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Epigenetic Screening & Profiling Services

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Overview

At Creative Biogene, we are committed to providing professional and efficient epigenetic drug discovery solutions to pharmaceutical companies, biotechnology firms, and academic research institutions worldwide. Leveraging our extensive expertise in the field, advanced technology platforms, and a team of experienced scientists, we aim to accelerate your drug development process targeting epigenetic mechanisms.

Epigenetic mechanisms and key examples of widely studied modifications and their modifying enzymes.Figure 1. Epigenetic mechanisms and key examples of widely studied modifications and their modifying enzymes. (Dai W et al., 2024)

Our platform supports multidimensional interrogation of enzyme activity modulation, protein–ligand interactions, and chromatin modification pathways, enabling rapid identification of therapeutically relevant lead compounds and generating robust datasets for downstream optimization, IND-enabling studies, and efficacy evaluation.

Drawing on front-edge literature, industry benchmarks, and comparisons with top competitors such as Reaction Biology, BPS Bioscience and Active Motif, we have established a broader, more customizable, and mechanism-centered screening system.

Core Service Offerings

We support an extensive range of epigenetic regulators involved in chromatin remodeling and gene expression control. Our target panel includes major histone-modifying enzymes—such as bromodomain family proteins, histone deacetylases, histone demethylases, and histone methyltransferases—along with DNA methyltransferases and TET-related pathways that shape methylation dynamics at the genomic level.

Histone Modification Targets:

DNA Methylation Targets:

Other Key Epigenetic Targets:

High-Throughput and High-Content Screening Technologies

To ensure accuracy, signal robustness, and reproducibility, we apply multiple internationally validated detection technologies tailored to the target class.

Available Technology Platforms

Typical Screening Modes

Available Technology Platforms

  • Fluorometric and luminescent biochemical assays designed for sensitive enzyme activity detection
  • AlphaLISA or TR-FRET–based interaction assays for protein binding and complex formation
  • Turnover assays for histone methylation and acetylation analysis
  • Mass-spectrometry-enabled profiling for high-resolution epigenetic modification assessment
  • Cell-based reporter or phenotypic readout systems for pathway-dependent evaluation

Typical Screening Modes

  • High-throughput hit identification for compound libraries ranging from 10,000 to 100,000 entries
  • Single-concentration hit verification
  • Full dose–response evaluation with IC50 or EC50 determination
  • Mechanism-of-action interrogation
  • Selectivity studies across expanded epigenetic target families
  • Cell-based functional validation

Mechanistic Characterization and Target Engagement Verification

Mechanistic studies are essential for transitioning from hit to lead. We provide analytical strategies widely adopted by global pharmaceutical companies.

Biochemical Mechanism-of-Action Analysis

  • Competitive and non-competitive inhibition models
  • Cofactor competition analysis for targets dependent on donors such as SAM, SAH, or acetyl-CoA
  • Assessment of catalytic dependencies involving iron, alpha-ketoglutarate, NAD⁺, and others

Biophysical Binding Characterization

  • Surface plasmon resonance, isothermal titration calorimetry, and differential scanning fluorimetry
  • BRET-based measurements of intracellular compound–target interactions
  • CETSA assays to quantify target stabilization within cells

Chromatin-Level Functional Assays

  • Profiling of histone modification states such as H3K27me3, H3K9ac, and H3K4me3
  • Quantification of methylation and hydroxymethylation changes by LC–MS or ELISA

Omics-Based Epigenetic Profiling

  • RNA-seq, ChIP-seq, and ATAC-seq
  • Epigenomic reprogramming maps and pathway-level analysis
  • Off-target prediction through multi-omic integration

Data Deliverables and Scientific Support

Each project concludes with a complete package of raw and processed data, quality-control metrics, assay validation details, and high-quality visual outputs that can be directly incorporated into manuscripts, patents, presentations, or regulatory documentation.

In addition to reporting results, our scientific team provides expert interpretation of potency, selectivity, and mechanism, and offers guidance on structure–activity relationships and next-step optimization strategies. This ensures that clients not only receive data but also meaningful scientific insight that advances the trajectory of their drug discovery program.

Contact Us

For customized epigenetic target screening, lead compound profiling, mechanistic studies, or development of tailored assay systems, contact our scientific team. We are committed to advancing your epigenetic drug discovery programs with deeper insight, higher precision, and greater translational value.

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