Linking Activity Across in vitro Assays for Informed Hit-to-Lead Decision-Making

Conference poster by Pharmaron discussing the importance of linking activity across multiple in vitro assay services for molecule understanding and progression.

Poster Authors:

Joanne Wayne1, Marta Westwood2, Haiyan Cui3, Yasong Cui3, Yan Sun3, Shuhua Zhao3, Jiaoping Hao3, Yuhui Wang3, Qiong Zhang3, Pengwei Pan3, Zhe Zhang3, Fang He3, Gillian Watt1

1Drug Discovery, Pharmaron, UK

2Biophysics, Pharmaron, UK

3In Vitro Biology, Pharmaron, China

This poster was presented at ELRIG Drug Discovery.

This poster explores evidence-based decision-making in drug discovery using MRTX1133, a KRAS G12D inhibitor, as a case study. It highlights the role of diverse in vitro assay services in linking data for disease relevance and informed decisions. We illustrate that data from increasingly complex in vitro assays can be applied to build a comprehensive drug discovery picture for a target.

In Vitro Assay Services used in this study:

  • IC50 analysis across KRAS mutant cell lines.
  • Surface plasmon resonance (SPR) assays to evaluate binding kinetics and affinity.
  • Target engagement and protein-protein interaction (PPI) assays to assess efficacy.
  • HTRF-based ERK phosphorylation assay.
  • Cytotoxicity testing in tumor organoids.

Interested in reading the full story? Please download the poster.