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GPCR

GPCR

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GPCR

ChemDiv offers high throughput screening (HTS) service
GPCR research platform

  • 411 protein assays depending on 74 classes of GPCRs are available (class A orphans, сlass C Orphans, Taste 1/2 receptors, adhesion GPCRs, adrenoceptors, chemokine receptors, dopamine receptors, histamine receptors, opioid receptors, serotonin receptors, etc.)

  • 2 HTS platforms: FLIPR® platform and LANCE® platform

  • The best choice of screening libraries on the market: 7 GPCR-focused libraries are available (GPCR Targeted Library, Human GPCR Annotated Library, and 4 privileged fragments annotated libraries: GPCR Family A, GPCR Family B, GPCR Family C, GPCR Taste Family), 45K compounds in total

  • We support you in compound selection based on your research project

  • Screening from 10000 compound sets up to 300000 and more

  • A quick start of your research project

  • 25 years of experience


More details on prices, time, or research specificity - please contact chemdiv@chemdiv.com


G-protein coupled receptors, or GPCRs, a family of proteins holds up to 40% of all modern drug targets. An example of chemokine GPCR targeting are CXCR3 antagonists designed for the treatment of multiple inflammatory and autoimmune diseases, including organ transplant rejection, multiple sclerosis, asthma, etc. Another approach to GPCR targeting is the development of agonists: bile acids, for instance, are natural agonists of TGR5, and GPR40 agonists TAK-875 and AMG 837 have shown results in type 2 diabetes treatment.

For GPCR studies ChemDiv offers FLIPR® and LANCE® approaches. Let’s consider the key aspects of each method.

FLIPR® platform:

  • The simultaneous record of transient fluorescent signals from all the wells of 384-well microplate.

  • GPCRs activation leads to an increase of intracellular calcium, which is detected by a specific masking dye and fluorescence signal intensity is measured (Figure 1).

  • Enhanced sensitivity is accomplished via a patented optical detection scheme, allowing to highly distinguish between specific cell signal and background fluorescence.

  • Two different fluid addition microplates gives an opportunity of dual stimulus experiments.

  • Temperature control makes it possible to conduct experiments at physiological conditions.

Figure 1. The increase in intracellular calcium caused by the GPCR activation is detected via measurement of the fluorescence using calcium-sensitive dye indicators. The masking dye does not enter the cell and reduces background fluorescence from extracellular indicators.


LANCE® platform:

  • In course of GPCRs signaling cAMP is produced.

  • Analysis is based on competitive binding of an intracellular cAMP and Europium-labeled cAMP tracer complex to cAMP-specific antibodies

  • Antibodies in complex with Europium-labeled cAMP tracer emit fluorescent signal.

Intracellular cAMP binding to antibodies results in inversely proportional decrease in fluorescence.

List of G-protein coupled receptors:




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