Human GPCR Panel Assay

We provide reliable and comprehensive human GPCR panel assay services on our proprietary functional assay platform (international patent application filed).
Our panel services include

  • FlexPanel48, two types of focused panels with 48 GPCRs and
  • large-scale comprehensive panels covering as many as 294 GPCRs.

Listed at the bottom are the 200 non-orphan GPCRs and the 94 orphan GPCRs eligible for panel assays and the 48 GPCRs in each of the FlexPanel48 Therapeutic Area Panels. If you have any questions, feel free to ask us.

FlexPanel48

FlexPanel48 is reasonable focusted panels with 48 receptors and consists of custom panels and therapeutic area panels.

Custom Panels

  • One can choose 48 receptors from the 200 non-orphan GPCRs and the 94 orphan 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.

FlexPanel48 Therapeutic Area Panels

13 Therapeutic Areas

  • Immunology/Infection
  • Oncology
  • Hematology
  • Endocrinology/Metabolism
  • Psychiatry
  • Neurology
  • Ophthalmology
  • Cardiology
  • Respiratory
  • Gastrointestinal
  • Dermatology
  • Musculoskeletal
  • Urology/Reproduction
  • 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.
  • One can customize a Therapeutic Area Panel by replacing receptors on the list with those of his/her choice.

Panel Assay Examples

FlexPanel48 Endocrinology/Metabolism Panel
TAK875 vs FlexPanel48 Metabol/Endocrinol

Figure 1. TAK-875 screened in the endocrinology/metabolism panel
TAK875 Concentration-response curve

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
1HTR2A11CALCR21FFAR131KISS1R41PTH1R
2HTR2C12CASR22GHSR32S1PR242PROKR2
3CHRM213CNR123GHRHR33MC1R43PTGER4
4CHRM314CCR524GIPR34MC2R44SSTR1
5ADRA1A15CXCR425GLP1R35MC4R45SSTR2
6ADRB116CCKAR26GCGR36MTNR1B46TACR3
7ADRB217CCKBR27FSHR37NPY1R47TRHR
8ADRB318DRD228LHCGR38NPY2R48AVPR2
9AGTR119EDNRA29TSHR39NPY5R
10BRS320EDNRB30GNRHR40OPRM1
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
1HTR1A11CHRM421CCKBR31HRH141OPRK1
2HTR1B12CHRM522CRHR132HRH242OPRM1
3HTR2A13ADORA2A23CRHR233HRH343OPRL1
4HTR2C14ADRA2A24DRD134GRM244HCRTR1
5HTR5A15ADRA2B25DRD235GRM845TACR1
6HTR616ADRB126DRD336NPSR146AVPR1A
7HTR717ADRB227DRD437NPY1R47OXTR
8CHRM118GRPR28DRD538NPY2R48ADCYAP1R1
9CHRM219CNR129EDNRA39NTSR1
10CHRM320CCKAR30GABBR1/240OPRD1

Large-Scale Comprehensive Panels

Our large-scale panel assays allow comprehensive screening for up to 200 non-orphan GPCRs and 94 orphan GPCRs.

The total of 294 GPCRs amenable to panel assays are listed below.

Panel Assay Example

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

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 α1A, α1B, α1D, β1, and β2 adrenoceptors. Next, carvedilol was shown to antagonize the above receptors in a concentration-dependent manner (Figure 6).

Panel Receptors

Listed are the total of 294 GPCRs amenable to panel assays and the GPCRs in the therapeutic area panels. Each panel is customizable.


Contact Us

Send us a message via the form below or write to us at info@tansobio.com.

Service Flow Chart

Request for Quotation

Tell us about the types of tests you need, the number of compounds, the receptors of interest, and other preferences. A non-disclosure agreement is optional.

STEP
1

Order

A non-disclosure agreement is optional.

STEP
2

Compound Shipment

The client ships test compounds to our laboratory. We usually perform assays and write a report in three weeks from the receipt of the compounds.

STEP
3

Receipt of the Report

We provide the report and raw data for the client via email or a cloud service.

STEP
4

Inquiry & RFQ Form