free fatty acid receptor 1 (FFAR1). Next, TAK-875 was shown to activate FFAR1 in a concentration-dependent manner (Figure 2).

Endocrinology/Metabolism Panel Receptors

FlexPanel48 Psychiatry Panel

Figure 3. Naloxone screened in the psychiatry panel

Figure 4. Concentration-response curves for naloxone

Naloxone, the opioid reversal drug, was screened in the antagonist mode in the FlexPanel48 Psychiatry Panel (Figure 3). Naloxone selectively antagonized opiate receptors OPRD1, OPRK1, and OPRM1. Next, naloxone was shown to antagonize the three opiate receptors in a concentration-dependent manner (Figure 4).

Psychiatry Panel Receptors

Large-Scale Comprehensive Panels

Our large-scale panel assays allow comprehensive screening for up to 294 human GPCRs and >250 mouse orthologs.

The total of >550 human and mouse GPCRs amenable to panel assays are listed below.

Panel Assay Example

Figure 5. Carvedilol screened for 200 non-orphan GPCRs.

Figure 6. Concentration-response curves for carvedilol

Carvedilol, an anti-hypertensive agent, was screened in the antagonist mode for 200 non-orphan GPCRs (Figure 5). Carvedilol selectively antagonized α_1A, α_1B, α_1D, β₁, and β₂ adrenoceptors. Next, carvedilol was shown to antagonize the above receptors in a concentration-dependent manner (Figure 6).

Safety Panels

Our GPCR Safety Panels are designed to help evaluate the off-target potency of candidate compounds in drug discovery and preclinical research. These panels include GPCRs often linked with common adverse reactions, making them a practical resource for pharmaceutical R&D. 

• Standard GPCR Safety Panel: Features a minimal set of 24 representative GPCRs, allowing for testing compounds in both agonistic and antagonistic modes.
• GPCR Safety Panel Premium: Includes 31 additional GPCRs from the same receptor families for broader coverage.

Key Advantages

Early Identification of Off-Target Interactions

Detect off-target interactions at the lead selection stage, which is crucial for mitigating unwanted activities through structure-activity relationship (SAR) studies.

Predictive Insights into Clinical Adverse Reactions

Predict clinical adverse reactions that may go unnoticed in vivo, such as valvulopathy associated with 5-hydroxytryptamine receptor 2B (HTR2B) agonists, using human GPCRs for better correlation with clinical effects.

Cost-Effective In Vitro Testing

Test a large number of compounds cost-effectively in vitro on human targets, facilitating early-stage drug discovery and lead identification.

Relevance to Physiology

Our proprietary GPCR functional assay measures the potency of test compounds against GPCRs, providing physiologically relevant insights aligned with clinical implications.

Accelerated Research Timeline

Obtain quicker results and explanations of off-target effects, allowing for efficient data integration from safety pharmacology profiling, pharmacokinetic experiments, ADME, and efficacy models.

Flexibility for Streamlined Research

Our GPCR collection covers 550 human receptors and mouse orthologues. We also offer the flexibility to prepare orthologues for other species used in preclinical studies, ensuring customized panels to suit your research needs.

Competitive Benchmarking

Benchmark against competitor compounds to support a best-in-class development strategy, addressing pharmacological promiscuity early on.

Panel Receptors

Listed are the GPCRs amenable to panel assays. Each panel is customizable.