GPCR, NR, Ion-channel, Transporter

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 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 and depression drugs, etc. 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.