GPCR assays

GPCR Screening & Profiling Assays

Glyph

SB Drug Discovery's GPCR screening & profiling assay services enable the evaluation of ligand binding as well as downstream effects of small molecules against a wide variety of GPCR targets. Our assays employ radioligand binding and whole-cell calcium and cAMP assays in order to investigate affinity and nature of compound interaction. GPCR assays are also used for functional characterization of recombinant GPCR cell lines during custom cell line generation.

SB performs high throughput screening as well as dose-response studies and selectivity profiling against a broad panel of GPCR targets including species orthologs. Our flexible service and fast turnaround times enhance medicinal chemistry campaigns with timely supply of high quality profiling data.

To discuss your next GPCR project or to receive a quote, contact us or call +44 141 587 6100.


Assay Reproducibility

GPCR binding assay
GPCR cell based assays

Assay reproducibility: Highly reproducible binding and cell-based GPCR assays. Examples show consistency of data generated from assay runs on four separate days using radioligand binding (left) and cell-based calcium assay (right).


Selectivity Panels

CHRM GPCR selectivity

Selectivity studies: Compare compound potency across a panel of related GPCR targets.

Species Orthologs

GLP2 cell based assay

Species ortholog studies: Custom assays using GPCR species orthologs. Example shows mouse GLP cAMP assay.


Core GPCR Safety Panel

Reducing costly safety-related attrition.

Identification of undesirable off-target effects is an essential process in any drug discovery campaign. In vitro pharmacological profiling against a broad panel of known potential hazards at an early stage in the discovery process can therefore aid decision-making in lead generation, lead optimization and candidate selection, resulting in significantly reduced downstream safety-related attrition.

SB’s GPCR safety assessment panel provides a broad pharmacological profile of your compounds and their potential to cause adverse drug reactions. Our flexible service allows you to screen against the complete panel or select only the targets that matter to you.

Safety panel targets

5HT1A 5HT1B 5HT2A 5HT2B
ADOR A2a ADR α1A ADR α2A ADR β1
ADR β2 CHRM1 CHRM2 CHRM3
CB1 CB2 CCKA D1
D2 ET-A H1 H2
Op-δ Op-κ Op-μ V1A

To discuss your next GPCR project or to receive a quote, contact us or call +44 141 587 6100.


GPCR Cell Line Generation
GPCR assays