GPCR/NR/Ion Channel/Transporter
GPCR, nuclear receptor, ion channel and transporter assay services across the target classes that need specialist formats. Binding, functional and electrophysiology readouts run on validated systems, with counter-screens that separate genuine pharmacology from assay artifact.
OVERVIEW
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 Class | Cellular Functional Assay(cAMP HTRF Assay / Calcium Flux Assay) |
|---|---|
| Adenosine Receptor | A1, hA2a, mA2a |
| Adrenergic Receptor | α1A, α1B, α2A, β1, β2 |
| Complement Component Receptor | C5AR1 (CD88) |
| Dopamine Receptor | D1, D2, D4 |
| Endothelin Receptor | ETA |
| Fatty Acid Receptor | GPR40, GPR119 |
| Histamine Receptor | H1, H2, hH3, mH3, rH3 |
| Glucagon-Like Peptide Receptor | GLP-1 |
| Muscarinic Acetylcholine Receptor | M1, M2, M3, M5 |
| NPY Receptor | NPY2, NPY4 |
| Serotonin Receptor | 5H1A, 5HT1B, 5HT2A, 5HT2B, 5HT2C |
| Opioid Receptor | OPRD1, OPRK1 |
| Apelin Receptor | APJR |
| NR CLASS | Biochemical Reporter Assay(TR-FRET / Gal4 / Native RE) | |
|---|---|---|
| NR1A | Thyroid Hormone Receptor | TRα, TRβ |
| NR1B | Retinoic Acid Receptor | RARα, RARβ, RARγ |
| NR1C | Peroxisome Proliferator-Activated Receptor | PPARα, PPARβ, PPARγ |
| NR1F | RAR-related Orphan Nuclear Receptor | RORγt |
| NR1H | Liver X Receptor-like Receptor | LXRα, LXRβ, FXR |
| NR1I | Vitamin D Receptor-like Receptor | VDR, PXR |
| NR2B | Retinoic X Receptor | RXRα, RXRβ, RXRγ |
| NR3A | Estrogen Receptor | ERα, ERβ |
| NR3C | e-Ketosteroid Receptor | AR, GR, MR, PR |
| Ion Channels | Family | Assay Format(Calcium Flux / Patch Clamp / Thallium Flux) |
|---|---|---|
| Ligand-gated Ion Channels | P2X Family | P2X3, P2X2/3, P2X4, P2X7 |
| TRP Family | TRPV1, TRPV3, TRPC6 | |
| GABAaR | GABAaR (α1A, α1B, 2β) | |
| GluR Family | AMPA, NMDA | |
| Voltage-gated Ion Channels | K+ | hERG |
| Na+ | Nav1.1, Nav1.5, Nav1.7 | |
| Transporters | Assay Format | |
| hURAT1 | Radiolabel Uptake Assay (14C) | |
| Glutamate | Radiolabel 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 Transporter | Release Assay |
