G-Protein Coupled Receptors (GPCR) represent a major research focus of many pharmaceutical and biotech companies in drug discovery. As a leading GPCR solution provider, HDB provides comprehensive GPCR assay development, HTS and selectivity profiling services. All the assays are made to be HTS compatible. The cell lines that over express GPCR are optimized with high S/N ratio measured by calcium, cAMP or reporter genes. In house experience and know-how enable HDB to overcome cytotoxicity issues and generate stable GPCR cell lines, e.g. mGluRs and other targets. HDB’s extensive experience in the GPCR field provides clients the best in class experience and results.
Figure 1. Ligand response curves on HEK293/GPR40 stable cell line. Dose response of calcium assay was monitored with FlexStation plate reader upon treatment with ligand
Proprietary homogenous assay solution for better assay window
Aequorin
Radiometric Assays
GTPγS binding assay
Radio-ligand binding assay
Promiscuous G-proteins for universal readout
Co-expression
Fusion with receptor to reduce false positive in screening
With HDB’s broad collection of over 100 GPCR, we are able to provide compound profiling service to determine the respective active and inhibitory profiles and selectivity of lead compounds to various drug targets. Our rapid cost-effective compound profiling service enable clients to prioritize the most promising compounds in hit-to-lead selection process.
Figure 2. Sample Compound Activity Profile Against 40 Targets Avaliable as part of
HDB’s Compound Profiling Service. All targets were evaluated using an individual dose of Compound A at 1uM.
