Resurrecting the phoenix: When an assay fails.

@article{Srinivasan2020ResurrectingTP,
  title={Resurrecting the phoenix: When an assay fails.},
  author={Bharath Srinivasan and Vasudev Kantae and James Robinson},
  journal={Medicinal research reviews},
  year={2020}
}
Understanding protein-small-molecule interactions is a critical component of rational drug-design. Structure-activity relationship (SAR)-guided medicinal chemistry is informed by the biological outcome, as assessed by biochemical activity or cellular effect, of chemical modifications on small molecules. The effectiveness of SAR is reliant on the sturdiness and durability of assay design and the quality of information garnered from assays. Lack of quality data at this step can lead to… 
2 Citations

A Novel High-Throughput FLIPR Tetra–Based Method for Capturing Highly Confluent Kinetic Data for Structure–Kinetic Relationship Guided Early Drug Discovery

TLDR
The use of the fluorescent imaging plate reader (FLIPR), a charge-coupled device (CCD) camera technology, is described, as a potential high-throughput tool for generating biochemical kinetic data with smaller time intervals and demonstrated the collection of highly confluent time-course data for various kinase protein targets with reasonable throughput to enable SKR-guided medicinal chemistry.

Explicit Treatment of Non‐Michaelis‐Menten and Atypical Kinetics in Early Drug Discovery **

TLDR
This review strives to present an overview of enzyme kinetic mechanisms that are atypical and, oftentimes, do not conform to the classical MM kinetics to enable effective screening and characterisation of small‐molecule inhibitors with desirable physiological outcomes.

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