Publications

Showing 13–24 of 35 results

Publications Examining Ligand-Based Stabilization of Proteins in Cells with MEK1 Kinase Inhibitors

In this study, we describe the evaluation of a cell-based protein stability assay using β-galactosidase fragment complementation technology performed in…

Publications Development of Three Orthogonal Assays Suitable for the Identification and Qualification of PIKfyve Inhibitors

FYVE-type zinc finger-containing phosphoinositide kinase (PIKfyve) catalyzes the formation of phosphatidylinositol 3,5-bisphosphate (PI(3,5)P2) from phosphatidylinositol 3-phosphate (PI(3)P).

Publications InCELL Target Engagement: A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1

A persistent problem in early small-molecule drug discovery is the frequent lack of rank-order correlation between biochemical potencies derived from…

Publications A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors

The non-receptor protein tyrosine phosphatase (PTP) SHP2 is encoded by the proto-oncogene PTPN11 and is a ubiquitously expressed key regulator…

Publications Cell-Based Protein Stabilization Assays for the Detection of Interactions between Small-Molecule Inhibitors and BRD4

Bromodomain protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) proteinfamily, acts as a central element in transcriptional…

Publications A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

Publications Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

By suppressing gene transcription through the recruitment of corepressor proteins, B-cell lymphoma 6 (BCL6) protein controls a transcriptional network required…

Publications A Pharmacochaperone-Based High-Throughput Screening Assay for the Discovery of Chemical Probes of Orphan Receptors.

G-protein-coupled receptors (GPCRs) have varying and diverse physiological roles, transmitting signals from a range of stimuli, including light, chemicals, peptides,…

Publications MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities

Mast cells play key roles in allergy, anaphylaxis/anaphylactoid reactions, and defense against pathogens/toxins. These cells contain cytoplasmic granules with a…

Publications Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the mu-Opioid Receptor.

With the hope of discovering effective analgesics with fewer side effects, attention has recently shifted to allosteric modulators of the…

Publications Measurement of β-Arrestin Recruitment for GPCR Targets.

β-Arrestins are ubiquitously expressed in all cell types, and function in the desensitization of G- protein coupled receptors (GPCRs), the…

Publications Navigating CYP1A induction and arylhydrocarbon receptor agonism in drug discovery. A case history with S1P1 agonists.

This article describes the finding of substantial upregulation of mRNA and enzymes of the cytochrome P450 1A family during a…