The Adenosine A2A Receptor (A2AR) was selected as a representative GPCR to establish an integrated fragment‑based discovery workflow capable of screening fragments on the active receptor state.
We present integrated capabilities for SH2 domain-focused drug discovery, emphasizing STAT protein binding affinity and targeted protein degradation (TPD).
Obesity is a chronic, multifactorial disease projected to affect over 50% of the global population by 2035.
WEE1 is a key regulator of the G2/M cell cycle checkpoint, inhibiting CDK1 to allow DNA repair before mitosis.
Explore the mechanistic basis and translational implications of GPCR biased agonism. Examine via modern GPCR functional assays the (1) detection and quantification of signaling bias, (2) influence of bias signaling on the therapeutic profiles of existing and emerging drugs. and (3) use of quantitative pharmacological tools to enable systematic comparison of biased agonists.
Per- and polyfluoroalkyl substances (PFAS) are persistent environmental contaminants posing significant health risks, including endocrine disruption, hepatotoxicity, immuno-toxicity, and developmental effects.
Secondary pharmacology data plays a critical role in new drug applications by characterizing the selectivity profiles of clinical candidates and identifying off-target molecular interactions.
Clinical attrition of drug candidates is frequently driven by unforeseen safety liabilities, which are often associated with off-target pharmacological interactions.
Early safety insights can make or break a program. Discover how current industry thinking and practical strategies to help you apply secondary pharmacology more effectively, so you can make risk-informed decisions earlier.
Learn about GPCR families and their targets. Discover target-specific coupling status and GPCR phylogenetic relationships. Review the available cell-based assay covering >90% of the GPCRome for: cAMP and calcium detection, β-Arrestin recruitment, ligand binding, GTPγS activation, pharmacochaperone discovery, and receptor internalization.
Ion channels are essential targets in drug discovery due to their critical roles in cellular signaling, electrical activity, and homeostasis.
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