A Guide to Measuring Drug-Target Residence Times with Biochemical Assays
Wednesday, 22 August 2018
- Published in HTS Assays
No Comments
Taking Up Residence: Using the Transcreener ADP Assay to Measure the Kinetics of Kinase Inhibitor Interactions
Wednesday, 30 August 2017
Classically speaking, assays for interactions between drug molecules and their targets have measured binding affinity under equilibrium conditions. In drug discovery projects, it had long been assumed that carefully measuring IC50 (half-maximal inhibitory concentration), EC50 (effector concentration for half-maximal response), Kd (equilibrium dissociation constant), and/or Ki (inhibition constant) would allow drug candidates to be prioritized
- Published in HTS Assays, Uncategorized
New Publication: HTS Method for Measuring Drug Residence Time
Tuesday, 25 April 2017
View our latest publication, “A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener® ADP2 Assay” in SLAS Discovery. Inhibitor residence times are increasingly being used to prioritize molecules early in lead discovery programs. Current methods for determining residence time are low-throughput or require the synthesis of labeled ligands. Our goal was to create
- Published in Company, HTS Assays, News
View Our Kinase Inhibitor Residence Time Webinar Anytime!
Monday, 11 May 2015
Analysis of inhibitor residence times is increasingly being incorporated into lead development efforts because longer engagement with the target can result in improved efficacy, increased therapeutic window and reduced side effects. Though residence time can be determined using immobilized ligand methods such surface plasmon resonance, conjugation of drugs can affect their binding. In this webinar,
- Published in HTS Assays, News
