We provide GPCR drug discovery and contract research services using proprietary high-sensitivity assay technology. Our platform enables comprehensive evaluation of all GPCRs, including orphan receptors and challenging Gi/o- and G12/13-coupled pathways. We offer panel assays, dose-response studies, and fully customized assay development to support efficient and scalable drug discovery.
G-protein-coupled receptors (GPCRs) play a vital role in biology and medicine, but only a small number of them have drugs that target them. Tanso Biosciences has developed a versatile and sensitive assay method to overcome the challenges in GPCR research and promote drug development (Patent granted in Japan and US and pending in Europe. Publication Number WO/2020/026979). This innovative platform enables the company to engage in drug discovery for orphan GPCRs and offer contract assay services.
Drug Discovery
Comprehensive Orphan GPCR Drug Discovery Project
Research on GPCRs, especially orphan GPCRs, has been hindered by a lack of adequate assays. To overcome the barriers of GPCR drug discovery, we have innovated a high-performance functional assay. It works excellently for all receptors coupled with any of the major Gα proteins including Gq, Gs, Gi/o, and G12/13.
We have taken advantage of our proprietary assay and embarked on orphan GPCR drug discovery, broadly targeting ~100 of them. As a first step, compound library screening is ongoing for their agonists, with a priority on disease-associated receptors.
We have identified agonists for six orphan GPCRs, namely, GPR39, GPR55, GPR65, GPR68, GPR132, and P2RY10, and characterized their concentration-dependent potency.
Agonists identified in the previous step will be further characterized. They will also play crucial roles in screening for orphan GPCR antagonists.
Contract Services
How Our GPCR Platform Accelerates Drug Discovery
Drug discovery success depends on selecting the right targets, understanding mechanisms, and minimizing safety risks early. Our proprietary GPCR functional assay platform empowers pharma and biotech partners to make better decisions, faster — reducing attrition and opening new therapeutic opportunities. Covering 550 validated receptors across all four G protein families, we provide clarity where conventional assays leave blind spots.
Hit Discovery and Lead Prioritization in Drug Discovery
Large-scale panel screening identifies active compounds across hundreds of GPCRs, while subsequent concentration-response analysis quantifies their potency and efficacy. Unwanted off-target activity is eliminated early, allowing development resources to focus on the most promising candidates.
Available as: Panel Assays, Concentration-Response Analysis →
Expanding Pipelines Through Drug Repurposing & MoA Discovery
Our high-sensitivity assays reveal unexpected GPCR interactions, uncovering new mechanisms of action and repurposing opportunities. This enables partners to extend the value of existing compounds and explore new disease areas.
Available as: Panel Assays, Concentration-Response Analysis →
De-risking Development with Safety & Selectivity Profiling
Off-target GPCR activity can cause adverse effects such as unwanted CNS side effects. Panel assays identify these liabilities early, preventing future development obstacles and accelerating lead optimization.
Available as: Safety Panels →
Bridging Bench to Bedside with Translational Research
Cross-species assays (human vs. mouse) confirm whether preclinical findings will translate to humans, supporting smoother IND-enabling studies and clinical development.
Available as: Inter-Species Analysis →
Contact Us
We welcome quotation requests and inquiries about our assay services, custom assay development, or co-development opportunities. Visit Contact Us for the ordering process and the inquiry form. Our team will respond within 24 hours.