Target-Based Screening (TBS)
INQUIRYBOC Sciences is committed to providing global clients with efficient and precise target-based screening services, covering multiple key drug target classes such as GPCRs, kinases, nuclear receptors, and ion channels. Relying on advanced high-throughput screening platforms and diversified detection technologies, we have established a comprehensive system that includes enzymatic screening, binding affinity analysis, cell-based functional screening, and structure-assisted virtual screening. These support the entire process from lead compound discovery to mechanism-of-action studies. We possess integrated capabilities in target protein expression, stable cell line development, virtual screening modeling, hit compound validation, and structural optimization, enabling clients to efficiently identify and optimize candidate molecules and accelerate drug development progress.
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Service Highlights and Advantages
- Target gene cloning, expression, and protein purification.
- Development of functional screening models at in vitro and cellular levels.
- Automated high-throughput screening (HTS) and medium-throughput screening (MTS) platforms.
- Various screening detection technologies (fluorescence, colorimetry, radioactivity, tagged enzymes, BRET, etc.).
- Hit compound validation and mechanism-of-action studies.
- Preliminary structure-activity relationship (SAR) assessment and optimization support.
Target-Based Screening Services from BOC Sciences
BOC Sciences has extensive experience in target construction, screening model development, high-throughput screening, and mechanism studies. We provide end-to-end target screening services covering GPCRs (G-protein-coupled receptors), kinases, nuclear receptors, and ion channels. These services deliver efficient and reliable solutions to clients in the fields of biomedicine, precision medicine, neuroscience, oncology, and anti-infectives.
GPCR Screening Services
BOC Sciences has established an advanced GPCR target screening platform, integrating radioligand binding, fluorescence resonance energy transfer (FRET), cAMP, and calcium flux detection technologies. We support high-throughput screening for agonists, antagonists, and allosteric modulators, covering both classical and orphan GPCR targets, with capabilities for rapid and highly sensitive screening.
Kinase Screening Services
BOC Sciences offers a diverse kinase target library covering Ser/Thr kinases and tyrosine kinases. Utilizing platforms such as TR-FRET, AlphaLISA, and fluorescence polarization, we enable multi-target parallel screening and quantitative analysis. Our services support high-throughput kinase inhibitor discovery and subsequent SAR optimization, meeting the needs of oncology and immunology-related projects.
Nuclear Receptor Screening Services
BOC Sciences is equipped with various cell-based and cell-free nuclear receptor screening systems. Using reporter gene assays, EMSA, and electrophoretic analysis, we accurately screen ligands for nuclear receptors including PPAR, LXR, FXR, and RAR. These services are applicable to research in metabolism, oncology, and immune regulation, offering customizable screening solutions.
Ion Channel Screening Services
BOC Sciences possesses automated patch-clamp and fluorescent membrane potential detection platforms, covering various targets including potassium, sodium, and calcium channels. We support electrophysiological function evaluation and small molecule modulator screening. Combined with AI-assisted analysis technologies, our platform ensures high-throughput and high-accuracy performance, catering to the drug discovery needs in the neurological and cardiovascular fields.
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BOC Sciences integrates innovative technologies to empower your drug discovery with strong momentum, fully dedicated to building next-generation drug screening platforms.
Target-Based Screening Platform at BOC Sciences
BOC Sciences features a professional screening platform backed by an interdisciplinary research team integrating structural biology, pharmacology, and molecular biology. We offer one-stop TBS services, ranging from target construction, expression, functional validation, and screening model development to compound screening, hit verification, and mechanism elucidation. Our core service modules include:
Target Selection and Validation
- Target Evaluation and Selection: Based on the client's research focus and literature data, we assist in identifying disease-related targets with clinical potential.
- Target Cloning and Expression: Target proteins are expressed using E. coli, mammalian cells, insect cells, or yeast systems.
- Purification and Functional Validation: High-purity separation is achieved via chromatography and tag protein techniques to ensure target activity for screening purposes.
High-Throughput Screening Platform
- Enzymatic Activity Screening: Establishment of highly sensitive enzymatic screening systems, suitable for a wide range of enzyme targets including kinases and proteases.
- Binding Affinity Screening: Techniques such as SPR, MST, and FP are employed to accurately measure binding affinity and kinetics between molecules and targets.
- Cell-Based Screening: Evaluation of the agonistic or inhibitory effects of small molecules using cell lines expressing the target.
- Structure-Based Screening: Virtual screening of potential small-molecule ligands using 3D structural modeling and molecular docking techniques.
Compound Resource Support
- A compound library comprising over 1 million structurally diverse and drug-like molecules.
- Coverage includes natural products, small molecule inhibitors, fragment compounds, polymer-modified molecules, etc.
- Custom screening libraries tailored to specific targets or structural categories can also be provided.
Hit Compound Analysis and Validation
- Secondary validation assays (IC₅₀/EC₅₀ determination).
- Target selectivity and in vitro stability tests.
- Preliminary Structure-Activity Relationship (SAR) analysis.
- Compound synthesis and optimization suggestions.
- Binding site prediction and mechanism studies (e.g., CETSA, Pull-Down, EMSA, etc.).
Project Workflow
Communication and Project Assessment
Prior to project initiation, the technical team will conduct in-depth communication with the client to clarify research goals, target types (e.g., GPCRs, kinases, nuclear receptors, ion channels), screening methods (enzymatic, affinity-based, cell function-based), and detection platforms. A preliminary feasibility and timeline assessment will be performed.
Customized Screening Strategy Design
Based on client requirements and target characteristics, we design the most appropriate screening strategy, select suitable experimental platforms (e.g., TR-FRET, AlphaLISA, FP, cell reporter gene systems), and define key experimental parameters and quality control standards to ensure scientific rigor and practical implementation.
Method Development and Pre-Validation
Before large-scale screening, small-scale method validation experiments are conducted, including reaction condition optimization, signal window evaluation, and positive/negative control setup, ensuring system stability, good reproducibility, and suitability for high-throughput screening.
High-Throughput Screening Execution
Using the optimized experimental system, large-scale compound library screening is conducted to evaluate the activity of various candidate molecules against the target. Optional modules include primary screening, re-screening, concentration-gradient testing, and secondary screening, ensuring the reliability of hit compounds.
Data Analysis and Result Reporting
After experiments are completed, a comprehensive analysis report is provided, including hit results, active molecule selection criteria, preliminary SAR analysis, and recommended directions for further optimization, aiding clients in rapidly identifying potential candidates.
Follow-Up Verification and Extended Services
BOC Sciences also offers follow-up services such as mechanism studies, target validation, secondary target testing, and in vitro pharmacodynamic evaluations to help clients advance from hit compounds to druggable molecules efficiently.
Applications of Target-Based Screening Services
Lead Compound Discovery for New Drugs
Leveraging a well-established TBS platform, BOC Sciences can rapidly identify lead compounds active against specific targets from large-scale compound libraries. This service is widely applied in early-stage drug development, significantly enhancing the efficiency of candidate molecule identification and laying the groundwork for subsequent pharmacological optimization and druggability research.
Structure Optimization and SAR Studies
Through in-depth SAR analysis of hit compounds, BOC Sciences supports clients in rational structure optimization. By integrating multiple rounds of target screening and control experiments, we improve selectivity, binding affinity, and metabolic stability of small molecules, accelerating the drug optimization process.
Target Validation and Mechanism of Action Studies
Utilizing target-specific screening systems, BOC Sciences validates small molecule mechanisms of action and clarifies regulatory relationships with the target, supporting target biology research and novel target identification. This contributes to elucidating drug mechanisms and evaluating therapeutic potential.
Drug Repositioning and Combination Screening
BOC Sciences offers multi-target screening for known drugs or clinical candidates to explore potential new indications. Additionally, combination screening services are available to identify multi-component therapies with synergistic effects, expanding therapeutic strategies.
FAQs
What types of target screening services does BOC Sciences offer?
We offer screening services for a wide range of targets including GPCRs, kinases, nuclear receptors, ion channels, etc., covering enzymatic, affinity, cell function, and structure-based screening technologies.
Do you support customized screening conditions or systems?
Yes. We provide highly customized services and can design screening strategies based on client-supplied target information, expression systems, screening throughput, and detection methods, flexibly addressing various R&D needs.
What are the scale and types of compound libraries available for screening?
We can screen compound libraries ranging from tens of thousands to hundreds of thousands, including commercial small molecule libraries, natural product libraries, and library-derived compound sets. Client-supplied compounds can also be incorporated into the screening process.
Are hit compound validation and follow-up services provided during screening?
Yes. We provide re-screening, dose-response analysis, mechanism studies, and can extend services to pharmacodynamic validation, SAR analysis, synthesis optimization, and ADMET evaluation.
Can I commission only part of the screening process, such as hit validation or affinity measurement?
Yes. Our services are highly flexible. Clients can select complete workflows or individual services, such as re-screening validation, SPR affinity analysis, IC₅₀/EC₅₀ determination, etc.
Is structure-based virtual screening (SBVS) available?
Yes. We have a high-performance computing platform and an experienced computational chemistry team, offering molecular docking, pharmacophore modeling, and virtual screening services based on 3D structures or homology models.
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