GPCR ASSAYS
BioMedha offers custom made GPCR assay development and screening services to meet your project needs with the interrogation of compounds against your target of interest.
GPCRs are popular and well-established protein targets, representing the largest individual family of drug targets used in current medications on the market. Our scientists work with you to develop robust, optimised assays that are bespoke to your specific needs, helping you to understand whether a compound acts on a biological target, how effective it is, and if it has any potential off-target effects.
Our experienced team works closely with clients to take into account the many considerations that determine the reliability, specificity and sensitivity of a compound’s action on a target.
Our custom GPCR assay support includes:
- Constitutive activity check, transient and stable transfections
- Stable cell line generation, assay development, and screening
- Single receptor, dual, and receptor dimerisation
- Screening cascade support (Hit to lead, Primary, Secondary, Selectivity and counter screens)
- Allosteric and Orthostatic site of action
- MOA studies and shield analysis
- GPCR knockdown (siRNA)
- Cell types: recombinant and endogenous cell lines
GPCR assay formats include:
- Ca2+ Flux (Gq) by Flexstation
- cAMP levels (Gi and Gs)
- IP-1 levels (Gq)
- pERK1/2 levels
- β-Arrestin recruitment
- nanoBRET in cell target engagement
- HiBit assays
- Receptor internalisation