GPCR, NR, Ion-channel, Transporter

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G Protein Coupled Receptors (GPCR), nuclear hormone receptors, ion channels, and transporters are all important drug targets. More than 50% of drugs targets are receptors; therefore, they have become the most important drug target.

GPCR targeted drugs have a wide range of indications, such as hypertension, obesity, multiple sclerosis, allergies, Alzheimer’s disease, analgesics, schizophrenia, depression drugs, and more. Currently, in the global therapeutic drug market, the proportion of drugs targeting GPCRs is as high as 27%.

The nuclear receptor superfamily is ligand-activated transcription factor, which plays an essential role in cell differentiation, proliferation, and metabolism, and is related to many diseases, such as cardiovascular disease, inflammation, and cancer.

About 6% of drugs targets are ion channels. The normal structure and function of cell ion channels are the basis for life maintenance. The opening or closing of the channels affects the transport of inorganic ions inside and outside the cell, which can quickly change cell functions, cause nerve excitement, glandular secretion, etc.

Transporters mediate the exchange of chemical substances and signals inside and outside the cell membrane and play an important role in cell activities. The dysfunction of ion channels and transporters is related to many diseases.

ChemPartner’s in vitro biology team utilizes FLIPR calcium flux, cAMP, reporter genes, and radiometric assays to provide customized assay development and high-throughput screening services to support our clients’ drug discovery for receptors, ion channels, and transporters.

GPCR ClassCellular Functional Assay  
(cAMP HTRF Assay / Calcium Flux Assay)
Adenosine ReceptorA1, hA2a, mA2a
Adrenergic Receptorα1A, α1B, α2A, β1, β2
Complement Component ReceptorC5AR1 (CD88)
Dopamine ReceptorD1, D2, D4
Endothelin ReceptorETA
Fatty Acid ReceptorGPR40, GPR119
Histamine ReceptorH1, H2, hH3, mH3, rH3
Glucagon-Like Peptide ReceptorGLP-1
Muscarinic Acetylcholine ReceptorM1, M2, M3, M5
NPY ReceptorNPY2, NPY4
Serotonin Receptor5H1A, 5HT1B, 5HT2A, 5HT2B, 5HT2C
Opioid ReceptorOPRD1, OPRK1
Apelin ReceptorAPJR
NR CLASSBiochemical Reporter Assay  
(TR-FRET / Gal4 / Native RE)
NR1AThyroid Hormone ReceptorTRα, TRβ
NR1BRetinoic Acid ReceptorRARα, RARβ, RARγ
NR1CPeroxisome Proliferator-Activated ReceptorPPARα, PPARβ, PPARγ
NR1FRAR-related Orphan Nuclear ReceptorRORγt
NR1HLiver X Receptor-like ReceptorLX, LX, FXR
NR1IVitamin D Receptor-like ReceptorVDR, PXR
NR2BRetinoic X ReceptorRXRα, RXRβ, RXRγ
NR3AEstrogen ReceptorERα, E
NR3Ce-Ketosteroid ReceptorAR, GR, MR, PR
Ion ChannelsFamilyAssay Format  
(Calcium Flux / Patch Clamp / Thallium Flux)
Ligand-gated Ion ChannelsP2X FamilyP2X3, P2X2/3, P2X4, P2X7
 TRP FamilyTRPV1, TRPV3, TRPC6
 GABAaRGABAaR (α1A, α1B, 2β)
 GluR FamilyAMPA, NMDA
Voltage-gated Ion ChannelsK+hERG
 Na+Nav1.1, Nav1.5, Nav1.7
TransportersAssay Format
hURAT1Radiolabel Uptake Assay (14C)
GlutamateRadiolabel Uptake Assay (3H)
Dopamine (DAT)Radiolabel Filter Binding Assay (3H)
Norepinephrine Transporter (NET)Radiolabel Filter Binding Assay (3H)
5-HT Transporter (SERT)Radiolabel Filter Binding Assay (3H)
xCT (SLC7A11)Radiolabel Uptake Assay (3H) / Glutamate
Cystine/Glutamate TransporterRelease Assay

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