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GPCR Target Library Screening Service

KMD Bioscience is an experienced provider of preclinical CRO services with a team of experts dedicated to providing our clients with a rapid, high-throughput drug target screening platform. We offer a wide range of compound library screening services to major research institutes and pharmaceutical companies. Clients simply provide us with their compound libraries and we screen potential compounds using standard experimental procedures.

G protein-coupled receptors (GPCRs) play an incredible role in a range of functions in the human body, and a better understanding of these receptors has greatly influenced modern medicine. Researchers estimate that between one-third and one-half of all marketed drugs work by binding to GPCRs.

GPCRs mediate many important physiological functions. The development and application of high-throughput GPCR assays are essential for early drug discovery, enabling cost-effective screening of large libraries of compounds to identify new drug candidates. Early functional GPCR assays relied primarily on the measurement of G protein-mediated second messengers. With the growing understanding of GPCR signaling, many G-protein independent pathways have been used to measure GPCR activity and can provide additional information on the functional selectivity of candidate compounds. Combined with an automated imaging system with label-free detection.

KMD Bioscience offers extensive GPCR binding and functional screening services to meet the chemical and biological research needs in GPCR drug discovery.


Service Content:



General Assay Methods



Receptor Binding Assay

 Radioactive ligand binding assay

* High throughput; low interference; agonists and antagonists in one assay

Fluorescent ligand binding assay

* Non-radioactive; high throughput; agonists and antagonists in a single assay


G Protein Dependence Assay

GTPγS binding test

* Functional cell-free assays; distinctions between full or partial agonists, neutral antagonists, inverse agonists, and allosteric modifiers

Report genetic test

* Homogeneous determination; high throughput; large background signal

cAMP assay

* High throughput; high sensitivity

Ca 2+ mobilization test

* High throughput; functional assay of living cells; agonists, antagonists and allosteric modifiers obtained in one assay

IP3/IP1 test

* High throughput; functional assay of living cells; suitable for slow binding ligands

G Protein Independent Assay

GPCR internalization test

* Image-based and informative; functional assays for living cells; universal methods for all

β-arrestin collection test

* High throughput; image or non-image based; functional assay of living cells; can be used for bias signal detection; common method for all GPCRs

label-free whole-cell assay

* Label-free function assay in living cells; sum of cellular events

Receptor Dimerization Assay

GPCR heterodimers considered as new pharmacological targets

The ideal assay for GPCR ligand screening should be simple, non-radioactive, stable, homogeneous and easily adaptable to microtitre plate formats (96, 384 or 1536 wells) for automation. With over 10 years of biopharmaceutical expertise, KMD Bioscience offers hundreds of functional and radioligand binding GPCR assays for high throughput screening, molecular pharmacology and molecular spectroscopy.


Customer Provides:




Bioinformatics and pharmacological information

Target protein or peptide

Structural classification (e.g. flavonoids, alkaloids, etc.)

Purity >90%, concentration 1mg/ml

Solubility information

Produced and prepared by KMD Bioscience based on target sequences provided by the customer

Signaling pathways or targets, etc.

For more information, please visit Protein Platform


Cell lines: KMD Bioscience provides overexpression cell line construction service. For more information, please visit IOS overexpression stable cell line construction service.


Service Highlights:


--Multiple assay formats to choose from

--Customized production of GPCR stable cell line

--High standards of quality control

--Fast turnaround time

--Accurate and reproducible results


How to Order?

If you have any questions regarding our services or products, please feel free to contact us by E-mail: or Tel: +86-400-621-6806;