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Apoptosis Biochemical Screening and Profiling
Epigenetic Screening & Profiling Services
GPCR Screening & Profiling Services
HSP90 Screening and Profiling
Ion Channel Screening & Profiling Services
Kinase Screening & Profiling Services
Nuclear Receptor Screening & Profiling Services
PDE Screening & Profiling Services
Phosphatase Screening & Profiling Services
Protease Screening & Profiling Services
Transporter Screening & Profiling Services
Ubiquitin Screening & Profiling Services

Target-based Drug Discovery Service

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In the development of complex diseases, simply pursuing target affinity is no longer sufficient for modern drug discovery. Creative Biogene breaks the traditional model by tightly integrating mechanistic understanding with physiological relevance, offering end-to-end target-based drug discovery services. From high-throughput biochemical screening to cellular functional validation, selectivity profiling, and early ADME-Tox risk assessment, we ensure that every candidate molecule demonstrates reliable, predictable efficacy and safety in disease-relevant models, making your R&D process faster and more precise.

Integrated workflow from high-throughput screening to validated hits and data-driven optimization across biochemical, biophysical, and structural assays.Figure 1. Integrated workflow from high-throughput screening to validated hits and data-driven optimization across biochemical, biophysical, and structural assays. (Kumar V, et al., 2023)

Our service goes beyond data provision—it delivers decision-driven biological insights. Through customized screening strategies, advanced cellular models, structure-activity relationship analysis, and integrated biology service packages, we help clients rapidly identify high-potential compounds, optimize lead molecules, and proactively mitigate off-target risks.

Core Capabilities and Advantages

Our Target-based Drug Discovery Service integrates diverse expertise and technologies across the drug discovery pipeline:

02

Structural and Biophysical Characterization

  • High-resolution crystallography, NMR spectroscopy, and cryo-EM
  • Binding kinetics and thermodynamics through SPR, ITC, and MST
  • Ligandability and druggability assessment with fragment-based screening
04

Computational and In Silico Modeling

  • AI-based drug design, deep learning for property prediction
  • Molecular dynamics simulations to refine binding hypotheses
  • Systems biology modeling to predict off-target effects and polypharmacology
01

Target Identification and Validation

  • Genome-wide CRISPR screens, siRNA/ASO knockdown, and functional genomics
  • Multi-omics profiling (transcriptomics, proteomics, metabolomics) to map disease networks
  • Biomarker correlation and clinical sample analysis to ensure translational relevance
03

Hit Discovery and Lead Generation

  • Virtual screening powered by AI/ML-driven molecular docking and dynamics
  • High-throughput screening (HTS) of small-molecule libraries
  • Hit-to-lead optimization with iterative medicinal chemistry and SAR analysis
05

Preclinical Pharmacology

  • In vitro cellular assays for efficacy and toxicity profiling
  • In vivo models for pharmacokinetics (PK), pharmacodynamics (PD), and efficacy
  • Translational pharmacology bridging preclinical findings to clinical endpoints

Specialized Screening & Profiling Services

Creative Biogene offers a suite of specialized screening and profiling services. These targeted solutions enable researchers to explore specific molecular families and signaling pathways with unmatched precision, providing critical insights that drive drug discovery. Advanced technologies, robust assay systems, and expert scientific interpretation support each service.

Apoptosis Biochemical Screening and Profiling

We provide comprehensive assays to evaluate compounds that regulate apoptosis pathways. These services enable detailed analysis of caspase activation, mitochondrial depolarization, and pro/anti-apoptotic protein interactions, supporting oncology and neurodegeneration drug discovery.

Epigenetic Screening & Profiling Services

Our epigenetic platforms focus on histone modification enzymes, chromatin remodelers, and DNA methylation regulators. With custom biochemical and cell-based assays, we support projects targeting epigenetic modulators in cancer, immunology, and rare diseases.

GPCR Screening & Profiling Services

GPCRs remain one of the largest and most validated drug target families. We offer binding and functional assays, including cAMP accumulation, calcium signaling readouts and arrestin-dependent reporter responses, enabling comprehensive GPCR profiling across diverse receptor subtypes.

HSP90 Screening and Profiling

HSP90 is a critical chaperone protein implicated in cancer, inflammation, and neurodegeneration. Our HSP90 assays allow precise evaluation of inhibitor binding, ATPase activity, and client protein stabilization, accelerating the development of targeted therapeutics.

Ion Channel Screening & Profiling Services

We provide electrophysiology-based and fluorescence-based assays for ion channels, covering ligand-gated and voltage-gated families. These services are essential for CNS, cardiovascular, and pain therapeutics development, offering insights into activity, selectivity, and safety.

Kinase Screening & Profiling Services

Kinases are central regulators of signaling pathways. Our kinase services include biochemical activity assays, phosphorylation readouts, and kinome-wide profiling, providing comprehensive support for oncology, immunology, and metabolic disorder programs.

Nuclear Receptor Screening & Profiling Services

Our assays cover nuclear receptors such as steroid hormone receptors, PPARs, and several less-characterized receptor subtypes. We provide ligand-binding and transcriptional activity profiling to identify compounds with selective modulatory activity.

PDE Screening & Profiling Services

Phosphodiesterases regulate cyclic nucleotide signaling. We offer PDE subtype-specific assays to support projects in cardiovascular, metabolic, and CNS indications, enabling precise evaluation of inhibitor potency and selectivity.

Phosphatase Screening & Profiling Services

We deliver specialized assays for protein phosphatases, a historically challenging but increasingly druggable target class. Our services include biochemical activity profiling and cell-based functional validation.

Protease Screening & Profiling Services

Proteases play critical roles in inflammation, infection, and cancer. We provide biochemical and cellular protease assays, including substrate cleavage and inhibitor profiling, to identify and optimize potent modulators.

Transporter Screening & Profiling Services

Transporters govern drug absorption and distribution. Our services include uptake and efflux assays for key transporters such as ABC and SLC families, supporting pharmacokinetic optimization and safety assessment.

Ubiquitin Screening & Profiling Services

We provide ubiquitin system assays covering E1, E2, and E3 enzymes as well as deubiquitinases. These services enable the discovery of modulators for protein degradation pathways, supporting innovative therapeutic strategies.

Service Workflow

Our service is structured into sequential yet flexible phases. Each project is customized based on client objectives, therapeutic area, and target class.

1

Target Identification and Validation

  • Literature mining, database integration, and clinical relevance analysis
  • Experimental validation using CRISPR, RNAi, and proteomics
  • Prioritization of targets with druggability scoring and safety profiling
2

Assay Development and Screening

  • Development of robust biochemical and cell-based assays
  • High-throughput screening of proprietary and client libraries
  • Hit confirmation and orthogonal validation
3

Hit-to-Lead Optimization

  • Medicinal chemistry to refine potency, selectivity, and ADME properties
  • In silico modeling integrated with iterative synthesis and testing
  • Pharmacological characterization in vitro and in vivo
4

Lead Candidate Selection

  • Efficacy validation in disease-relevant models
  • PK/PD optimization and safety assessment
  • IND-enabling studies to prepare for clinical translation

Applications

Our platform has been successfully applied across diverse therapeutic domains:

Oncology

Identification of kinase inhibitors targeting novel oncogenic drivers; development of small molecules disrupting protein–protein interactions in tumor signaling pathways.

Immunology

Discovery of selective modulators of immune checkpoints and cytokine signaling; validation of druggable nodes in autoimmune disease pathways.

Neurology

Targeting synaptic receptors and ion channels for neurodegenerative disorders; development of BBB-penetrant compounds with improved CNS selectivity.

Infectious Diseases

Identification of host-pathogen interaction targets; discovery of antivirals with novel mechanisms against resistant strains.

These case studies demonstrate the versatility of our approach and its adaptability to complex biological challenges.

Quality Assurance and Compliance

Ensuring data integrity and regulatory alignment is central to our service:

Quality Management Systems

SOP-driven workflows ensuring reproducibility and traceability

GLP and GMP Standards

Compliance with international regulatory guidelines

Data Security and Confidentiality

Secure data management systems protecting client IP

Analytical Rigor

Multiple orthogonal validation methods to reduce false positives

Our clients receive comprehensive project documentation, including assay protocols, raw data, and interpretive reports suitable for regulatory submission. We continuously upgrade our platform by incorporating these innovations, ensuring our clients remain at the forefront of therapeutic discovery.

Why Partner with Creative Biogene?

Seamless End-to-End Discovery

From target identification to preclinical candidate selection, all under one integrated platform.

Multimodal Expertise

Small molecules, biologics, RNA therapeutics, and bifunctional degraders supported by proprietary, diverse compound libraries.

Physiologically Relevant Models

Primary cells, 3D cultures, and high-content imaging ensure predictive, in vivo-like results.

Proactive Risk Management

Off-target profiling and polypharmacology analysis turn potential challenges into actionable insights.

True Partnership

We act as an extension of your R&D team, empowering decisions and accelerating project success.

Contact Us

Accelerate your drug discovery programs with our expertise and platform. Contact us today to discuss your target and learn how our Target-Based Drug Discovery Services can fast-track your clinical development.

FAQ

1. How do you ensure that a selected target is clinically relevant during the target identification and validation phase?

Our approach to ensuring clinical relevance is rooted in a comprehensive integration of systems biology and multi-omics data. We systematically correlate findings from human genetics, such as genome-wide association studies (GWAS) and rare mutation databases, with clinical sample data to establish a strong link between the target and the human disease pathophysiology. Furthermore, we employ advanced functional genomics, including CRISPR-based screening, and analyze protein-protein interaction networks to assess the target's centrality within disease-associated pathways. This multi-faceted strategy helps us prioritize targets that are not only mechanistically sound but also demonstrably significant in the clinical context, thereby minimizing the risk of pursuing targets with limited therapeutic potential.

2. What strategies are in place to mitigate false positives in high-throughput screening (HTS) campaigns?

We implement a rigorous, multi-tiered validation strategy to effectively eliminate false positives. Following the primary screen, all initial hits undergo immediate confirmation through dose-response curves to determine precise potency metrics (IC₅₀/EC₅₀). We then employ counter-screening assays specifically designed to identify and filter out compounds that interfere with the assay technology itself, such as fluorescent or reactive compounds. To proactively address off-target binding, we utilize chemical proteomics techniques to profile compound interactions across the proteome. Additionally, we integrate machine learning models, trained on extensive toxicological data, to predict and flag compounds with potential promiscuity or toxicity liabilities early in the process.

3. How do you proceed with structure-based optimization when a high-resolution 3D structure of the target is unavailable?

In the absence of an experimental crystal structure, we leverage a powerful combination of computational prediction and AI-driven design. We generate highly reliable structural models using state-of-the-art tools like AlphaFold2 or through sophisticated homology modeling. These models serve as a foundation for molecular dynamics simulations, which provide critical insights into the target's flexible regions and conformational dynamics. To inform the design process, we use generative AI models to propose novel molecular scaffolds with optimized binding characteristics. Furthermore, we employ experimental techniques like fragment-based screening and site-directed mutagenesis to probe the active site and validate computational predictions, ensuring a rational approach to optimization even without a starting crystal structure.

4. How is the challenge of polypharmacology addressed in your target-based discovery process?

We recognize that polypharmacology can be both a risk and an opportunity. To manage it systematically, we offer extensive selectivity profiling right from the hit-validation stage. This includes screening against dedicated panels for major target families such as kinases, GPCRs, and ion channels. For a broader, unbiased assessment, we use chemical proteomics to map a compound's interaction profile across thousands of proteins. Crucially, we integrate phenotypic readouts in disease-relevant cellular models early on to determine whether a multi-target profile translates into a therapeutic synergistic effect or poses an unacceptable risk of off-target toxicity, allowing for informed decision-making.

5. Do you support target discovery for complex diseases involving intricate biology, such as neurodegenerative disorders or the tumor microenvironment?

Absolutely. We have developed a specialized suite of advanced cellular models to tackle the complexity of such diseases. Our capabilities include utilizing induced pluripotent stem cell (iPSC)-derived neurons, glial cells, and various other somatic cell types to create patient-specific models. We further enhance physiological relevance by employing 3D culture systems, such as organoids and spheroids, which better mimic the tissue architecture and cellular heterogeneity of human diseases. For studying systemic interactions, we leverage organ-on-a-chip technology. To pinpoint targets within these complex systems, we integrate our assays with high-resolution and spatial transcriptomic analyses, enabling the discovery of targets that are specific to defined cell types or localized microenvironments.

6. What methodologies are used to distinguish a true "driver" target from a passive "passenger" in validation studies?

Distinguishing driver from passenger events is a critical step. We employ a dual strategy of functional gain-of-function and loss-of-function studies using precise genetic tools like CRISPR activation (CRISPRa) and interference (CRISPRi) to modulate target expression levels and observe the consequent phenotypic impact. This is coupled with deep molecular profiling—including transcriptomics and proteomics—to confirm the activation or suppression of expected downstream pathways upon target modulation. The most promising targets are then validated in vivo using relevant animal models to establish a definitive causal link between the target and the disease phenotype.

7. What approaches are used to accelerate the critical transition from an initial Hit to a qualified Lead compound?

We accelerate the hit-to-lead journey through a parallelized, data-driven optimization cycle. Instead of sequential steps, we conduct Structure-Activity Relationship (SAR) studies alongside early Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) profiling to avoid late-stage failures due to poor drug-like properties. Automation and microfluidic-based synthesis platforms enable rapid compound iteration. We also incorporate the concept of Structure-Tissue Exposure/Selectivity-Activity Relationship (STAR) to guide the optimization of tissue targeting and selectivity. Underpinning all this is the use of AI-based predictive models that prioritize the synthesis of compounds with the highest probability of success.

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