Abstract 3164: Micro-TagTM cell target engagement platform - From discovery to optimization

Abstract Smartly designed drug discovery programs can amplify the success rate and accelerate the progress from hit discovery to optimization. Drug discovery for challenging or “undruggable” drug targets such as transcription factors necessitates the proteomic complexities of the cellular milieu for proper folding and function. Therefore, conventional drug discovery methods are not sufficient for most of these proteins. The incorporation of recent cell target engagement methodologies has helped improve drug discovery efforts. However, currently available high throughput cell target engagement methods are limited to measurement of end-point signal, poor utility across multiple challenging target families and insufficient resolution for kinetic and mechanistic readouts. Here we present MICRO-TAGTM cell target engagement platform for challenging drug targets. We provide data demonstrating utility of MICRO-TAG platform for rapid discovery of novel interacting drug molecules to several challenging drug targets. The platform enables cross experimentation with the same cell reporter system for comprehensive hit identification, validation, lead identification and optimization employing several experimental strategies. Citation Format: Ivan Babic, Elmar Nurmemmedov. Micro-TagTM cell target engagement platform - From discovery to optimization [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2025; Part 1 (Regular Abstracts); 2025 Apr 25-30; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2025;85(8_Suppl_1):Abstract nr 3164.